Bioorganic and Medicinal Chemistry Letters p. 1084 - 1089 (2010)
Update date:2022-07-29
Topics:
Lange, Jos H.M.
van der Neut, Martina A.W.
Wals, Henri C.
Kuil, Gijs D.
Borst, Alice J.M.
Mulder, Arie
den Hartog, Arnold P.
Zilaout, Hicham
Goutier, Wouter
van Stuivenberg, Herman H.
van Vliet, Bernard J.
The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold).
View MoreHubei Lingsheng Pharmaceuticals Co., Ltd.
Contact:+86-0710-3538058
Address:Xiangyang City Xiangcheng Economic Development Zone, Hubei Province
Contact:17316303296
Address:240 Amboy Ave
Beijing Harmony Chemical Co., Ltd.
Contact:86-010-84956928
Address:Room 207, Jin feng he B building, No 8 Xin Jie Kou Wai Street, Xi Cheng District, Beijing,PRC. 10008
Beijing Mediking Biopharm Co., Ltd.
Contact:+86-10-89753524/81760121/81769521
Address:Hongxianghong Incubator, Beiqijia Town, Changping district, Beijing, China
Fujian Wanke Pharmaceutical Co., LTD.
Contact:+86-598-5026002
Address:Economic development zone,jiangle county
Doi:10.1021/ic801879x
(2009)Doi:10.1007/BF01518096
(1935)Doi:10.1016/j.jorganchem.2008.10.010
(2009)Doi:10.1007/s00706-007-0797-9
(2008)Doi:10.1007/BF00810042
(1987)Doi:10.1080/00397910802398256
(2009)
