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The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections.

Abstract：

:Two series of ω-phenoxy contained acylhydroxamic acids as novel urease inhibitors were designed and synthesized. Biological activity evaluations revealed that ω-phenoxypropinoylhydroxamic acids were more active than phenoxyacetohydroxamic acids. Out of these compounds, 3-(3,4-dichlorophenoxy)propionylhydroxamic acid c24 showed significant potency against urease in both cell free extract (IC50 = 0.061 ± 0.003 μM) and intact cell (IC50 = 0.89 ± 0.05 μM), being over 450- and 120-fold more potent than the clinically prescribed urease inhibitor AHA, repectively. Non-linear fitting of experimental data (V-[S]) suggested a mixed-type inhibition mechanism and a dual site binding mode of these compounds.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Ni WW,Liu Q,Ren SZ,Li WY,Yi LL,Jing H,Sheng LX,Wan Q,Zhong PF,Fang HL,Ouyang H,Xiao ZP,Zhu HL

doi

10.1016/j.bmc.2018.07.003

subject

Has Abstract

pub_date

2018-08-07 00:00:00

pages

4145-4152

issue

14

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(18)31043-5

journal_volume

26

pub_type

杂志文章

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