Chemical and Pharmaceutical Bulletin p. 1510 - 1520 (1996)
Update date:2022-08-02
Topics:
Sakurai, Shunichiro
Ogawa, Nobuo
Suzuki, Tomio
Kato, Ken-Ichi
Ohashi, Tetsuo
Yasuda, Shingo
Kato, Hideo
As part of our search for a dual inhibitor possessing both thromboxane A2 (TXA2) receptor antagonistic and TXA2 synthase inhibitory activities, some [[(benzenesulfonamido)alkyl]phenyl]alkanoic acid derivatives possessing a pyridyl or imidazolyl group were synthesized. Their TXA2 receptor antagonistic and TXA2 synthase inhibitory activities were evaluated in terms of the inhibitory effects on U-46619-induced guinea-pig platelet aggregation and on thromboxane B2 (TXB2) production in human platelets, respectively. It was found that 3-[4-[2-(1-imidazolyl)1-(4- chlorobenzenesulfonamido)ethyl]phenyl]propionic acid (22a), containing an imidazolyl group, is a well-balanced dual inhibitor having both TXA2 receptor antagonistic activity (IC50=0.31 μM) and TXA2 synthase inhibitory activity (IC50=0.39 μM).
View MoreShanghai shibo Chemical Co., Ltd
Contact:+86-021-60753516
Address:688 Qiushi Road, Jinshan High-tech Park, Shanghai, China,201512
Contact:+86-(0)21-3770 9035
Address:Room 301, Building 2, Meijiabang Road 1508, Shanghai China
Nantong Kaixin Pharma Chemical Co.,Ltd.
Contact:86-513-85250786
Address:2-1103 Huachen Mansion, 111 Gongnong Road,Nantong, Jiangsu, China
Shanghai Taibao Pharmaceutical Technology Co., Ltd(expird)
Contact:021-52217366
Address:shanghai
Jining Shengrun Chemical Industry Co., Ltd.
Contact:+86-537-7121666 ,
Address:West Ring Road,Wenshang County Shandong Province
Doi:10.1016/j.tetlet.2007.08.108
(2007)Doi:10.1016/0040-4039(96)01504-3
(1996)Doi:10.1016/j.tetlet.2014.10.043
(2014)Doi:10.1016/S0040-4039(00)74478-9
(1991)Doi:10.1016/0040-4020(96)00652-7
(1996)Doi:10.1016/0040-4020(96)00613-8
(1996)
