EMAIL THIS PAGE TO A FRIEND

European journal of medicinal chemistry

Synthesis and antileishmanial activity of piperoyl-amino acid conjugates.


PMID 20546981

Abstract

Based on reported antileishmanial activity of naturally occurring alkaloid piperine and amino acid esters, their conjugates were synthesized by the hydrolysis of piperine to piperic acid followed by reaction with amino acid methyl esters. These conjugates were further converted to compounds with free carboxyl group and those with reduced double bonds. The synthesized compounds were evaluated for activity against promastigote and amastigote forms of L. donovani in vitro. All the compounds showed better activity than either piperine or the amino acid methyl esters. Piperoyl-valine methyl ester was the most active compound showing an IC50 of 0.075 mM against the amastigotes. Two active compounds were evaluated for in vivo activity in golden hamster model of leishmaniasis.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

T90808
L-Tyrosine methyl ester, 98%
C10H13NO3
P49007
Piperine, ≥97%
C17H19NO3