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Chemoenzymatic synthesis and biological evaluation of 2- and 3-hydroxypyridine derivatives against Leishmania mexicana.

Abstract：

:A series of hydroxyalkyl and acyloxyalkyl derivatives of 2- and 3-hydroxypyridine was synthesized and their biological activity was evaluated as growth inhibitors of protozoan Leishmania mexicana. Thirty novel compounds were obtained through a chemoenzymatic methodology in two reaction steps. The influence of various reaction parameters in the enzymatic step, such as enzyme source, acylating agent/substrate ratio, enzyme/substrate ratio, solvent and temperature, was studied. Some of the evaluated compounds showed a remarkable activity as Leishmania mexicana growth inhibitors, obtaining the best results with the acetylated derivatives. The advantages showed by the enzymatic methodology, such as mild reaction conditions and low environmental impact, make the biocatalysis a convenient way to prepare these derivatives of substituted pyridines with application as potential antiparasitic agents.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

García Liñares G,Parraud G,Labriola C,Baldessari A

doi

10.1016/j.bmc.2012.06.028

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

4614-24

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00506-8

journal_volume

20

pub_type

杂志文章

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