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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antileishmanial activity of piperoyl-amino acid conjugates.
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Synthesis and antileishmanial activity of piperoyl-amino acid conjugates.

机译：哌酰基-氨基酸缀合物的合成和抗衰老活性。

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摘要

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.
机译：基于已报道的天然生物碱胡椒碱和氨基酸酯的抗衰老活性，通过将胡椒碱水解为胡椒酸，然后与氨基酸甲酯反应来合成它们的结合物。这些缀合物进一步转化为具有游离羧基和具有减少的双键的化合物。评价了合成的化合物在体外对前鞭毛体和鞭毛体形式的多诺氏乳杆菌的活性。所有化合物均显示出比胡椒碱或氨基酸甲酯更好的活​​性。哌酰基-缬氨酸甲酯是最具活性的化合物，对变形虫的IC50为0.075 mM。评价了两种活性化合物在利什曼病的金黄仓鼠模型中的体内活性。

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