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Phenylhydrazides as inhibitors of Leishmania amazonensis arginase and antileishmanial activity.

Abstract：

:Searching for new substances with antileishmanial activity, we synthesized and evaluated a series of α,α-difluorohydrazide and α,α-difluoramides against Leishmania amazonensis arginase (LaArg). Four α,α-difluorohydrazide derivatives showed activity against LaArg with Ki in the range of 1.3-26 μM. The study of the kinetics of LaArg inhibition showed that these substances might act via different inhibitory mechanisms or even by a combination of these. The compounds were tested against L. amazonensis promastigotes and the best result was obtained to the compound 4 (EC50 of 12.7 ± 0.3 μM). In addition, in order to obtain further insight into the binding mode of such compounds, molecular docking studies were performed to obtain additional validation of experimental results. Considering these results, it is possible to conclude that α,α-difluorohydrazide derivatives are a promising scaffold in the development of new substances against the etiological agent of leishmaniasis by targeting LaArg.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Crizanto de Lima E,Castelo-Branco FS,Maquiaveli CC,Farias AB,Rennó MN,Boechat N,Silva ER

doi

10.1016/j.bmc.2019.07.022

subject

Has Abstract

pub_date

2019-09-01 00:00:00

pages

3853-3859

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(19)30316-5

journal_volume

27

pub_type

杂志文章

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