SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL SCREENING OF DIANDRINE A.

Abstract

Synthesis of a proline-rich cyclic hexapeptide - diandrine A [VI] was accomplished by coupling of tetrapeptide unit Boc-Gly-Pro-Trp-Pro-OH with dipeptide unit Tyr-Phe-OMe followed by cyclization of linear peptide unit [V] under alkaline condition. Structure of newly synthesized cyclopolypeptide was elucidated by means of spectral techniques including FTIR, 'H NMR, "C NMR, MS analyses. VI was subjected to pharmacological screening and found to exhibit good antifungal activity against dermatophytes. Further, VI possessed potent antihelmintic activity against earthworms M. konkanensis, P. corthruses and Eudrilus sp.