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 MoreKaymossy BioChem Tech Co., Ltd
website:http://www.kaimosi.com
Contact:0571-87191913/0571-87199097
Address:Room 215, Building 3rd, No.288 Ningxia Road, Qingdao city, China
GUANGZHOU MEDCAN PHARMATECH LTD
website:http://www.gzmedcan.com
Contact:+86-20-82519649
Address:Building J,Room 101,1 JiangtashanRd,Guang Zhou Science City,Guang Zhou ,China
LIANYUNGANG YC FINE CHEMICAL CO., LTD
Contact:+86-518-858 99188
Address:Shangdong Modern Bldg, South Greenpark Road, Lianyungang, Jiangsu Pro. China
Jiangsu Cale New Material Co.ltd
Contact:+86-515-88334667/88203550
Address:Zhongshan 3rd Road, Coastal Chemical Industry Park, Yancheng, Jiangsu, China
Zhejiang Haizhou Pharmaceutical Co., Ltd.
website:https://www.haizhoupharma.com/
Contact:+86-576-88221016
Address:No. 19, Donghai 5th Avenue, Yanhai Industrial Zone, Linhai, Zhejiang, China
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)