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Thioamide hydroxypyrothiones supersede amide hydroxypyrothiones in potency against anthrax lethal factor.

Abstract：

:Anthrax lethal factor (LF) is a critical virulence factor in the pathogenesis of anthrax. A structure-activity relationship (SAR) of potential lethal factor inhibitors (LFi) is presented in which the zinc-binding group (ZBG), linker, and backbone moieties for a series of hydroxypyrone-based compounds were systematically varied. It was found that hydroxypyrothione ZBGs generate more potent inhibitors than hydroxypyrone ZBGs. Furthermore, coupling the hydroxypyrothione to a backbone group via a thioamide bond improves potency when compared to an amide linker. QM/MM studies show that the thioamide bond in these inhibitors allows for the formation of two additional hydrogen bonds with the protein active site. In both types of hydroxypyrothione compounds, ligand efficiencies of 0.29-0.54 kcal mol(-1) per heavy atom were achieved. The results highlight the need for a better understanding to optimize the interplay between the ZBG, linker, and backbone to get improved LFi.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Agrawal A,de Oliveira CA,Cheng Y,Jacobsen JA,McCammon JA,Cohen SM

doi

10.1021/jm8013212

subject

Has Abstract

pub_date

2009-02-26 00:00:00

pages

1063-74

issue

4

eissn

0022-2623

issn

1520-4804

pii

10.1021/jm8013212

journal_volume

52

pub_type

杂志文章

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