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

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

doi:10.1016/j.bmcl.2012.11.097

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

Bioorg Med Chem Lett. 2013 Feb 1;23(3):711-4. doi: 10.1016/j.bmcl.2012.11.097. Epub 2012 Dec 3.

Authors

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

Affiliation

¹ Post Graduate & Research Centre, Department of Chemistry, MES Abasaheb Garware College, Pune, India.

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

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.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Antitubercular Agents / chemical synthesis*
Antitubercular Agents / pharmacology*
Benzofurans / chemical synthesis*
Benzofurans / chemistry
Benzofurans / pharmacology*
Drug Discovery*
Humans
Inhibitory Concentration 50
Molecular Structure
Mycobacterium tuberculosis / drug effects*
Solvents

Substances

Antitubercular Agents
Benzofurans
Solvents