Literature DB >> 23265877

One pot solvent free synthesis and in vitro antitubercular screening of 3-Aracylphthalides against Mycobacterium tuberculosis.

Rohan A Limaye1, Virendra B Kumbhar, Arun D Natu, Madhusudan V Paradkar, Varsha S Honmore, Rubia R Chauhan, Suwarna P Gample, Dhiman Sarkar.   

Abstract

One pot synthesis of 3-Aracylphthalide was accomplished in good yield by reacting 2-carboxy benzaldehyde with various aromatic methyl ketones in presence of methane sulphonic acid. Various phthalides thus obtained were characterized with spectral techniques. These phthalides were subjected to in vitro antitubercular screening against Mycobacterium tuberculosis H37Ra (MTB) by using XRMA protocol. Among the phthalides screened, four exhibited half maximal inhibitory concentration (IC(50)) in the range of 0.81-1.24 μg/ml thereby providing potential lead compounds for future drug discovery studies.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23265877     DOI: 10.1016/j.bmcl.2012.11.097

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis.

Authors:  Vadim Makarov; Elena Salina; Robert C Reynolds; Phyo Phyo Kyaw Zin; Sean Ekins
Journal:  J Med Chem       Date:  2020-04-20       Impact factor: 7.446

2.  Sustainable synthesis of 3-substituted phthalides via a catalytic one-pot cascade strategy from 2-formylbenzoic acid with β-keto acids in glycerol.

Authors:  Lina Jia; Fuzhong Han
Journal:  Beilstein J Org Chem       Date:  2017-07-19       Impact factor: 2.883

3.  Synthesis and Spectral Characterization of Benzo-[6,7][1,5]diazocino[2,1-a]isoindol-12-(14H)-one Derivatives.

Authors:  Jatinder P Bassin; Bhavani Anagani; Christopher Benham; Madhu Goyal; Maryam Hashemian; Ute Gerhard
Journal:  Molecules       Date:  2016-07-23       Impact factor: 4.411

  3 in total

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