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

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.