Journal of Medicinal Chemistry p. 2235 - 2246 (1988)
Update date:2022-08-03
Topics:
Evans, B. E.
Rittle, K. E.
Bock, M. G.
DiPardo, R. M.
Freidinger, R. M.
et al.
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described.Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effective ligands selective for peripheral (CCK-A) receptors, with binding affinities approaching or equaling that of the natural ligand CCK-8.The distinction between CCK-A receptors on the one hand and CNS (CCK-B), gastrin, and central benzodiazepine receptors on the other is demonstrated by using the structure-activity profiles of the new compounds.Details of the binding of these agents to CCK-A receptors are examined, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
View MoreContact:+86-371-55981030
Address:Room 1571, Macalline Soho, No.1, Shangdu Road, Zhengzhou, Henan
Hangzhou Donglou Bio-nutrient Co., Ltd.
Contact:+86-571-82225795,13967112289
Address:Louta Town, Xiaoshan,Hangzhou,Zhejiang
Hangzhou Kai Peng Biotechnology Co., Ltd.
Contact:86-571-89939007
Address:NO. 499, Wensan West Road, Xihu District, Hangzhou, 310012, China
Contact:13813902930 025-52714267
Address:20 Fengji Road, Yuhua Economic Development Zone, Nanjing, Jiangsu, P. R. China
Yangzhou Siyu Chemical Co.,Ltd.
Contact:+86-514-87325867 13358126196
Address:Room 620 Exposition Pavilion,No. 98 Huaihai Road,Guangling District,Yangzhou City, Jiangsu Province
Doi:10.1021/acs.orglett.5b03431
(2016)Doi:10.1016/j.jorganchem.2008.02.032
(2008)Doi:10.1016/j.bmcl.2008.03.078
(2008)Doi:10.1007/s00706-007-0642-1
(2007)Doi:10.1016/S0040-4020(01)93173-4
(1960)Doi:10.1246/cl.1986.771
(1986)