Journal of Medicinal Chemistry p. 1934 - 1943 (1985)
Update date:2022-08-05
Topics:
Janssens, Frans
Torremans, Joseph
Janssen, Marcel
Stokbroekx, Raymond A.
Luyckx, Marcel
Janssen, Paul A. J.
The synthesis of a series of 1-<(4-fluorophenyl)methyl>-N-(4-piperidinyl)-1H-benzimidazol-2-amines and the preliminary evaluation of their in vivo antihistamine activity are described.The title compounds were obtained starting from either 1, 4, 10, or 55 by different synthetic methods.Substitution on the phenyl nucleus of the benzimidazole ring (84-87) was achieved by two different approaches.The in vivo antihistamine activity was evaluated by the compound 48/80 induced lethality test in rats and the antihistamine-induced lethality test in guinea pigs after oral and/o r subcutaneous administration.The duration of action was studied in the guinea pig for three compounds (4, 51, and 55).Compound 51, "astemizole", was also studied in histamine- and serotonin-induced cutaneous reaction and for mydriatic activity in the rat and tested for peripheral and central effects not related to histamine antagonism in a variety of systems.Astemizole has been selected for clinical investigation.
View MoreJinan Decheng Hemu Medical Technology Co.,Ltd.
Contact:+86-531-68650525
Address:NO.554 Zhengfeng Road High-new Technology Development Zone
website:http://www.jairadhesales.com
Contact:0091-79-26431096
Address:309 Harikrupa Tower,Nr old Sharda Mandir Char Rasta,Ellisbridge
Shanghai Yuantai Chemical Products Co., Ltd
Contact:021--66129803
Address:Chengyin Road,Shanghai,China
Shenzhen Feiming Science and Technology Co,. Ltd
Contact:+86-755-85232577
Address:#B2309, Fenglin International Center ,Jixiang Road, Longcheng street, LongGang District, Shenzhen city, Guangdong province, China.
Henan Yellow River New Material Technology Co.Ltd.
website:http://www.yellowriverchem.com
Contact:0086-373-7278760
Address:Chengguan Town, Yuanyang County
Doi:10.1002/asia.201403361
(2015)Doi:10.1246/bcsj.53.281
(1980)Doi:10.1039/jr9610002428
(1961)Doi:10.1016/S0008-6215(00)85131-9
(1980)Doi:10.1039/jr9350000873
(1935)Doi:10.1055/s-0031-1290343
(2012)