Synthesis, Conformational Studies and Biological Profiles of Tetrahydrofuran Amino-Acid-Containing Cationic Antitubercular Peptides

Pal, Sudip and Ghosh, Uttam and Singh, Gajendra and Alam, Faiyaz and Singh, Shyam and Chopra, Sidharth and Sinha, Sudhir and Ampapathi, Ravi Sankar and Chakraborty, Tushar Kanti (2017) Synthesis, Conformational Studies and Biological Profiles of Tetrahydrofuran Amino-Acid-Containing Cationic Antitubercular Peptides. In: ASIAN JOURNAL OF ORGANIC CHEMISTRY, 6 (9, SI). pp. 1240-1249.

PDF Asi_Jou_Org_Che_6-9_1240_2017.pdf - Published Version Restricted to Registered users only Download (1MB) | Request a copy

Abstract

Linear cationic tetra- and octapeptides containing a tetrahydrofuran amino acid were synthesised, a conformational analysis performed, and their structure-activity relationships explored by evaluating their antibacterial, antitubercular and cytotoxic properties. Only the octapeptides showed activities, which was weak to moderate against Gram-positive and Gram-negative bacteria for only two peptides, but was very significant against Mycobacterium tuberculosis, and peptides were devoid of toxicity towards mammalian Vero cells. N-Terminus-deprotected esters showed the best results with excellent selectivity for M.tuberculosis and these peptides promise to be potential leads.

Item Type:	Journal Article
Publication:	ASIAN JOURNAL OF ORGANIC CHEMISTRY
Additional Information:	Copy right for this article belongs to the WILEY-V C H VERLAG GMBH, POSTFACH 101161, 69451 WEINHEIM, GERMANY
Department/Centre:	Division of Chemical Sciences > Organic Chemistry
Date Deposited:	13 Oct 2017 04:52
Last Modified:	13 Oct 2017 04:52
URI:	http://eprints.iisc.ac.in/id/eprint/58026

Actions (login required)

View Item