Publications by authors named "Saikrishna Balabadra"

5 Publications

  • Page 1 of 1

Synthesis, anti-microbial activity, cytotoxicity of some novel substituted (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs.

Chem Cent J 2018 Jan 9;12(1). Epub 2018 Jan 9.

Molecular Modelling and Medicinal Chemistry Group, Department of Chemistry, Osmania University, Hyderabad, Telangana, India.

Background: There is a dire need for the discovery and development of new antimicrobial agents after several experiments for a better resistance of microorganisms towards antimicrobial agents become a serious health problem for a few years in the past. As benzimidazole possess various types of biological activities, it has been synthesized, in the present study, a new series of (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs by using the condensation and screened for its in vitro antimicrobial activity and cytotoxicity.

Results: The synthesized (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl) benzofuran-2-yl)(phenyl)methanone analogs were confirmed by IR, H and C-NMR, MS spectra and HRMS spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial potential against Gram-positive (Bacillus subtilis, Bacillus megaterium, Staph aureus and Streptococcus pyogenes), Gram-negative (Escherichia coli, Proteus vulgaris, Proteus mirabilis and Enterobacter aerogenes) bacterial and fungal (Aspergillus niger, Candida albicans, Fusarium oxysporum, Fusarium solani) strains by disc diffusion method and the minimum inhibitory concentration (MIC) in which it has been recorded in microgram per milliliter in comparison to the reference drugs, ciprofloxacin (antibacterial) and nystatin (antifungal). Further, the cytotoxicity (IC value) has also been assessed on human cervical (HeLa), Supt1 cancer cell lines by using MTT assay.

Conclusions: The following screened compounds (4d), (4f), (4g), (4k), (4l), (4o) and (4u) were found to be the best active against all the tested bacterial and fungal strains among all the demonstrated compounds of biological study. The MIC determination was also carried out against bacteria and fungi, the compounds (4f) and (4u) are found to be exhibited excellent potent against bacteria and fungi respectively. The compounds (4f) and (4u) were shown non-toxic in nature after screened for cytotoxicity against the cancer cell lines of human cervical (HeLa) and Supt1. Additionally, structure and antibacterial activity relationship were also further supported by in silico molecular docking studies of the active compounds against DNA topoisomerase.
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http://dx.doi.org/10.1186/s13065-017-0364-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5760494PMC
January 2018

Bis-spirochromanones as potent inhibitors of Mycobacterium tuberculosis: synthesis and biological evaluation.

Mol Divers 2017 Nov 24;21(4):999-1010. Epub 2017 Aug 24.

X-ray Crystallography Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana State, 500 007, India.

On the basis of reported antimycobacterial property of chroman-4-one pharmacophore, a series of chemically modified bis-spirochromanones were synthesized starting from 2-hydroxyacetophenone and 1,4-dioxaspiro[4.5] decan-8-one using a Kabbe condensation approach. The synthesized bis-spirochromanones were established based on their spectral data and X-ray crystal structure of 6e. All synthesized compounds were evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain, finding that some products exhibited good antimycobacterial activity with minimum inhibitory concentration as low as [Formula: see text]. Docking studies were carried out to identify the binding interactions of compounds II, 6a and 6n with FtsZ. Compounds exhibiting good in vitro potency in the MTB MIC assay were further evaluated for toxicity using the HEK cell line.
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http://dx.doi.org/10.1007/s11030-017-9779-yDOI Listing
November 2017

Synthesis of -butyl (substituted benzamido)phenylcarbamate derivatives: anti-inflammatory activity and docking studies.

J Chem Biol 2017 Jul 5;10(3):105-115. Epub 2017 Apr 5.

Department of Biochemistry, University College of Science, Osmania University, Hyderabad, Telangana 500007 India.

A series of new -butyl 2-(substituted benzamido) phenylcarbamate - were synthesized by the condensation of -butyl 2-amino phenylcarbamate () with various substituted carboxylic acid in the presence of EDCI and HOBt as coupling reagent, obtain in excellent yields. The structures of all newly synthesized compounds were characterized spectroscopically and evaluated for in vivo anti-inflammatory activity compared to the standard drug, indomethacin, by using the carrageenan-induced rat paw edema protocol. Most of the compounds exhibited a promising anti-inflammatory activity within 9 to 12 h, the percentage of inhibition values ranging from 54.239 to 39.021%. The results revealed that the compounds and exhibited better or equivalent anti-inflammatory activity with the percentage of inhibition of 54.239 and 54.130%, respectively, which was comparable to standard drug. In addition to experimental results, in silico docking studies was used as a tool to verify and expand the experimental outcomes.
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http://dx.doi.org/10.1007/s12154-017-0168-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5480262PMC
July 2017

Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones.

Medchemcomm 2017 Mar 3;8(3):559-570. Epub 2017 Jan 3.

Molecular Modeling and Medicinal Chemistry Group , Department of Chemistry , Osmania University , Hyderabad , Telangana-500 007 , India.

As part of an ongoing effort to develop new antitubercular and antimicrobial agents, a series of substituted xanthenone derivatives () were synthesized. Xanthenone derivatives () were prepared a one-pot three-component thermal cyclization reaction of β-naphthol (), substituted 1-aryl-1-[1,2,3]triazole-4-carbaldehydes (), and cyclic-1,3-diones (, ) in the presence of a catalytic amount of iodine. The newly synthesized compounds were characterized by IR, NMR, mass spectral data, and elemental analysis. These compounds ( and ) were screened for antitubercular activity against the HRv (ATCC 27294) strain, for antibacterial activity against Gram-positive and Gram-negative strains, and for antifungal activity against a pathogenic strain of fungi. Among the compounds tested, most of them showed good to excellent antimicrobial and antitubercular activity. The active compounds displaying good potency in the MTB were further examined for toxicity in a HEK cell line. In addition, the structure and antitubercular activity relationship were further supported by molecular-docking studies of the active compounds against the pantothenate synthetase (PS) enzyme of .
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http://dx.doi.org/10.1039/c6md00593dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6072411PMC
March 2017

Synthesis and evaluation of naphthyl bearing 1,2,3-triazole analogs as antiplasmodial agents, cytotoxicity and docking studies.

Bioorg Med Chem 2017 01 25;25(1):221-232. Epub 2016 Oct 25.

Centre for Cellular and Molecular Biology, Habsiguda, Uppal Road, Hyderabad 500007, Telangana, India.

Novel series of naphthyl bearing 1,2,3-triazoles (4a-t) were synthesized and evaluated for their in vitro antiplasmodial activity against pyrimethamine (Pyr)-sensitive and resistant strains of Plasmodium falciparum. The synthesized compounds were assessed for their cytotoxicity employing human embryonic kidney cell line (HEK-293), and none of them was found to be toxic. Among them 4j, 4k, 4l, 4m, 4n, 4t exhibited significant antiplasmodial activity in both strains, of which compounds 4m, 4n and 4t (∼3.0-fold) displayed superior activity to Pyr against resistant strain. Pyr and selected compounds (4n, 4p and 4t) that repressed parasite development also inhibited PfDHFR activity of the soluble parasite extract, suggesting that anti-parasitic activity of these compounds is a result of inhibition of the parasite DHFR. In silico studies suggest that activity of these compounds might be enhanced due to π-π stacking.
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http://dx.doi.org/10.1016/j.bmc.2016.10.029DOI Listing
January 2017
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