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Synthesis, antimicrobial and cytotoxic activity of new heterocyclic hybrids based on 2,5-dimethylpyrrole and pyrrole scaffolds

Authors :
Venkatrao H. Kulkarni
Shrinivas D. Joshi
Uttam A. More
Source :
Indian Journal of Pharmaceutical Sciences
Publication Year :
2013
Publisher :
OMICS Publishing Group, 2013.

Abstract

A series of 4-(2,5-dimethylpyrrol-1-yl)/4-pyrrol-1-yl benzoic acid hydrazide analogs, some derived triazoles, azetidinones, thiazolidinones, and pyrroles have been synthesized in good yields and structures of these compounds were established by IR, 1 H NMR, 13 C NMR, mass spectral, and elemental analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal, and antitubercular activity against Mycobacterium tuberculosis H 37 Rv strain by the broth dilution assay method. Twenty one of these compounds displayed good antimicrobial activity, with a MIC value of 1-4 μg/ml. Several compounds 4c, 8-10, 15b-15h, and 16b-16d exhibited good in vitro antitubercular activity with MIC value 1-2 μg/ml. Further, some title compounds were also assessed for their cytotoxic activity (IC 50 ) against mammalian Vero cell lines and A 549 (lung adenocarcinoma) cell lines using the MTT assay method. The results revealed that these compounds exhibit antitubercular activity at non-cytotoxic concentrations.

Details

ISSN :
0250474X
Volume :
75
Database :
OpenAIRE
Journal :
Indian Journal of Pharmaceutical Sciences
Accession number :
edsair.doi.dedup.....6304b23e78a1c66ad44e311be757b91e