3,180 results match your criteria Current Topics in Medicinal Chemistry [Journal]


Trends in Enzyme Inhibition and Activation in Drug Design - Part-I.

Curr Top Med Chem 2019 ;19(4):244-245

School of Health, Faculty of Pharmacy Aristotle University of Thessaloniki Thessaloniki 54124, Greece.

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http://dx.doi.org/10.2174/156802661904190411090238DOI Listing
January 2019
1 Read

Advanced Theranostic Application of Bio-Nanoparticle Systems.

Curr Top Med Chem 2019 ;19(4):243

Division of Engineering in Medicine Brigham and Women's Hospital Harvard Medical School, Boston, MA 02139, United States.

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http://dx.doi.org/10.2174/156802661904190411090002DOI Listing
January 2019
1 Read

Role of natural product in modulation of drug transporters and New Delhi Metallo- β lactamases.

Curr Top Med Chem 2019 Apr 15. Epub 2019 Apr 15.

ICMR-Regional Medical Research Centre (Dept. of Health Research, Govt. of India), Chandrasekharpur, Bhubaneswar. India.

The rapid growth in the drug resistance has bought the treatment options to treat antimicrobial resistance to halt. Bacteria evolve to accumulate many genes that code resistance for a single drug within a single cell. Drug transporters are the major factors for the pharmacokinetics of drugs and alternations of drug transport is one of the causes for interactions. Read More

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http://dx.doi.org/10.2174/1871529X19666190415110724DOI Listing

Therapeutic Potential of Endophytic Compounds: A Special Reference to Drug Transporter Inhibitors.

Curr Top Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Microbiology Department, ICMR-Regional Medical Research Centre, Bhubaneswar. India.

From the discovery to the golden age of antibiotics (miracle), millions of lives have been saved. Era of negligence towards chemotherapeutic agents gave birth to drug resistance. Among all the regulators of drug resistance the drug transporters are considered to be the key regulator for multidrug resistance. Read More

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http://dx.doi.org/10.2174/1568026619666190412095105DOI Listing
April 2019
1 Read

Recent Status and Advancements in the development of Antifungal Agents: Highlights on Plant and Marine Based Antifungals.

Curr Top Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Unit of Microbiology and Molecular Biology, ICMR-Vector Control Research Center, Puducherry. India.

The developing resistant in fungai has become the key challenge, which is being faced nowadays towards the available antifungal agents in the market. Further search for novel compounds from different sources have been explored to meet this problem. The current review describes and highlights recent advancement in the drug production from from plant and marine based sources. Read More

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http://dx.doi.org/10.2174/1568026619666190412102037DOI Listing
April 2019
1 Read

Recent Developments in Natural Product Inspired Synthetic 1,2,4-Trioxolanes (Ozonides): An Unusual Entry into Antimalarial Chemotherapy.

Curr Top Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Laboratory of Organic and Medicinal Chemistry, Department of Chemistry, Malaviya National Institute of Technology Jaipur, Jawaharlal Nehru Marg, Jaipur-302017. India.

According to WHO "World health statistics 2018", malaria, alongside acute respiratory infections and diarrhoea, is one of the major infectious disease causing children's death in between the age of 1-5 years. Similarly, according to another report (2016), malaria accounts for approximately 3.14% of the total disease burden by cause of the world. Read More

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http://dx.doi.org/10.2174/1568026619666190412104042DOI Listing
April 2019
1 Read

Medicinal chemistry of Alternative therapeutics: Novelty and hopes with genus Ammannia.

Curr Top Med Chem 2019 Apr 11. Epub 2019 Apr 11.

Laboratory of Chemistry, Department of Applied Sciences, Rajkiya Engineering College (An associate college of Dr. A.P.J. Abdul Kalam Technical University, Lucknow), Churk, Sonbhadra-231206. India.

The plants have formed the basis of folklore remedy since beginning of human civilization. The cumulative human endeavor and experience over a period of thousands of years developed into well to organize traditional medicine systems viz. Ayurvedic, Unani, Chinese amongst others. Read More

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http://dx.doi.org/10.2174/1568026619666190412101047DOI Listing

Comparative drug resistance reversal potential of natural glycosides Synergy potential of niaziridin&niazirin.

Curr Top Med Chem 2019 Apr 12. Epub 2019 Apr 12.

Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow-226015. India.

Due to limited availability of antibiotics, Gram negative bacteria (GNB) acquire different levels of drug resistance. It raised an urgent need to identify such agents, which can reverse the phenomenon of drug resistance. The present study was intended to understand the mechanism of drug resistance reversal of glycosides namely niaziridin, niazirinisolated from Moringaoleiferaand ouabain (control)against clinical isolates of multidrug resistant Escherichia coli (MDREC). Read More

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http://dx.doi.org/10.2174/1568026619666190412120008DOI Listing
April 2019
1 Read

ABC transporters in neurological disorders: an important gateway for botanical compounds mediated neuro-therapeutics.

Curr Top Med Chem 2019 Apr 12. Epub 2019 Apr 12.

Unit of Microbiology and Molecular Biology, ICMR-Vector Control Research Center, Puducherry-605006. India.

Neurodegeneration is a distinguishing feature of many age related disorders. There are a number of factors that can modulate the pathology of these disorders. ATP-binding cassette (ABC) transporters are primarily involved in the maintenance of normal brain homeostasis by eliminating toxic peptides and compounds from the brain. Read More

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http://dx.doi.org/10.2174/1568026619666190412121811DOI Listing
April 2019
6 Reads

Functional Peptides and Small Molecules in Medicinal Chemistry-Part II.

Curr Top Med Chem 2019 ;19(3):186

Huaxi MR Research Center, Department of Radiology, West China Hospital and West China School of Medicine, Sichuan University, Chengdu (610041), China.

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http://dx.doi.org/10.2174/156802661903190328160356DOI Listing
January 2019

Functional Inhibition of VEGF and EGFR Suppressors in Cancer Treatment.

Curr Top Med Chem 2019 ;19(3):178-179

Principal Scientist In silico Research Laboratory Eminent Biosciences 91, Sector-A, Mahalakshmi Nagar Indore - 452010, Madhya Pradesh, India.

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http://dx.doi.org/10.2174/156802661903190328155731DOI Listing
January 2019
1 Read

Leishmaniasis and Chagas Disease - Neglected Tropical Diseases: Treatment Updates.

Curr Top Med Chem 2019 ;19(3):174-177

Laboratorio de Estudos Avancados de Microrganismos Emergentes e Resistentes, Departamento de Microbiologia Geral, Instituto de Microbiologia Paulo de Goes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.

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http://dx.doi.org/10.2174/156802661903190328155136DOI Listing
January 2019

Recent In Silico Research in High-Throughput Drug Discovery and Molecular Biochemistry.

Curr Top Med Chem 2019 ;19(2):103-104

College of Medical, Veterinary and Life Sciences University of Glasgow, United Kingdom.

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http://dx.doi.org/10.2174/156802661902190328150226DOI Listing
January 2019
1 Read
3.402 Impact Factor

Dereplication in Natural Product Discovery.

Curr Top Med Chem 2019 ;19(2):101-102

Biology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, Telangana, India.

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http://dx.doi.org/10.2174/156802661902190328145951DOI Listing
January 2019
3.402 Impact Factor

Functional Peptides and Small Molecules in Medicinal Chemistry-Part I.

Curr Top Med Chem 2019 ;19(1):2-3

Huaxi MR Research Center, Department of Radiology, West China Hospital and West China School of Medicine, Sichuan University, Chengdu (610041), China.

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http://dx.doi.org/10.2174/156802661901190326145944DOI Listing

Preface.

Authors:
Allen B Reitz

Curr Top Med Chem 2019 ;19(1)

Fox Chase Chemical Diversity Center, Inc Doylestown, PA 18902, United States.

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http://dx.doi.org/10.2174/156802661901190326145545DOI Listing
April 2019
1 Read

Protein-Protein Interactions of Phosphodiesterases.

Curr Top Med Chem 2019 Mar 31. Epub 2019 Mar 31.

Faculty of Pharmaceutical Sciences, UCSI University, Kuala Lumpur. Malaysia.

Phosphodiesterases (PDEs) are enzymes that play a key role in terminating cyclic nucleotides signalling by catalysing the hydrolysis of 3', 5' cyclic adenosine monophosphate (cAMP) and/or 3', 5' cyclic guanosine monophosphate (cGMP), the second messengers within the cell that transport the signals produced by extracellular signalling molecules which are unable to get into the cells. PDEs are critical determinants in controlling the intracellular concentrations and, subsequently, the biological actions of the second messengers. PDE superfamily contains 11 highly regulated and structurally-related gene families (PDEs 1-11). Read More

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http://dx.doi.org/10.2174/1568026619666190401113803DOI Listing
March 2019
2 Reads

Recent Advances in Use of Topoisomerase Inhibitors in Combination Cancer Therapy.

Curr Top Med Chem 2019 Mar 31. Epub 2019 Mar 31.

Department of Chemistry and Biochemistry, Florida International University, Miami, Florida. United States.

Inhibitors targeting human topoisomerase I and topoisomerase II alpha have provided a useful chemotherapy option for treatment of many patients suffering from a variety of cancers. While the treatment can be effective in many patient cases, use of these human topoisomerase inhibitors is limited by side-effects that can be severe. A strategy of employing the topoisomerase inhibitors in combination with other treatments can potentially sensitize the cancer to increase the therapeutic efficacy and reduce resistance or adverse side effects. Read More

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http://dx.doi.org/10.2174/1568026619666190401113350DOI Listing

Topoisomerase Inhibitors and Targeted Delivery in Cancer Therapy.

Curr Top Med Chem 2019 Mar 31. Epub 2019 Mar 31.

Antibody Discovery and Protein Engineering, MedImmune, One MedImmune Way, Gaithersburg, MD 20878. United States.

DNA topoisomerases are enzymes that catalyze the alteration of DNA topology with transiently induced DNA strand breakage, essential for DNA replication. Topoisomerases are validated cancer chemotherapy targets. Anticancer agents targeting Topoisomerase I and II have been in clinical use and proved to be highly effective, though with significant side effects. Read More

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http://dx.doi.org/10.2174/1568026619666190401112948DOI Listing

Potentiation of PBD dimers by lipophilicity manipulation.

Curr Top Med Chem 2019 Mar 31. Epub 2019 Mar 31.

Spirogen-Medimmune, Queen Mary BioEnterprises Innovation Centre, 42 New road, Whitechapel, London E1 2AX. United Kingdom.

Pyrrolobenzodiazepine (PBD) dimers are highly potent DNA cross linking agents used as warheads in Antibody Drug Conjugates (ADCs) for cancer therapy. We propose to investigate the correlation existing between the lipophilicity of those molecules and their activity (both in vitro and in vivo) as well as any effect observed during conjugation. Read More

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http://dx.doi.org/10.2174/1568026619666190401112517DOI Listing

Nitrogen Mustards As Anticancer Chemotherapies: Historic Perspective, Current Developments, And Future Trends.

Curr Top Med Chem 2019 Mar 31. Epub 2019 Mar 31.

Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201. United States.

Nitrogen mustards, a family of DNA alkylating agents, marked the start of cancer pharmacotherapy. While traditionally characterized by their dose-limiting toxic effects, nitrogen mustards have been the subject of intense research efforts, which have led to safer and more effective agents. Even though the alkylating prodrug mustards were first developed decades ago, active research on ways to improve their selectivity and cytotoxic efficacy are a currently active topic of research. Read More

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http://dx.doi.org/10.2174/1568026619666190401100519DOI Listing

Pharmaceutical Interfering of Neddylation as Promising Treatments for Various Cancers.

Curr Top Med Chem 2019 Mar 10. Epub 2019 Mar 10.

School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou. China.

Background: Neddylation is an important post-translational modification of proteins, in which a NEDD8 (neural-precursor-cell-expressed developmentally down-regulated 8, ) is covalently introduced onto the substrate proteins to regulate their functions and homeostasis. As neddylation is frequently up-regulated in various cancers, its interference was proposed as a promising therapy of related diseases.

Objective: The recent advances in developing neddylation interfering agents were summarized to provide an overview of current achievements and perspectives for future development. Read More

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http://dx.doi.org/10.2174/1568026619666190311110646DOI Listing
March 2019
3 Reads

Small-Molecule Immuno-Oncology Therapy: Advances, Challenges and New Directions.

Curr Top Med Chem 2019 ;19(3):180-185

CAS Key Laboratory of Receptor Research and the State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.

Oncology immunotherapy has gained significant advances in recent years and benefits cancer patients with superior efficacy and superior clinical responses. Currently over ten immune checkpoint antibodies targeting CTLA-4 and PD-1/PD-L1 have received regulatory approval worldwide and over thousands are under active clinical trials. However, compared to the rapid advance of Monoclonal Antibody (mAb), studies on immunotherapeutic small molecules have far lagged behind. Read More

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http://dx.doi.org/10.2174/1568026619666190308131805DOI Listing
April 2019
2 Reads

Algorithmic and Stochastic Representations of Gene Regulatory Networks and Protein-Protein Interactions.

Curr Top Med Chem 2019 Mar 11. Epub 2019 Mar 11.

King Fahd Medical Research Center, King Abdulaziz University, Jeddah. Saudi Arabia.

The impact of Protein-Protein Interactions on physiologic functions and biological structures is a challenging task and a research field of great interest. For years researchers aim to identify their importance and effects, resulting in remarkable discoveries. Those findings are limited though by restrictions in technology, lack of necessary scientific knowledge and the complex nature of the biological systems. Read More

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http://dx.doi.org/10.2174/1568026619666190311125256DOI Listing

Protein-Protein Interaction and Aggregation Inhibitors in Alzheimer's Disease.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005. India.

Proteins, involved in a variety of structural and physiological functions, are an integral component of cells. The diverse cellular signaling processes and cross-talks involve protein-protein interactions. Disruption of protein-protein interaction interface remains an unexplored subject, although a massive increase in the number of peptides, peptidomimetics and small molecule inhibitors targeting such interactions is seen. Read More

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http://dx.doi.org/10.2174/1568026619666190304153353DOI Listing
March 2019
2 Reads
3.402 Impact Factor

Applications of in silico Methods for Design and Development of Drugs Targeting Protein-Protein Interactions.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Department of Biotechnology, Chemistry and Pharmacy (Dept. of Excellence 2018-2022), University of Siena, via A. Moro 2, 53100 Siena. Italy.

Identification of protein-protein interactions (PPIs) is a major challenge in modern molecular biology and biochemistry research, due to the unquestionable role of proteins in cells, biological process and pathological states. Over the past decade, the PPIs have evolved from being considered a highly challenging field of research to being investigated and examined as targets for pharmacological intervention. Comprehension of protein interactions is crucial to known how proteins come together to build signalling pathways, to carry out their functions, or to cause diseases, when deregulated. Read More

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http://dx.doi.org/10.2174/1568026619666190304153901DOI Listing

Quantum Molecular Dynamics, Topological, Group Theoretical and Graph Theoretical Studies of Protein-Protein Interactions.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Department of Pharmaceutical Technology, Meerut Institute of Engineering Technology, Meerut-250002. India.

When two or more protein molecules come into physical contacts of high specificity involving electrostatic forces or hydrogen bondings or hydrophobic effect, it is called protein-protein interactions (PPIs).These PPIs form the basis of multiple aggregation-related diseases such as cancer, Creutzfeldt-Jakob, and Alzheimer's diseases. Therefore, PPIs have been the subject of not only biochemistry but also of medicinal chemistry that involve both experimental and theoretical aspects. Read More

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http://dx.doi.org/10.2174/1568026619666190304152704DOI Listing
March 2019
1 Read

Protein/ Hormone Based Nanoparticles as Carriers for Drugs Targeting Protein-Protein Interactions.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Univ Lyon, University Claude Bernard Lyon-1, CNRS, LAGEP-UMR 5007, F-69622 Lyon. France.

The use of protein-based nanoparticles as carriers for drugs targeting protein-protein interactions (PPIs) is an interesting, relatively recent drug delivery strategy. . This review explains protein and protein interactions roles in normal and diseased conditions at nuclear, molecular and cellular levels. Read More

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http://dx.doi.org/10.2174/1568026619666190304152320DOI Listing
March 2019
2 Reads

Influence of Amino Acid Mutations and Small Molecules for Targeted Inhibition of Proteins Involved in Cancer.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Protein Bioinformatics Lab, Department of Biotechnology, Bhupat and Jyoti Mehta School of Biosciences, Indian Institute of Technology Madras, Chennai. India.

Protein-protein interactions (PPIs) are of crucial importance in regulating the biological processes of cells both in normal and diseased conditions. Recently, significant progress has been made in targeting PPIs using small molecules and achieved promising results. In this review, we focus on the advancements in computational research for targeted inhibition of proteins involved in cancer on two aspects: (i) understand the key roles of amino acid mutations in epidermal growth factor receptor (EGFR) as well as mutation-specific inhibitors and (ii) design of small molecule inhibitors for Bcl-2 to disrupt PPIs. Read More

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http://dx.doi.org/10.2174/1568026619666190304143354DOI Listing
March 2019
7 Reads

Dihydroartemisinin and its analogs: A new class of antitubercular agents.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow. India.

Tuberculosis (TB) is one of the leading causes of mortality worldwide. Resistance against the frontline anti-tubercular drugs has worsened the already alarming situation, which requires intensive drug discovery to develop new, more effective, affordable and accessible anti-tubercular agents possessing novel modes of action. Dihydroartemisinin, a metabolite of artemisinin was semi-synthesized into 8 acyl (DHA-2 - DHA-9) derivatives and were evaluated for anti-tubercular potential against H37Rv virulent strain of Mycobacterium tuberculosis by agar-based proportion assay. Read More

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http://dx.doi.org/10.2174/1568026619666190304142802DOI Listing

Screening of anti-mycobacterial phytochemical compounds for potential inhibitorsagainst Mycobacterium tuberculosis isocitrate lyase.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Biotechnology division,CSIR-Central Institute of Medicinal and Aromatic Plant (CIMAP), Lucknow-226015,Uttar Pradesh. India.

Tuberculosis (TB) is a leading infectious disease caused by Mycobacterium tuberculosiswith high morbidity and mortality. Isocitrate lyase (MtbICL), a key enzyme of glyoxylate pathway has been shown to be involved in the persistence, is attractive drug target against persistent mycobacteria. Virtual screening, molecular docking and MD simulation study has been integrated for screening of phytochemical based anti-mycobacterial compounds. Read More

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http://dx.doi.org/10.2174/1568026619666190304125603DOI Listing
March 2019
3 Reads
3.402 Impact Factor

Synthesis and antibacterial activity of Mefloquine-based analogs against sensitive and resistant Mycobacterium tuberculosis strains.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Fiocruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Farmanguinhos, Rua Sizenando Nabuco, 100, Manguinhos, 21041-250, Rio de Janeiro, RJ. Brazil.

A series of new 2,8-bis(trifluoromethyl)quinoline derivatives 2 - 9 were synthesized and evaluated for their in vitro antibacterial activity against sensitive Mycobacterium tuberculosis ATCC 27294, using the microplate Alamar Blue assay (MABA). The compounds 3c (37.2 µM), 7 (68. Read More

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http://dx.doi.org/10.2174/1568026619666190304124952DOI Listing

How cancer cells resist chemotherapy: Design and Development of Drugs Targeting.

Curr Top Med Chem 2019 03 5. Epub 2019 Mar 5.

Sechenov First Moscow State Medical University (Sechenov University), 8-2 Trubetskaya St., Moscow 119991. Russia.

Nowadays, it is well known that tumor is not a simple set of cells, but a highly organized structure, which can adapt to the changing conditions of adverse microenvironment, including exposure to chemotherapy. In this review, we have discussed the feasibility of prediction of development general and specific resistance mechanisms to chemotherapy. It is shown that not all theoretical knowledge about factors of drug resistance, including alteration in DNA-repair machinery, drug reflux, autophagy, apoptosis evasion, immune system evasion, the influence of tumor microenvironment etc. Read More

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http://dx.doi.org/10.2174/1568026619666190305130141DOI Listing
March 2019
2 Reads

Tryptanthrin analogues as inhibitors of enoyl-acyl carrier protein reductase: activity against Mycobacterium tuberculosis, toxicity, modeling of enzyme binding.

Curr Top Med Chem 2019 03 4. Epub 2019 Mar 4.

Laboratory of Organic Synthesis and Biopharmaceuticals, Institute of Chemistry, Chisinau. Moldova.

A new group of tryptanthrin analogues were obtained and evaluated for their activity against Mycobacterium tuberculosis H37Rv. Tryptanthrin is a known inhibitor of Mtb enoyl-acyl carrier protein reductase (InhA) and modifications in its structure gave a group of 5H-[1,3,4]thiadiazolo[2,3-b]quinazolin-5-one analogues with antimycobacterial various potency. The most active compound in the series, 2-(propylthio)-5H-[1,3,4]thiadiazolo[2,3-b]quinazolin-5-one, exhibited the superior inhibition activity (up to 100%) against mycobacterial growth at MIC 6. Read More

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http://dx.doi.org/10.2174/1568026619666190304125740DOI Listing
March 2019
1 Read

Targeting DNA gyrase to combat Mycobacterium tuberculosis: An update.

Curr Top Med Chem 2019 Mar 4. Epub 2019 Mar 4.

Division of Microbiology, CSIR-Central Drug Research Institute, Lucknow-226031, Uttar Pradesh. India.

DNA gyrase is a clinically validated drug target, currently targeted only by fluoroquinolone class of antibacterials. However, owing to increasing drug resistance as well as concomitant reduction in availability of newer classes of antibiotics, fluoroquinolones are increasingly being over-utilized in order to treat serious infections, including multi-drug resistant tuberculosis. This in turn, increases the probability of resistance to fluoroquinolones, which is mediated by a single amino acid change in gyrA, leading to class wide resistance. Read More

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http://dx.doi.org/10.2174/1568026619666190304130218DOI Listing
March 2019
2 Reads

Synthesis, Screening and Docking Analysis of Hispolon Pyrazoles and Isoxazoles as Potential Antitubercular Agents.

Curr Top Med Chem 2019 Mar 5. Epub 2019 Mar 5.

Medicinal Chemistry Research Labs, College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, AP. India.

Back ground: Hispolons are natural products known to possess cytoprotective, antioxidant and anti-cancer activities. We have found recently anti TB activity in these compounds. Efforts were made to optimize the structure with bioisosteric replacement of 1,3-diketo functional group with the corresponding pyrazole and isoxazole moieties. Read More

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http://dx.doi.org/10.2174/1568026619666190305124954DOI Listing
March 2019
2 Reads

4H-1,3-Benzothiazin-4-one a promising class against MDR/XDR-TB.

Curr Top Med Chem 2019 Mar 5. Epub 2019 Mar 5.

FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos. Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro. Brazil.

Nowadays, tuberculosis (TB) is an important global public health problem, being responsible for millions of TB-related deaths worldwide. Due to the increased number of cases and resistance of Mycobacterium tuberculosis to all drugs used to the treatment of this disease, we desperately need new drugs and strategies that could reduce treatment time with fewer side effects, reduced cost and highly active drugs against resistance strains and latent disease. Considering that, 4H-1,3-benzothiazin-4-one is a promising class of antimycobacterial agents in special against TB-resistance strains being the aim of this review¬ the discussion of different aspects of this chemical class such as synthesis, mechanism of action, medicinal chemistry and combination with other drugs. Read More

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http://dx.doi.org/10.2174/1568026619666190305130809DOI Listing

In Vitro, In Silico and Ex Vivo Studies of Dihydroartemisinin derivatives as antitubercular agents.

Curr Top Med Chem 2019 Mar 5. Epub 2019 Mar 5.

Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow. India.

As a part of our drug discovery program for anti-tubercular agents, dihydroartemisinin (DHA-1) was screened against Mtb H37Rv, which showed moderate anti-tubercular activity (>25 .0 μg/mL). These results prompted us to carry out chemical transformation of DHA-1 into various derivatives and study their antitubercular potential. Read More

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http://dx.doi.org/10.2174/1568026619666190305131425DOI Listing
March 2019
2 Reads

Resveratrol in Various Pockets: A Review.

Curr Top Med Chem 2019 ;19(2):116-122

Laboratory of Preservation Technology and Enzyme Inhibition Studies, Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, India.

Several phenolic compounds bind to proteins (such as enzymes) and interfere in their catalytic mechanism. Interaction studies of natural polyphenol; Resveratrol with various targets like with tubulin, protein kinase C alpha (PKCα), phosphodiesterase-4D, human oral cancer cell line proteins, DNA sequences having AATT/TTAA segments, protein kinase C alpha, lysine-specific demethylase 1 have been reviewed in this article. Simulation studies indicate that resveratrol and its analogs/ derivatives show good interaction with the target receptor through its hydroxyl groups by forming hydrogen bonds and hydrophobic interactions with amino acid residues at the binding site. Read More

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http://dx.doi.org/10.2174/1568026619666190301173958DOI Listing
January 2019
1 Read
3.402 Impact Factor

Synthesis and in vitro Enzymatic Studies of new 3-Aryldiazenyl Indoles as Promising Helicobacter Pylori IMPDH Inhibitors.

Curr Top Med Chem 2019 02 27. Epub 2019 Feb 27.

Biological Engineering & Physics, Indian Institute of Technology Gandhinagar, Gujarat, India.

Background & Objective: Helicobacter pylori infection is one of the primary causes of peptic ulcer followed by gastric cancer in the world population. Due to increased occurrences of multi-drug resistance to the currently available antibiotics, there is an urgent need for a new class of drugs against H. pylori. Read More

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http://dx.doi.org/10.2174/1568026619666190227212334DOI Listing
February 2019
6 Reads

Imidazole and 1,2,4-Triazole-based Derivatives Gifted with Antitubercular Activity: Cytotoxicity and Computational Assessment.

Curr Top Med Chem 2019 02 27. Epub 2019 Feb 27.

Department of Chemistry and Pharmaceutical Sciences, P.le Europa 1, University of Trieste, 34127 Trieste,. Italy.

Background: Mycobacterium Tuberculosis (Mtb) is the causative pathogen of tuberculosis (TB) and outbreaks are more common among immunosuppressed persons infected with HIV. The current treatment regimens are lengthy and toxic, yet the therapy has remained unchanged for many decades, so there is a need to find new structures with selective mechanism of action. Moreover, the increased incidence of severe disseminated infections produced by undiagnosed multidrug-resistant (MDR), worsen clinical treatment and contribute the spread of the disease. Read More

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http://dx.doi.org/10.2174/1568026619666190227183826DOI Listing
February 2019
3 Reads

An Overview on the Potential Antimycobacterial Agents Targeting Serine/Threonine Protein Kinases from Mycobacterium tuberculosis.

Curr Top Med Chem 2019 02 27. Epub 2019 Feb 27.

Dipartimento di Biologia e Biotecnologie "Lazzaro Spallanzani", Università degli Studi di Pavia, via Ferrata 9, 27100 Pavia,. Italy.

Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), still remains an urgent global health issue, mainly due to the emergence of multi-drug resistant strains. Therefore, there is a pressing need to develop novel and more efficient drugs to control the disease. In this context, targeting the pathogen virulence factors, and particularly signal mechanisms, seems to be a promising approach. Read More

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http://dx.doi.org/10.2174/1568026619666190227182701DOI Listing
February 2019

An Overview of HDAC Inhibitors and their Synthetic Routes.

Curr Top Med Chem 2019 Feb 27. Epub 2019 Feb 27.

School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, Guangzhou 510515, . China.

Epigenetics play a key role in the origin, development and metastasis of cancer. Epigenetic processes include DNA methylation, histone acetylation, histone methylation, and histone phosphorylation, among which, histone acetylation is the most common one that plays important roles in the regulation of normal cellular processes, and is controlled by histone deacetylases (HDACs) and histone acetyltransferases (HATs). HDACs are involved in the regulation many key cellular processes, such as DNA damage repair, cell cycle control, autophagy, metabolism, senescence and chaperone function, and can lead to oncogene activation. Read More

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http://dx.doi.org/10.2174/1568026619666190227221507DOI Listing
February 2019
1 Read

Acid Ceramidase; A Novel Therapeutic Target in Cancer.

Curr Top Med Chem 2019 Feb 27. Epub 2019 Feb 27.

Cancer Research Program, Rajiv Gandhi Centre for Biotechnology (RGCB), Thiruvananthapuram, Kerala State, . India.

Sphingolipids are important constituents of eukaryotic cell membrane which govern various signaling pathways related to different aspects of cell survival. Ceramide and Sphingosine are inter convertible sphingolipid metabolites, out of which Ceramide is pro-apoptotic and sphingosine is anti-apoptotic in nature. The conversion of ceramide to sphingosine is mediated by Acid Ceramidase (ASAH1) thus maintaining a rheostat between a tumor suppressor and a tumor promoter. Read More

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http://dx.doi.org/10.2174/1568026619666190227222930DOI Listing
February 2019

Mycobacterial enzyme targets and their inhibitors.

Curr Top Med Chem 2019 Feb 18. Epub 2019 Feb 18.

Division of Medicinal and Process Chemistry, CSIR Central Drug Research Institute, Lucknow 226 001. India.

Background: Tuberculosis (TB) is a major health problem worldwide. Mycobacterium tuberculosis has a unique ability to survive within the host, alternating between active and latent disease states, and escaping the immune system defences. There is an urgent need for new antibiotics active against drug-resistant organisms and that can shorten standard therapy due to the extended duration of anti-TB regimens and the increasing prevalence of multidrug- (MDR) and extensively drug-resistant (XDR) M. Read More

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http://dx.doi.org/10.2174/1568026619666190219105722DOI Listing
February 2019
1 Read

Docking Assisted Prediction And Biological Evaluation Of Sideritis L. Components With Ptp1b Inhibitory Action And Probable Anti-Diabetic Properties.

Curr Top Med Chem 2019 Feb 18. Epub 2019 Feb 18.

Department of Medical Laboratory Studies, School of Health and Medical Care, Alexander Technological Educational Institute of Thessaloniki, ATEITH campus, Sindos, 57400, Thessaloniki. Greece.

Background: The main characteristic of Diabetes type II is the impaired activation of intracellular mechanisms triggered by the action of insulin. PTP1b is a Protein Tyrosine Phosphatase that dephosphorylates insulin receptor causing its desensitization. Since, inhibition of PTP1b may prolong insulin receptor activity, PTP1b has become a drug target for the treatment of Diabetes II. Read More

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http://dx.doi.org/10.2174/1568026619666190219104430DOI Listing
February 2019
1 Read
3.402 Impact Factor

Anti-Cancer Drug Discovery: Structure, Function and Novel Strategy - (Part-I).

Authors:
Suman S Thakur

Curr Top Med Chem 2018 ;18(30):2543

Proteomics and Cell Signaling, Lab E409 Centre for Cellular & Molecular Biology Habsiguda, Uppal Road Hyderabad - 500 007 Telangana, India.

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http://dx.doi.org/10.2174/156802661830190213150943DOI Listing

Targeting Epigenetic Targets for Cancer Therapy.

Authors:
Bin Yu

Curr Top Med Chem 2018 ;18(28):2379

Henan Provincial Key Laboratory of Children's Genetics and Metabolic Diseases Children's Hospital Affiliated to Zhengzhou University Zhengzhou Children's Hospital. School of Pharmaceutical Sciences Zhengzhou University Zhengzhou 45001, China.

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http://dx.doi.org/10.2174/156802661828190212093039DOI Listing

Current Advances in Computational Approaches for Drug Discovery- Part II.

Authors:
Amit K Gupta

Curr Top Med Chem 2018 ;18(27):2267

Keck Computational Biology Fellow Department of Integrative Biology and Pharmacology The University of Texas Health Science Center at Houston, 6431 Fannin Street, Houston TX 77030, United States.

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http://www.eurekaselect.com/169260/article
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http://dx.doi.org/10.2174/156802661827190123105909DOI Listing
April 2019
3 Reads

Quinoline-based Protein-protein Interaction Inhibitors of LEDGF/p75 and HIV Integrase: An In Silico Study.

Curr Top Med Chem 2018 ;18(32):2800-2815

Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, 151001, India.

The failure of the Integrase Strand Transfer Inhibitors (INSTIs) due to the mutations occurring at the catalytic site of HIV integrase (IN) has led to the design of allosteric integrase inhibitors (ALLINIs). Lens epithelium derived growth factor (LEDGF/p75) is the host cellular cofactor which helps chaining IN to the chromatin. The protein-protein interactions (PPIs) were observed at the allosteric site (LEDGF/p75 binding domain) between LEDGF/p75 of the host cell and IN of virus. Read More

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http://dx.doi.org/10.2174/1568026619666190208164801DOI Listing
April 2019
1 Read
3.402 Impact Factor