Tetrahydrofuran amino acid-containing gramicidin S analogues with improved biological profiles

Pal, Sudip and Singh, Gajendra and Singh, Shyam and Tripathi, Jitendra Kumar and Ghosh, Jimut Kanti and Sinha, Sudhir and Ampapathi, Ravi Sankar and Chakraborty, Tushar Kanti (2015) Tetrahydrofuran amino acid-containing gramicidin S analogues with improved biological profiles. In: ORGANIC & BIOMOLECULAR CHEMISTRY, 13 (24). pp. 6789-6802.

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Abstract

Gramicidin S (GS) is a cyclic cationic antimicrobial peptide (CAP) with a wide spectrum of antibiotic activities whose usage has been limited to topical applications owing to its cytotoxic side effects. We have synthesized tetrahydrofuran amino acid (Taa)-containing GS analogues, and we have carried out conformational analysis and explored their structure activity relationships by evaluating their antitubercular, antibacterial and cytotoxic properties. Two of these analogues showed impressive as well as selective activity against Mycobacterium tuberculosis (MTB) without toxicity towards mammalian Vero cells or human RBCs, and are promising as potential leads.

Item Type:	Journal Article
Publication:	ORGANIC & BIOMOLECULAR CHEMISTRY
Publisher:	ROYAL SOC CHEMISTRY
Additional Information:	Copy right for this article belongs to the ROYAL SOC CHEMISTRY, THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND
Department/Centre:	Division of Chemical Sciences > Organic Chemistry
Date Deposited:	19 Jul 2015 09:43
Last Modified:	19 Jul 2015 09:43
URI:	http://eprints.iisc.ac.in/id/eprint/51900

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