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Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-08-09 , DOI: 10.1016/j.bmcl.2020.127463 John M Keith 1 , William Jones 1 , Joan M Pierce 1 , Mark Seierstad 1 , James A Palmer 1 , Michael Webb 1 , Mark Karbarz 1 , Brian P Scott 1 , Sandy J Wilson 1 , Lin Luo 1 , Michelle Wennerholm 1 , Leon Chang 1 , Michele Rizzolio 1 , Raymond Rynberg 1 , Sandra Chaplan 1 , J Guy Breitenbucher 1
中文翻译：
具有稠合双环二胺核心的杂芳基脲，可作为脂肪酸酰胺水解酶的抑制剂。
更新日期：2020-08-10
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-08-09 , DOI: 10.1016/j.bmcl.2020.127463 John M Keith 1 , William Jones 1 , Joan M Pierce 1 , Mark Seierstad 1 , James A Palmer 1 , Michael Webb 1 , Mark Karbarz 1 , Brian P Scott 1 , Sandy J Wilson 1 , Lin Luo 1 , Michelle Wennerholm 1 , Leon Chang 1 , Michele Rizzolio 1 , Raymond Rynberg 1 , Sandra Chaplan 1 , J Guy Breitenbucher 1
Affiliation
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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.
中文翻译：
具有稠合双环二胺核心的杂芳基脲，可作为脂肪酸酰胺水解酶的抑制剂。
描述了一系列基于机制的具有稠合双环二胺核的杂芳基脲脂肪酸酰胺水解酶（FAAH）抑制剂。与围绕哌嗪核心构建的化合物形成对比，大多数制备的带有稠合双环二胺的类似物对rFAAH的抑制作用均比人类酶高。在体内鉴定并鉴定了对两种物种均等的几种化合物。
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