5-烷基-2-脲取代吡啶：具有改进性质的有效葡萄糖激酶激活剂的鉴定

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

作者信息

Kohn Todd J, Du Xiaohui, Lai SuJen, Xiong YuMei, Komorowski Renee, Veniant Murielle, Fu Zice, Jiao Xianyun, Pattaropong Vatee, Chow David, Cardozo Mario, Jin Lixia, Conn Marion, DeWolf Walter E, Kraser Christopher F, Hinklin Ronald J, Boys Mark L, Medina Julio C, Houze Jonathan, Dransfield Paul, Coward Peter

机构信息

Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.

Amgen Inc. , 1120 Veterans Boulevard, South San Francisco, California 94080, United States.

出版信息

ACS Med Chem Lett. 2016 Jun 1;7(7):666-70. doi: 10.1021/acsmedchemlett.6b00145. eCollection 2016 Jul 14.

DOI:10.1021/acsmedchemlett.6b00145

PMID:27437074

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4948010/

Abstract

Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure-activity relationship studies are presented along with relevant pharmacokinetic and in vivo data.

摘要

鉴定出两种1-(4-芳基-5-烷基-吡啶-2-基)-3-甲基脲葡萄糖激酶激活剂，它们在体内具有强大的疗效。这两种化合物的溶解度高于先前鉴定出的三芳基化合物（即AM-2394）。本文介绍了构效关系研究以及相关的药代动力学和体内数据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dc26/4948010/df75430dff27/ml-2016-00145b_0002.jpg

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5-烷基-2-脲取代吡啶：具有改进性质的有效葡萄糖激酶激活剂的鉴定

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

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5-烷基-2-脲取代吡啶：具有改进性质的有效葡萄糖激酶激活剂的鉴定

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

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