Journal of Medicinal Chemistry p. 2055 - 2061 (1992)
Update date:2022-08-04
Topics:
Guinn
Summers
Heyman
Conway
Rhein
Albert
Magoc
Carter
A class of N-substituted tetrahydrobenzopyrano[3,4-c]pyridines, I, have been identified as antagonists of platelet activating factor (PAF). The structural features essential for PAF binding were determined by systematic modification of three sites in the molecule. While O-alkyl analogues had little affect on binding potency, N-alkyl analogues exhibited a wide range of activity. Structural changes in the core ring system generally resulted in a loss of binding activity. Optimization of the N- and O-substituents resulted in the analogues 25-27 which exhibited K(i) values ranging between 131 and 167 nM in a [3H]PAF binding assay. Compound 23 was also active in a model of PAF-induced shock in the mouse following intravenous administration.
View MoreContact:+86-021-50792271
Address:Building 24A, 300 Chuantu Road, Chuansha, Pudong new area, Shanghai, China, 201202
Chongqing KonAo Health Co.,Ltd
Contact:13687578375
Address:wuhan hubei china
website:http://www.sagechem.com
Contact:+86-571-86818502
Address:Room C1301, New Youth Plaza, 8 Jia Shan Road, Hangzhou, China
Contact:+86-21-56338808
Address:799 Dunhuang Road, Putuo
Shanghai Gsyn Chemical Co.,Ltd.
Contact:86-021-67158290
Address:86-021-67158291
Doi:10.1021/jo301924e
(2012)Doi:10.1021/ic3017722
(2012)Doi:10.1021/op300263w
(2012)Doi:10.1016/S0040-4039(00)91905-1
(1992)Doi:10.1021/ac00278a059
(1984)Doi:10.1002/hlca.19580410614
(1958)