Journal of Medicinal Chemistry p. 5751 - 5769 (2015)
Update date:2022-08-28
Topics:
Han, Shuang
Zhang, Fei-Fei
Qian, Hai-Yan
Chen, Li-Li
Pu, Jian-Bin
Xie, Xin
Chen, Jian-Zhong
The cannabinoid type 2 receptors (CB2Rs) play crucial roles in inflammatory diseases. There has been considerable interest in developing potent and selective ligands for CB2R. In this study, quinoline-2,4(1H,3H)-dione analogs have been designed, synthesized, and evaluated for their potencies and binding properties toward the cannabinoid type 1 receptor (CB1R) and CB2R. C5- or C8-substituted quinoline-2,4(1H,3H)-diones demonstrate CB2R agonist activity, while the C6- or C7-substituted analogs are antagonists of CB2R. In addition, oral administration of 21 dose-dependently alleviates the clinical symptoms of experimental autoimmune encephalomyelitis in a mouse model of multiple sclerosis and protects the central nervous system from immune damage. Furthermore, the interaction modes predicted by docking simulations and the 3D-QSAR model generated with CoMFA may offer guidance for further design and modification of CB2R modulators.
View MoreJinan Jiaquan Chemical Co.,Ltd
Contact:+86-531-62318366
Address:Room 502 of Yidonghuayuan No.601 Huaxin Road Licheng District Jinan China
Contact:+1-284-4950244
Address:Box 3069, Road Town, Tortola, British Virgin Islands
Hubei Xinjing New Material Co.,Ltd
Contact:+86-27-83313147
Address:Room402.#Bthe 7th,Headquarter of Huifeng Corporation Qiaokou District,Wuhan China
Springchem New Material Technology Co.,Limited
website:http://www.spring-chem.com
Contact:86-21-62885108
Address:602B, Building 1, No. 641, Tianshan Road
Luojiang Chenming Biological Products Co
Contact:+86 15000297032
Address:GROUP NO.4, HE SHENG VILLAGE, PANLONG TOWN,
Doi:10.1063/1.3263942
(2009)Doi:10.1080/00397910008086915
(2000)Doi:10.3390/md10122912
(2012)Doi:10.1016/j.jssc.2008.05.013
(2008)Doi:10.1039/c8dt02848f
(2018)Doi:10.1016/S0022-328X(98)01172-3
(1999)