喹唑啉/嘧啶-2,4(1,3)-二酮作为大麻素2型受体激动剂的开发
Development of Quinazoline/Pyrimidine-2,4(1,3)-diones as Agonists of Cannabinoid Receptor Type 2.
作者信息
Qian Hai-Yan, Wang Zhi-Long, Pan You-Lu, Chen Li-Li, Xie Xin, Chen Jian-Zhong
机构信息
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, P. R. China.
CAS Key Laboratory of Receptor Research, National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, P. R. China.
出版信息
ACS Med Chem Lett. 2017 May 1;8(6):678-681. doi: 10.1021/acsmedchemlett.7b00007. eCollection 2017 Jun 8.
Abstract
Starting from a prototypical structure , we describe our efforts to design and obtain novel quinazoline/pyrimidine-2,4(1,3)-diones with high CB2 agonist potency and selectivity as well as improved physicochemical characteristics, mainly hydrophilicity. The most potent and selective CB2 agonists, and , in this series were also endowed with lower logP values than that of GW842166X and lead compound . These derivatives appear to be promising lead compounds for the development of future CB2 agonists.
摘要
从一个原型结构出发，我们描述了为设计并获得具有高CB2激动剂效力和选择性以及改善的物理化学特性（主要是亲水性）的新型喹唑啉/嘧啶-2,4(1,3)-二酮所做的努力。该系列中最有效和选择性最高的CB2激动剂 和 ，其logP值也低于GW842166X和先导化合物 。这些衍生物似乎是开发未来CB2激动剂的有前景的先导化合物。
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