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

Pal, Sudip ; Ghosh, Uttam ; Singh, Gajendra ; Alam, Faiyaz ; Singh, Shyam ; Chopra, Sidharth ; Sinha, Sudhir ; Ampapathi, Ravi Sankar ; Chakraborty, Tushar Kanti (2017) Synthesis, Conformational Studies and Biological Profiles of Tetrahydrofuran Amino-Acid-Containing Cationic Antitubercular Peptides Asian Journal of Organic Chemistry, 6 (9). pp. 1240-1249. ISSN 21935807

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Official URL: http://doi.org/10.1002/ajoc.201700183

Related URL: http://dx.doi.org/10.1002/ajoc.201700183

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:Article
Source:Copyright of this article belongs to John Wiley & Sons, Inc.
ID Code:131085
Deposited On:02 Dec 2022 10:09
Last Modified:02 Dec 2022 10:09

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