The Clitocybins and 2-Substituted-Isoindolin-1-Ones: Synthesis and in Vitro Antimycobacterial Activities

JOURNAL OF ADVANCES IN CHEMISTRY

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Title The Clitocybins and 2-Substituted-Isoindolin-1-Ones: Synthesis and in Vitro Antimycobacterial Activities
 
Creator Mejai, Amani
Rakotoarivelo , Nambinina V.
Najahi , Ennaji
Perio , Pierre
Hollande, Etienne
Pasca, Maria Rosalia
Abidi, Rym
Nepveu , Françoise
 
Subject Isoindolinone
Tuberculosis
Clitocybins
Cytotoxicity
Antibiotics
study biological activity of isoindolinone
 
Description Despite strong indications of antimycobacterial activities for clitocybins reported since 1945, no reports linking chemical structure and activity have been reported in the literature since then. In this study, we synthesized some clitocybin derivatives (also called 2-substituted-isoindolinones), and tested their activities and carried out some chemical derivations. Isoindolinones were prepared from methyl 2-formyl-3,5-dimethoxybenzoate and various primary aromatic amines. Compounds were evaluated for in vitro activity against Mycobacterium tuberculosis H37Rv, as well as for cytotoxicity (CC50) on the Vero cell line. 4,6-dihydroxy-2-(4-hydroxyphenyl)isoindolin-1-one, 7, and 4-hydroxy-2-(4-hydroxyphenyl)-6-methoxy-isoindol-1-one, 5, exhibited the highest antimycobacterial activities (minimum inhibitory concentration = 19.45 µM and 18.45 µM, respectively) and were non-toxic (CC50 = 30 µM and 29 µM, respectively).
 
Publisher KHALSA PUBLICATIONS
 
Date 2019-10-28
 
Type info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
Peer-reviewed Article
 
Format application/pdf
 
Identifier http://rajpub.com/index.php/jac/article/view/8476
10.24297/jac.v16i0.8476
 
Source JOURNAL OF ADVANCES IN CHEMISTRY; Vol. 16 (2019); 5387-5394
2321-807X
 
Language eng
 
Relation http://rajpub.com/index.php/jac/article/view/8476/7850
 
Rights Copyright (c) 2019 amani mejai
http://creativecommons.org/licenses/by/4.0
 

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