Dr. Shailendra K Saraf, M.Pharm.,Ph.D.,LL.B. - Babu Banarasi Das Northern India Institute of Technology - Professor & Director(Pharmacy)

Dr. Shailendra K Saraf

M.Pharm.,Ph.D.,LL.B.

Babu Banarasi Das Northern India Institute of Technology

Professor & Director(Pharmacy)

Lucknow, U.P. | India

Additional Specialties: Pharmaceutical Chemistry, Pharmaceutical Analysis, Natural Products

ORCID logohttps://orcid.org/0000-0002-0569-1213

Dr. Shailendra K Saraf, M.Pharm.,Ph.D.,LL.B. - Babu Banarasi Das Northern India Institute of Technology - Professor & Director(Pharmacy)

Dr. Shailendra K Saraf

M.Pharm.,Ph.D.,LL.B.

Introduction

Shailendra K. Saraf did his Bachelor’s, Master’s and Doctoral degrees from Department of Pharmaceutical Sciences, Dr. H. S. Gour Vishwavidyalaya, Sagar and HNB Garhwal Central University, Srinagar. He further did his Bachelor’s degree in Law from Lucknow University. He is a Professor of Pharmaceutical Chemistry and presently working as Director (Pharmacy), Babu Banarasi Das Northern India Institute of Technology, Lucknow (UP), INDIA. Presently, he is also the Dean-Pharmacy and Convenor of BOS-Pharmacy of Dr. A.P.J. Abdul Kalam Technical University, Lucknow, INDIA. He has more than twenty seven years of industrial, teaching and research experience.
His major research interests have been in the areas related to Synthetic Medicinal Chemistry, Phytopharmaceutical Chemistry and Nanochemistry. He is the Affiliation Coordinator in the MOU with Eli-Lilly & Company for the Open Innovation Drug Discovery (OIDD) program.
He has guided more than a hundred M. Pharm. dissertations and many research scholars for Ph. D. He has published more than 75 papers in national and international journals. He is a co-author of fifteen books/book chapters at international level and is the Principal Investigator for two AICTE funded projects. He has delivered more than two dozen invited/plenary lectures at national and international conferences. He is a recipient of six prestigious awards. He is a reviewer and advisory board member of various international and national journals and has been associated with academic work and various committees of different Governing bodies like PCI, CSIR, etc. He is a life member of IPA, APTI, IPGA, LASAI, IHPA, Society of Pharmacovigilance (India) and MRS, Singapore.

Primary Affiliation: Babu Banarasi Das Northern India Institute of Technology - Lucknow, U.P. , India

Additional Specialties:

Education

Mar 2009
Lucknow University
LL.B.
May 2005
H.N.B. Garhwal University
Ph.D.
Jan 1999 - Jan 2005
H.N.B.Garhwal University
Ph.D.
Pharm.Chem.
Aug 1989 - Jul 1991
Dr.Hari Singh Gour University
M.Pharm.
Department of Pharmaceutical Sciences
Jul 1991
Saugor University
M.Pharm.
Aug 1985 - Jul 1989
Dr.Hari Singh Gour University
B.Pharm.
Department of Pharmaceutical Sciences
Jul 1989
Saugor University
B.Pharm.

Experience

Mar 2001
B.B.D.N.I.I.T.
Professor & Director(Pharmacy)
Pharmacy

Publications

74Publications

435Reads

-Profile Views

55PubMed Central Citations

PHD-2 activation: a novel strategy to control HIF-1α and mitochondrial stress to modulate mammary gland pathophysiology in ER+ subtype.

Naunyn Schmiedebergs Arch Pharmacol 2019 Jun 1. Epub 2019 Jun 1.

Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University (A Central University), VidyaVihar, Raebareli Road, Lucknow, UP, 226025, India.

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http://dx.doi.org/10.1007/s00210-019-01658-7DOI Listing
June 2019
14 Reads
2.471 Impact Factor

Schizonticidal antimalarial sesquiterpene lactones from Magnolia champaca (L.) Baill. ex Pierre: microwave-assisted extraction, HPTLC fingerprinting and computational studies.

Nat Prod Res 2019 Feb 31;33(4):568-572. Epub 2017 Oct 31.

a Faculty of Pharmacy, Division of Pharmaceutical Chemistry , Babu Banarasi Das Northern India Institute of Technology , Lucknow , India.

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http://dx.doi.org/10.1080/14786419.2017.1396595DOI Listing
February 2019
7 Reads
0.919 Impact Factor

Novel 2-(Substituted Phenyl Imino)-5-Benzylidene-4-Thiazolidinones As Possible Non-Ulcerogenic Tri-Action Drug Candidates: Synthesis, Characterization, Biological Evaluation And Docking Studies

Medicinal Chemistry Research

The present research was aimed at the synthesis and screening of 35 novel 2-(substituted phenyl imino)-5-benzylidene-4-thiazolidinones having different substitutions at imino phenyl and arylidene groups. The title compounds were synthesized by Knoevenagel condensation at the 5th position of the 4-thiazolidinone ring, in the presence of sodium acetate. The structures were assigned on the basis of spectral data. The compounds were screened for in vivo anti-inflammatory, antinociceptive and in vitro free-radical scavenging activities. The compounds exhibited significant activities when compared with standard drugs. The distinctive property of the derivatives was that none of them had an acidic group, like conventional NSAIDs, but exhibited significant in vivo activity in acute inflammation models. Further, the active compounds of each series were docked against cyclooxygeanase (COX)-2 enzyme using Glide module of Maestro 11.1 program. It was evident from the docking results that 3-chlorophenylimino and 2-chloro moiety on 5-benzylidene nucleus of the 4-thiazolidinone derivative (30) could easily fit into the COX-2-binding pocket, considered as critical interaction for COX-2 inhibition. Interestingly, some of the compounds exhibited the potential of becoming dual action or even triple action drug candidates, which could target degenerative disorders associated with excessive free-radical generation.

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January 2019
3 Reads

Development of Some Quinolone/Fluoroquinolone- Latentiated Drug Polypeptide Systems and Their Antimicrobial Evaluation

International Journal of Chem. Tech. Research

The present study envisages to synthesize and evaluate some Quinolone/Flouroquinolone-polypeptide conjugates and to investigate whether, such drug latentiated systems possess any biological activity (antimicrobial) by themselves and to what extent the physical properties of these conjugates vary with different polypeptides. To accomplish this, four established antibiotics namely Nalidixic acid (NDA), Norfloxacin (NFC), Ciprofloxacin (CFC) and Ofloxacin (OFC) were conjugated with two different polypeptides, polyglutamic acid (PGA) and polyaspartic acids (PAA), respectively and evaluated for their physicochemical properties as well as antimicrobial action. The synthesized derivatives were characterized by various physicochemical and other methods. The partition coefficient of the NFC-PGA derivative was found to be highest amongst others. The rates of hydrolysis in simulated gastric and intestinal fluids showed that latentiated derivatives were resistant to hydrolysis in the gastric fluid but show hydrolysis in the intestinal fluid. Finally, the synthesized drug conjugates were screened for antibacterial activity, at concentrations of 10 and 50 μg/mL concentrations, against P. morganii and S. aureus bacterial strains using agar diffusion (filter paper disc) method. Almost all the drug-polymer conjugates showed good antibacterial potency but in particular, CFC and OFC conjugates of PGA exhibited maximum zone of inhibition against both the Gram positive as well as Gram negative microorganisms. The enhanced antibacterial potency activities observed for all the latentiated derivatives can be attributed to the synergistic effect of drug and polypeptides. Especially, improved activities of NDA-PGA and NDA-PAA against S. aureus was possible only due to conjugation with the polypeptides because NDA is not effective against Gram positive microorganisms.

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November 2018
1 Read

Assessment of improved buccal permeation and bioavailability of felodipine microemulsion-based cross-linked polycarbophil gel.

Drug Deliv Transl Res 2018 06;8(3):591-601

Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University (A Central University), VidyaVihar, Raebareli Road, Lucknow, UP, 226025, India.

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http://link.springer.com/10.1007/s13346-018-0489-5
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http://dx.doi.org/10.1007/s13346-018-0489-5DOI Listing
June 2018
22 Reads

Privileged scaffolds as MAO inhibitors: Retrospect and prospects.

Eur J Med Chem 2018 Feb 4;145:445-497. Epub 2018 Jan 4.

Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, UP, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2018.01.003DOI Listing
February 2018
52 Reads
1 Citation
3.450 Impact Factor

Privileged scaffolds as MAO inhibitors: Retrospects and prospects

European Journal of Medicinal Chemistry

This review aims to be a comprehensive, authoritative, critical, and readable review of general interest to the medicinal chemistry community because it focuses on the pharmacological, chemical, structural and computational aspects of diverse chemical categories as monoamine oxidase inhibitors (MAOIs). Monoamine oxidases (MAOs), namely MAO-A and MAO-B represent an enormously valuable class of neuronal enzymes embodying neurobiological origin and functions, serving as potential therapeutic target in neuronal pharmacotherapy, and hence we have coined the term “Neurozymes” which is being introduced for the first time ever. Nowadays, therapeutic attention on MAOIs engrosses two imperative categories; MAO-A inhibitors, in certain mental disorders such as depression and anxiety, and MAO-B inhibitors, in neurodegenerative disorders like Alzheimer's disease (AD) and Parkinson's disease (PD). The use of MAOIs declined due to some potential side effects, food and drug interactions, and introduction of other classes of drugs. However, curiosity in MAOIs is reviving and the recent developments of new generation of highly selective and reversible MAOIs, have renewed the therapeutic prospective of these compounds. The initial section of the review emphasizes on the detailed classification, structural and binding characteristics, therapeutic potential, current status and future challenges of the privileged pharmacophores. However, the chemical prospective of privileged scaffolds such as; aliphatic and aromatic amines, amides, hydrazines, azoles, diazoles, tetrazoles, indoles, azines, diazines, xanthenes, tricyclics, benzopyrones, and more interestingly natural products, along with their conclusive SARs have been discussed in the later segment of review. The last segment of the article encompasses some patents granted in the field of MAOIs, in a simplistic way.

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February 2018
5 Reads

N1-Benzenesulfonyl-2-Pyrazoline Hybrids In Neurological Disorders: Syntheses, Biological Screening And Computational Studies

EXCLI Journal

A novel series of 1,3,5-trisubstituted-2-pyrazolines (5a-5t) was prepared via Claisen Schmidt condensation, followed by heterocyclization with hydrazine hydrate, substitution of N1 hydrogen of 2-pyrazoline nucleus with 4-chlorobenzenesulfonylchloride, applying conventional and green chemistry approaches. Among the two, microwave assisted organic synthesis (MAOS) emerged as a better synthetic tool in terms of faster reaction rate and high yield. Various physicochemical and spectral studies were conducted to characterize the synthesized derivatives including- IR, Mass, 1H-NMR, 13C-NMR and elemental analysis. During pharmacological evaluation, compound 5b showed excellent anti-anxiety activity and compound 5k exhibited the best antidepressant effect at the tested doses, 50 and 100 mg/kg b.w., being comparable to diazepam and imipramine, respectively. The docking experiments confirmed the probable mechanism of neuropharmacological action, showing excellent affinity towards MAO-A target protein, which was also evidenced from some of the key interactions with binding site residues Ala68, Tyr69 and Phe352. Furthermore, complimentary in silico pharmacokinetic recital without any potential risk of neurotoxicity (as evaluated by rotarod and actophotometer tests), or carcinogenicity, mutagenicity, reproductive toxicity, acute toxicity and irritancy (as predicted by LAZAR and OSIRIS programs) signified their probable use in depression and anxiety disorders.

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February 2018
6 Reads

Schizonticidal antimalarial sesquiterpene lactones from Magnolia champaca (L.) Baill. ex Pierre: microwave-assisted extraction, HPTLC fingerprinting and computational studies

Natural Product Research

The present study explored the schizonticidal potential of traditionally used Magnolia champaca (L.) Baill. ex. Pierre flowers, identifying constituents of interest. The extraction of phytoconstituents was carried out by microwave-assisted technique, isolated via column chromatography, and characterised by various physicochemical, spectral (IR, 1H-NMR and Mass) and chromatographic (HPTLC) techniques. Both the isolated compounds (parthenolide and costunolide diepoxide) exhibited potent schizonticidal antimalarial activity during primary screening in rodent models, with maximum parasitaemia suppression (85.18% and 83.65%, respectively) at a dose of 20 mg/kg body weight when compared to the standard drugs chloroquine and artesunate. In silico techniques were employed to identify the probable biological target and mechanism of action of these isolated compounds. Molecular docking studies also predicted the binding orientations and multi-targeted action of these compounds, in particular costunolide diepoxide with maximum affinity towards SERCA and DHFR proteins. Additionally, favourable in silico ADMET parameters were envisaged through various computational programmes.

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November 2017
6 Reads

2-Pyrazoline Derivatives In Neuropharmacology: Synthesis, Adme Prediction, Molecular Docking And In-Vivo Biological Evaluation

EXCLI Journal

A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives (PFC-1 to PFC-16) were synthesized in a three step reaction using conventional and microwave assisted green chemistry approach. The synthesized derivatives were characterized and their chemical structures were established by various physicochemical methods such as IR, Mass, 1H-NMR, 13C-NMR and elemental analysis. The synthesized compounds were tested for their neuropharmacological potential. The compounds exhibited significant antidepressant and anti-anxiety activities against various behavioral in vivo models. Compounds PFC-3 and PFC-12 were found to be the most active derivatives in the series. The 2-pyrazoline analogs, having 2-hydroxyphenyl and anthracen-9-yl substitution at 3rd position while 4-benzyloxyphenyl and 4-methylphenyl substitution at 5th position, were decisive in eliciting good antidepressant and anxiolytic properties, respectively. The docking experiments revealed that the synthesized derivatives were potential inhibitors of MAO-A protein, which plays a central role in managing depression and anxiety disorders. The most potent derivatives were found to be involved in some key interactions with Tyr407, Tyr444, Phe352 and Ala68 amino acid residues at the binding site of MAO-A protein. All the synthesized derivatives successfully passed the pharmacokinetic barriers of absorption, distribution, metabolism and elimination as predicted using in silico techniques without showing any substantial indication of acute and neurotoxicity. This was further confirmed in the laboratory by performing acute toxicity studies as per OECD guidelines.

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May 2017
6 Reads

Synthesis and Development of Some Biodegradable Polypeptides as Antimicrobial Agents

International Journal of ChemTech Research

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March 2017
6 Reads

Schiff Bases of Benzothiazol-2-ylamine and Thiazolo[5,4-b] pyridin-2-ylamine as Anticonvulsants: Synthesis, Characterization and Toxicity Profiling.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):240-248

Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Sector-2, Dr. Akhilesh Das Nagar, Faizabad Road, Lucknow, 227105, U.P., India.

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February 2017
38 Reads

Isolation and characterization of quinine from : A new marker approach to identify substitution and adulteration.

J Adv Pharm Technol Res 2016 Oct-Dec;7(4):153-158

Department of Herbal Drug Technology, University Centre of Excellence in Research, Baba Farid University of Health Sciences, Faridkot, Punjab, India.

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http://dx.doi.org/10.4103/2231-4040.191427DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5052943PMC
November 2016
42 Reads
2 Citations

Bioactive non-sterol triterpenoid from Streblus asper: microwave-assisted extraction, HPTLC profiling, computational studies and neuro-pharmacological evaluation in BALB/c mice.

Pharm Biol 2016 Nov 6;54(11):2454-2464. Epub 2016 Apr 6.

a Division of Pharmaceutical Chemistry, Faculty of Pharmacy , Babu Banarasi Das Northern India Institute of Technology , Lucknow , UP , India.

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http://dx.doi.org/10.3109/13880209.2016.1160132DOI Listing
November 2016
17 Reads
1 Citation
1.340 Impact Factor

Process optimization and photostability of silymarin nanostructured lipid carriers: effect on UV-irradiated rat skin and SK-MEL 2 cell line.

Drug Deliv Transl Res 2016 10;6(5):597-609

Babasaheb Bhimrao Ambedkar University, Lucknow, UP, India.

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http://dx.doi.org/10.1007/s13346-016-0317-8DOI Listing
October 2016
33 Reads
1 Citation

Phytochemical, chromatographic and spectroscopic investigation of Carum copticum seeds and their potential as immunomodulatory agents.

Pharm Biol 2016 1;54(3):494-502. Epub 2015 Jun 1.

c Faculty of Pharmacy , Babu Banarasi Das Northern India Institute of Technology , Lucknow , Uttar Pradesh , India.

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http://dx.doi.org/10.3109/13880209.2015.1050116DOI Listing
October 2016
33 Reads
1.340 Impact Factor

Structural Insights into the Molecular Design of HER2 Inhibitors

Open Pharmaceutical Sciences Journal

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July 2016
11 Reads

Novel 4-Thiazolidinone Derivatives as Anti-Infective Agents: Synthesis, Characterization, and Antimicrobial Evaluation.

Biochem Res Int 2016 26;2016:8086762. Epub 2016 Jan 26.

Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Sector-II, Dr. Akhilesh Das Nagar, Faizabad Road, Lucknow, Uttar Pradesh 227105, India.

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http://dx.doi.org/10.1155/2016/8086762DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4746384PMC
February 2016
31 Reads

An Expeditious One-Pot Microwave Facilitated Versus Conventional Syntheses, In-vivo Biological Screening and Molecular Docking Studies of Some 3,5-Disubstituted-4,5-Dihydro-(1H)-Pyrazole Derivatives

Medicinal Chemistry Research

A series of 3,5-disubstituted-2-pyrazoline derivatives (2a–2t) were synthesized by reacting different aromatic/heteroaromatic aldehydes and ketones, in a two step reaction through Claisen Schmidt condensation, followed by cyclization of the resulted chalcones with hydrazine hydrate in the presence of a base using conventional and microwave approaches. The synthesized derivatives were characterized by various physicochemical methods, and their chemical structures were established by IR, Mass, 1H-NMR, 13C-NMR spectroscopic data and elemental analysis. The antidepressant with tail suspension test and forced swim test and anti-anxiety with Elevated Plus Maze Test activities were evaluated using suitable animal models. Compounds 2i, and 2j showed noticeable antidepressant activity, by reducing the duration of immobility in both the tests, while compounds 2a and 2b were found to possess good anxiolytic activity, by increasing the number of arm entries and open arm exploratory time at the tested doses (50 and 100 mg/kg b.w.), when compared to the standard drugs imipramine and diazepam, respectively. In order to ascertain the binding interactions of the synthesized derivatives to the MAO-A target protein, molecular docking was employed which demonstrated the key interactions with the amino acid residues Asn181, Phe208, Tyr69, Tyr197, Tyr444 and Met445 at the binding site. In addition, the most active derivatives 2i and 2b showed some imperative conserved interactions of the PDB co-crystal ligand 2Z5X with the amino acid residues at the binding site of MAO-A protein.The results of the study also demonstrated that the Glide gscores of the synthesized derivatives were in close correlation with the in vivo biological activity data, in particular with the forced swim test of the antidepressant activity with a very good correlation coefficient of 0.754103. Furthermore, the ADME properties of the synthesized derivatives were predicted and found to be within the affirmed limits.

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January 2016
8 Reads

Novel 4-Thiazolidinone Derivatives as Anti-infective Agents: Synthesis, Characterization and Antimicrobial Evaluation

Biochemistry Research International

A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600

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January 2016
5 Reads

Stability Indicating RP-HPLC Method for Simultaneous Estimation of Antidiabetic and Antihypertensive Drugs

Rasayan Journal of Chemistry

A new simple, selective, accurate, rapid, stability indicating High Performance Liquid Chromatographic (HPLC) method was developed and validated for the analysis of such a combination of losartan potassium, glimepiride and metformin. Chromatographic separation was achieved isocratically on C18 column [PRINCETON SPHER – 100, (100 A0- 5μm, 150 mm x 4.6 i.d.).] utilizing a mobile phase composition of 10 mM disodium hydrogen phosphate and 10 mM sodium dodecyl sulphate buffer and acetonitrile (68:32, v/v), with a pH of 7.5 (adjusted with orthophosphoric acid) at a flow rate of 1.0 mL/min, with UV detection at 230 nm. The calibration graphs were linear with r2 >0.999 and % RSD> 3 for intra-day and inter-day precision. The retention time of losartan, glimepiride and metformin was 1.39, 4.27, 9.36 min., respectively. The limit of detection and limit of quantitation for losartan, glimepiride and metformin was 0.0382, 0.00473, 0.09331 and 0.1273, 0.0157, 0.31104 respectively. The drugs were subjected to various stress conditions, as per ICH guidelines. The stability indicating studies showed that neither the degradation products nor the excipients interfered in the estimation of drugs. Hence, this method was specific and can be successfully used for the estimation of these drugs in combined dosage forms.

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August 2015
5 Reads

Carbon Nanotropes: The Contemporary Paradigm in Drug Delivery

Materials 2015, 8, 3068-3100; doi:10.3390/ma8063068

Materials

Discovery of fullerenes and other nanosized carbon allotropes has opened a vast new field of possibilities in nanotechnology and has become one of the most promising research areas. Carbon nanomaterials have drawn interest as carriers of biologically pertinent molecules due to their distinctive physical, chemical and physiological properties. We have assigned the nomenclature “Carbon Nanotropes” to the nanosized carbon allotropes. Carbon nanotropes such as fullerenes, carbon nanotubes (CNTs) and graphenes, have exhibited wide applicability in drug delivery, owing to their small size and biological activity. The nanotherapeutics/diagnostics will allow a deeper understanding of human ills including cancer, neurodegenerative diseases, genetic disorders and various other complications. Recently, nanomaterials with multiple functions, such as drug carrier, MRI, optical imaging, photothermal therapy, etc., have become more and more popular in the domain of cancer and other areas of research. This review is an endeavor to bring together the usefulness of the carbon nanomaterials in the field of drug delivery. The last section of the review encompasses the recent patents granted on carbon nanotropes at United State Patent Trademark Office (USPTO) in the related field.

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June 2015
6 Reads

Immunomodulatory Activity of Fruit Rinds of Garcinia indica (Family Guttiferae) on Swiss Albino Mouse Model

International Journal of Pharmacognosy and Phytochemical Research

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June 2015
8 Reads

Ulcerogenicity devoid novel non steroidal anti-inflammatory agents (NSAIDS): syntheses, computational studies and activity of 5-aryliden-2-imino-4-thiazolidinones

Medicinal Chemistry Research

A series of new 5-aryliden-2-imino-4-thiazolidinones (5a-e and 6a-e) were synthesized via a three step reaction and characterized by physicochemical and spectral data. The uniqueness of the derivatives lies in the fact that none of them had an acidic group, like conventional NSAIDS, but exhibited significant in vivo activity in acute inflammation models. In particular, 5-(3-chlorobenzyliden)-2-(pyridin-2-yl-imino)-4-thiazolidinone(5a) and 5-(3-chlorobenzyliden)-2-(5-methylisoxazol-3-yl-imino)-4-thiazolidinone (6a) showed remarkable paw oedema inhibition (67.76% and 74.47% oedema inhibition respectively, after 3h) comparable to that of Ibuprofen (74.56% oedema inhibition, after 3h) at half of the dose of the standard drug. Also, compounds 5a (72.86%) and 6a (80.20%) were found to possess significant inhibition of albumin denaturation when screened for in vitro anti-inflammatory activity. In addition, these compounds were docked into the known active site of COX-2 protein using Glide XP and QPLD algorithms and the binding-free energy was calculated using Prime MM/GBSA simulation methods. The combined use of molecular docking and MM/GBSA methods gave a good correlation between the predicted binding-free energy and experimentally determined biological activities. It was also evident from the docking results that 2-methylisoxazolylimino or 2-(pyridin-2-yl-imino substitution and 3-chloro moiety on 5-benzylidin nucleus of these 4-thiazolidinone derivatives can easily occupy the COX-2 binding pocket, considered as the critical interaction for COX-2 inhibition. Moreover, pharmacokinetic properties of all the synthesized compounds were predicted, with good results. Further, the synthesized derivatives showed neither acute toxicity nor symptoms of gastric ulceration, at extended doses, owing to the absence of an acidic group. Ulcerogenicity devoid novel non steroidal anti-inflammatory agents (NSAIDS): Syntheses, computational studies and activity of 5-aryliden-2-imino-4-thiazolidinones - ResearchGate. A series of new 5-aryliden-2-imino-4-thiazolidinones (5a-e and 6a-e) were synthesized via a three step reaction and characterized by physicochemical and spectral data. The uniqueness of the derivatives lies in the fact that none of them had an acidic group, like conventional NSAIDS, but exhibited significant in vivo activity in acute inflammation models. In particular, 5-(3-chlorobenzyliden)-2-(pyridin-2-yl-imino)-4-thiazolidinone(5a) and 5-(3-chlorobenzyliden)-2-(5-methylisoxazol-3-yl-imino)-4-thiazolidinone (6a) showed remarkable paw oedema inhibition (67.76% and 74.47% oedema inhibition respectively, after 3h) comparable to that of Ibuprofen (74.56% oedema inhibition, after 3h) at half of the dose of the standard drug. Also, compounds 5a (72.86%) and 6a (80.20%) were found to possess significant inhibition of albumin denaturation when screened for in vitro anti-inflammatory activity. In addition, these compounds were docked into the known active site of COX-2 protein using Glide XP and QPLD algorithms and the binding-free energy was calculated using Prime MM/GBSA simulation methods. The combined use of molecular docking and MM/GBSA methods gave a good correlation between the predicted binding-free energy and experimentally determined biological activities. It was also evident from the docking results that 2-methylisoxazolylimino or 2-(pyridin-2-yl-imino substitution and 3-chloro moiety on 5-benzylidin nucleus of these 4-thiazolidinone derivatives can easily occupy the COX-2 binding pocket, considered as the critical interaction for COX-2 inhibition. Moreover, pharmacokinetic properties of all the synthesized compounds were predicted, with good results. Further, the synthesized derivatives showed neither acute toxicity nor symptoms of gastric ulceration, at extended doses, owing to the absence of an acidic group. Ulcerogenicity devoid novel non steroidal anti-inflammatory agents (NSAIDS): Syntheses, computational studies and activity of 5-aryliden-2-imino-4-thiazolidinones - ResearchGate. Available from: A series of new 5-aryliden-2-imino-4-thiazolidinones (5a–e and 6a–e) were synthesized via a three-step reaction and characterized by physicochemical and spectral data. The uniqueness of the derivatives lies in the fact that none of them had an acidic group, like conventional NSAIDS, but exhibited significant in vivo activity in acute inflammation models. In particular, 5-(3-chlorobenzyliden)-2-(pyridin-2-yl-imino)-4-thiazolidinone(5a) and 5-(3-chlorobenzyliden)-2-(5-methylisoxazol-3-yl-imino)-4-thiazolidinone (6a) showed remarkable paw oedema inhibition (67.76 and 74.47 % oedema inhibition, respectively, after 3 h) comparable to that of Ibuprofen (74.56 % oedema inhibition, after 3 h) at half of the dose of the standard drug. Also, compounds 5a (72.86 %) and 6a (80.20 %) were found to possess significant inhibition of albumin denaturation when screened for in vitro anti-inflammatory activity. In addition, these compounds were docked into the known active site of COX-2 protein using Glide XP and QPLD algorithms, and the binding-free energy was calculated using Prime MM/GBSA simulation methods. The combined use of molecular docking and MM/GBSA methods gave a good correlation between the predicted binding-free energy and experimentally determined biological activities. It was also evident from the docking results that 2-methylisoxazolylimino or 2-(pyridin-2-yl-imino substitution and 3-chloro moiety on 5-benzylidin nucleus of these 4-thiazolidinone derivatives can easily occupy the COX-2 binding pocket, considered as the critical interaction for COX-2 inhibition. Moreover, pharmacokinetic properties of all the synthesized compounds were predicted, with good results. Further, the synthesized derivatives showed neither acute toxicity nor symptoms of gastric ulceration, at extended doses, owing to the absence of an acidic group.

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May 2015
10 Reads

Phytochemical investigation and anti-spermatogenic potential of Artocarpus lakoocha fruits

The Natural Products Journal

The present study was undertaken to investigate the preliminary phytochemical screening and antispermatogenic activity of different extracts of Artocarpus lakoocha Roxb fruits and the major constituent isolated from the active extract. The powdered plant material was defatted with petroleum ether and then successively extracted with chloroform, ethanol and distilled water. The prepared extracts were screened for the presence of various phytoconstituents, which showed the presence of alkaloids, steroids, carbohydrates, glycosides, saponin, protein and phenolic compounds. Petroleum ether, chloroform, ethanolic and aqueous extracts of Artocarpus lakoocha fruits were tested for their antispermatogenic potential, at the doses of 100, 200 and 300mg/kg, body weight, p.o., for 45 days. The chloroform extract of fruit (at a dose of 300 mg/kg body weight) was found to be most active among all. Therefore, it was subjected to the isolation of phytoconstituent responsible for the activity using column chromatography. The isolated compound was characterized by TLC, melting point, UV, IR, 1H-NMR and Mass spectroscopy and was identified as β-sitosterol. Antispermatogenic activity of the isolated compound was evaluated at a dose of 5 mg/kg body weight/day, for 45 days. The treatment caused significant decrease (P<0.01) in the weight of reproductive organs such as; testis, epididymis and seminal vesicle. Moreover, the sperm count, sperm viability and serum testosterone levels were significantly lowered when compared to that of the control group. - See more at: http://eurekaselect.com/128602#sthash.h2WkS8ek.dpuf

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February 2015
6 Reads

Natural male contraceptive: phytochemical investigation and anti-spermatogenic activity of Pistia stratiotes Linn.

Nat Prod Res 2014 25;28(16):1313-7. Epub 2014 Mar 25.

a Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology , Lucknow , 226028 UP , India.

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http://dx.doi.org/10.1080/14786419.2014.900772DOI Listing
November 2014
16 Reads
0.920 Impact Factor

Green Nanoparticle Strategies: Utilizing Excipients Sourced from Nature

Journal of Nanopharmaceutics and Drug Delivery

Green nanotechnology offers a wide range of applications in nanotechnology-enabled and ecofriendly manufacturing processes, which not only reduce the use of chemicals/organic solvents but also promote the use of natural exipients. This review presents a detailed insight in to the green nanotechnology based strategies for nanocarriers, with special reference to solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and polymeric nanoparticles (PNPs). The literature has been exhaustively studied with respect to the use of excipients which are of natural origin, or derived from natural origin. The techniques with minimum utilization of organic solvents during formulation of lipoidal and polymeric nanoparticles have been highlighted. The use of green excipients represents one of the strategies towards the development of environment friendly approaches for the development of nanocarriers. The basic properties and structures of excipients and their principal constituents have also been discussed. The major applications of SLNs, NLCs and PNPs have been discussed in detail with respect to different delivery routes like topical, oral, ocular, parenteral, pulmonary and also for specific diseases like cancer, malaria and gene delivery. Nanotechnology as such has tremendous benefits, which may be further supplemented by the green nanotechnology approach.

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September 2014
5 Reads

Syntheses, characterization and evaluation of novel 2,6-diarylpiperidin-4-ones as potential analgesic-antipyretic agents.

Eur J Med Chem 2014 Jul 2;82:439-48. Epub 2014 Jun 2.

Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Lucknow 226028, Uttar Pradesh, India. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S02235234140051
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http://dx.doi.org/10.1016/j.ejmech.2014.05.080DOI Listing
July 2014
14 Reads
3.450 Impact Factor

4-Thiazolidinones: the advances continue….

Eur J Med Chem 2014 Jan 27;72:52-77. Epub 2013 Nov 27.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, BBD City, Faizabad Road, Lucknow 226028, U.P., India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2013.11.017DOI Listing
January 2014
15 Reads
16 Citations
3.450 Impact Factor

Nitrogen containing privileged structures and their solid phase combinatorial synthesis.

Comb Chem High Throughput Screen 2013 Jun;16(5):345-93

Pharmacy Department, Faculty of Technology & Engineering, The M S University of Baroda, Kala Bhavan, Vadodara-390001, Gujarat, India.

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June 2013
12 Reads
1 Citation
1.222 Impact Factor

Piperidin-4-one: the potential pharmacophore.

Mini Rev Med Chem 2013 Apr;13(4):565-83

Babu Banarasi Das Northern India Institute of Technology, BBD City, Faizabad Road, Lucknow, U.P., India.

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April 2013
16 Reads
1 Citation
2.903 Impact Factor

SLN approach for nose-to-brain delivery of alprazolam.

Drug Deliv Transl Res 2012 Dec;2(6):498-507

Faculty of Pharmacy, Babu Banarasi Das National Institute of Technology & Management, Lucknow, Uttar Pradesh, India.

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http://dx.doi.org/10.1007/s13346-012-0110-2DOI Listing
December 2012
6 Reads
3 Citations

SLN Approach for nose to brain targeting of alprazolam

Drug Delivery and Translational Research

In the present study, alprazolam-loaded solid lipid nanoparticles were prepared and characterized. They were evaluated for their efficiency in nose-to-brain targeting and biodistribution in a suitable animal model after intranasal delivery. Solid lipid nanoparticles may offer an improvement to nose-to-brain drug delivery since they are able to protect the encapsulated drug from biological and/or chemical degradation. The distribution of the drug to different organs was recorded through biodistribution studies in male Wistar rats and gamma scintigraphy imaging in New Zealand rabbits by tagging the formulation with radioactive substance 99mTc. The radioactivity count of various organs was taken as a function of the drug concentration. The study reveals that alprazolam can be rapidly transferred to the brain via intranasal route, bypassing the blood–brain barrier and a direct nose-to-brain transfer. The enhanced rate and extent of transport may help in reducing the dose and dosing frequency, thereby providing ease for ambulatory patients.

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November 2012
12 Reads

Phytochemical investigation characterisation and anticonvulsant activity of Ricinus communis seeds in mice.

Nat Prod Res 2011 Nov 26;25(19):1881-4. Epub 2011 Aug 26.

Faculty of Pharmacy, Northern India Engineering College, Lucknow, UP, India.

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http://dx.doi.org/10.1080/14786419.2010.551753DOI Listing
November 2011
8 Reads
0.920 Impact Factor

Synthesis of Bezimidazoles as Antimicrobial Agents

Indian Journal of Heterocyclic Chemistry

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February 2011
8 Reads

Fullerenes-From Carbon To Nanomedicine

Mini Reviews In Medicinal Chemistry

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August 2010
6 Reads

Fullerenes: from carbon to nanomedicine.

Mini Rev Med Chem 2010 Jul;10(8):662-77

Faculty of Pharmacy, Babu Banarasi Das National Institute of Technology and Management, Lucknow-227105, India.

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July 2010
38 Reads
6 Citations
2.903 Impact Factor

4-thiazolidinone--a biologically active scaffold.

Eur J Med Chem 2008 May 6;43(5):897-905. Epub 2007 Aug 6.

Faculty of Pharmacy, Northern India Engineering College, Dr. Akhilesh Das Nagar, Sector-2, Faizabad Road, Lucknow 227105, Uttar Pradesh, India.

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http://dx.doi.org/10.1016/j.ejmech.2007.07.017DOI Listing
May 2008
12 Reads
21 Citations
3.450 Impact Factor

Iontophoretic drug delivery system: a review.

Technol Health Care 2007 ;15(4):237-45

Department of Pharmaceutical Sciences, H.N.B.G. University, Srinagar (UA), India.

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April 2008
9 Reads
2 Citations
0.640 Impact Factor

Properties and formulation of oral drug delivery systems of proteins and peptides

Indian Journal of Pharmaceutical Sciences

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June 2007
7 Reads

Top co-authors

Avinash C Tripathi
Avinash C Tripathi

Babu Banarasi Das Northern India Institute of Technology

10
Pankaj K Sonar
Pankaj K Sonar

Babu Banarasi Das Northern India Institute of Technology

4
Amit Verma
Amit Verma

Albert Einstein College of Medicine

3
Ranjit Singh
Ranjit Singh

Patient Safety Research Center

3
Mahendra Singh
Mahendra Singh

Indira Gandhi Institute of Medical Sciences

2
Viney Chawla
Viney Chawla

Babu Banarasi Das Northern India Institute of Technology

2
Malti Arya
Malti Arya

School of Biosciences & Biotechnology

2
Gul Naz Fatima
Gul Naz Fatima

Babu Banarasi Das Northern India Institute of Technology

1