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Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors.

Abstract：

:Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic, a modified dione scaffold was designed and elaborated into a >300 member library, which was subsequently screened to establish the SAR for esterase inhibition. This allowed the identification of single digit nanomolar hiCE inhibitors that showed improvement in selectivity and measured solubility.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Young BM,Hyatt JL,Bouck DC,Chen T,Hanumesh P,Price J,Boyd VA,Potter PM,Webb TR

doi

10.1021/jm101101q

subject

Has Abstract

pub_date

2010-12-23 00:00:00

pages

8709-15

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

53

pub_type

杂志文章

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