Synthesis and Biological Evaluation of Coumarin Derivatives as Inhibitors of Mycobacterium bovis (BCG).

Ali Hossein Rezayan (1) , Parisa Azerang (2) , Soroush Sardari (3) , Afshin Sarvary (4)

1 Department of Life Science Engineering
2 Institut Pasteur d'Iran
3 Drug Design and Bioinformatics Unit
4 Department of Chemistry

The coumarin compounds are an important class of biologically active molecules, which have attractive caught the attention of many organic and medicinal chemists, due to potential pharmaceutical implications and industrial applications. We herein report the one-pot procedure for the efficient synthesis of coumarin derivatives using commercially available substrates via isocyanide-based multicomponent condensation reactions. These compounds were evaluated for anti-mycobacterium activity against Mycobacterium bovis (Bacillus Calmette-Guerin). The preliminary results indicated that all of the tested compounds showed relatively good activity against the test organism. The compounds 7e, 7l, and 7m showed high anti-tuberculosis activity.

Keywords: coumarin derivatives; multicomponent reaction; Mycobacterium bovis

Domains: Life Sciences [q-bio]; Pharmaceutical sciences; Pharmacology

Ali Hossein Rezayan, Parisa Azerang, Soroush Sardari, Afshin Sarvary. Synthesis and Biological Evaluation of Coumarin Derivatives as Inhibitors of Mycobacterium bovis (BCG).. Chemical Biology and Drug Design, 2012, 80 (6), pp.929-36. ⟨10.1111/cbdd.12044⟩. ⟨pasteur-00753191⟩