One pot solvent free synthesis and in vitro antitubercular screening of 3-aracylphthalides against mycobacterium tuberculosis

TitleOne pot solvent free synthesis and in vitro antitubercular screening of 3-aracylphthalides against mycobacterium tuberculosis
Publication TypeJournal Article
Year of Publication2013
AuthorsLimaye, RA, Kumbhar, VB, Natu, AD, Paradkar, MV, Honmore, VS, Chauhan, RR, Gample, SP, Sarkar, D
JournalBioorganic & Medicinal Chemistry Letters
Volume23
Issue3
Pagination711-714
Date PublishedFEB
ISSN0960-894X
Keywords3-Aracylphthalide, Antitubercular activity, Methane sulphonic acid, One pot synthesis
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 (IC50) in the range of 0.81-1.24 mu g/ml thereby providing potential lead compounds for future drug discovery studies. (c) 2012 Elsevier Ltd. All rights reserved.

DOI10.1016/j.bmcl.2012.11.097
Type of Journal (Indian or Foreign)

Foreign

Impact Factor (IF)

2.331

Divison category: 
Organic Chemistry