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Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.喹啉-2,4(1H,3H)-二酮的发展作为大麻素受体 2 的有效和选择性配体。
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A randomized, controlled study to investigate the analgesic efficacy of single doses of the cannabinoid receptor-2 agonist GW842166, ibuprofen or placebo in patients with acute pain following third molar tooth extraction.一项随机、对照研究，旨在探讨大麻素受体-2 激动剂 GW842166、布洛芬或安慰剂单次给药在第三磨牙拔除后急性疼痛患者中的镇痛效果。
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Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.发现2-[(2,4-二氯苯基)氨基]-N-[(四氢-2H-吡喃-4-基)甲基]-4-(三氟甲基)-5-嘧啶甲酰胺，一种用于治疗炎性疼痛的选择性CB2受体激动剂。
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Rimonabant.利莫那班
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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.

DOI:10.1021/acsmedchemlett.7b00007
PMID:28626532
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5467194/
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。