当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.

Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2014.06.075

subject

Has Abstract

pub_date

2014-09-12 00:00:00

pages

118-26

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00604-7

journal_volume

84

pub_type

杂志文章

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