Expansion of a novel lead targeting M. tuberculosis DHFR as antitubercular agents.

Antitubercular Agents / chemical synthesis Dose-Response Relationship, Drug Enzyme Inhibitors / chemical synthesis Humans Indoles / chemical synthesis Microbial Sensitivity Tests Models, Molecular Molecular Structure Mycobacterium tuberculosis / drug effects Structure-Activity Relationship Tetrahydrofolate Dehydrogenase / metabolism

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 04 2019
Historique:
received: 19 11 2018
revised: 21 02 2019
accepted: 25 02 2019
pubmed: 5 3 2019
medline: 28 2 2020
entrez: 5 3 2019
Statut: ppublish

Résumé

A series of 1-(1-benzyl-2-methyl-5-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-1H-indol-3-yl)ethanone and ethyl 1-benzyl-2-methyl-5-((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)-1H-indole-3-carboxylate derivatives were designed based on bioisosteric replacement of previously reported antitubercular agent (IND-07). Twenty ligands were successfully synthesized and some of them were found to have good in vitro activity (MIC < 10 μM) against the H

Identifiants

DOI: 10.1016/j.bmc.2019.02.053 PMID: 30827867
pubmed: 30827867
pii: S0968-0896(18)31967-9
doi: 10.1016/j.bmc.2019.02.053
pii:
doi:

Substances chimiques

Antitubercular Agents 0
Enzyme Inhibitors 0
Indoles 0
Tetrahydrofolate Dehydrogenase EC 1.5.1.3

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1421-1429

Informations de copyright

Copyright © 2019 Elsevier Ltd. All rights reserved.

Auteurs

Kalicharan Sharma (K)

Department of Pharmaceutical Chemistry, SPER, Jamia Hamdard, New Delhi 110062, India.

Omprakash Tanwar (O)

Department of Pharmaceutical Chemistry, SPER, Jamia Hamdard, New Delhi 110062, India.

Girdhar Singh Deora (GS)

Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

S Ali (S)

Department of Biochemistry, SCLS, Jamia Hamdard, New Delhi 110062, India; Bioinformatics Infrastructure Facility Lab, Jamia Hamdard, New Delhi 110062, India.

M M Alam (MM)

Department of Pharmaceutical Chemistry, SPER, Jamia Hamdard, New Delhi 110062, India.

M S Zaman (MS)

Department of Pharmaceutical Chemistry, SPER, Jamia Hamdard, New Delhi 110062, India.

Vagolu Siva Krishna (VS)

Department of Pharmacy, Birla Institute of Technology & Science, Pilani, Hyderabad 500078, India.

Dharmarajan Sriram (D)

Department of Pharmacy, Birla Institute of Technology & Science, Pilani, Hyderabad 500078, India.

Mymoona Akhter (M)

Department of Pharmaceutical Chemistry, SPER, Jamia Hamdard, New Delhi 110062, India; Department of Biochemistry, SCLS, Jamia Hamdard, New Delhi 110062, India. Electronic address: mymoonaakhter@gmail.com.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Antituberculeux › Expansion of a novel lead targeting M....
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Expansion of a novel lead targeting M....
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Expansion of a novel lead targeting M....
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Expansion of a novel lead targeting M....
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Expansion of a novel lead targeting M....
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Expansion of a novel lead targeting M....
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › Expansion of a novel lead targeting M....
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Expansion of a novel lead targeting M....
questionsmedicales.fr › Bactéries › Bactéries à Gram positif › Bâtonnets à Gram positif › Bâtonnets asporogènes à Gram positif › Bâtonnets asporogènes réguliers à Gram positif › Mycobacteriaceae › Mycobacterium › Mycobacterium tuberculosis › Expansion of a novel lead targeting M....
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Expansion of a novel lead targeting M....
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Oxidoreductases acting on CH-NH group donors › Dihydrofolate reductase › Expansion of a novel lead targeting M....