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Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.

Abstract：

:A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Keith JM,Jones W,Pierce JM,Seierstad M,Palmer JA,Webb M,Karbarz M,Scott BP,Wilson SJ,Luo L,Wennerholm M,Chang L,Rizzolio M,Rynberg R,Chaplan S,Guy Breitenbucher J

doi

10.1016/j.bmcl.2020.127463

subject

Has Abstract

pub_date

2020-10-15 00:00:00

pages

127463

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(20)30574-6

journal_volume

30

pub_type

杂志文章

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