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  • Title: Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.
    Author: Pagadala LR, Mukkara LD, Singireddi S, Singh A, Thummaluru VR, Jagarlamudi PS, Guttala RS, Perumal Y, Dharmarajan S, Upadhyayula SM, Ummanni R, Basireddy VS, Ravirala N.
    Journal: Eur J Med Chem; 2014 Sep 12; 84():118-26. PubMed ID: 25016370.
    Abstract:
    A novel synthesis of highly substituted pyrrole-N-acetic derivatives is described through the coupling of 1,4-diketones with amino acids following Paal-Knorr's approach. These pyrrole-N-acetic acid derivatives are found to exhibit potent anti-mycobacterial activity against Mycobacterium smegmatis and Mycobacterium tuberculosis strain H37Rv. In particular, 5n, 5q &5r are found to display excellent anti-mycobacterial activity against M. tuberculosis strain H37Rv with MIC values in the range of 2.97 μM. Conversely, these compounds showed low cytotoxicity (selectivity index: >16.83) against HEK-293T cell line.
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