Journal of Medicinal Chemistry p. 831 - 836 (1984)
Update date:2022-07-30
Topics:
Fuhrer
Ostermayer
Zimmermann
Meier
Mueller
The synthesis of a group of potential β-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for β-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the β-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)(n)CHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of β-blocking potency were found for n = 0 and 2. Moreover, the carbon isostere of the corresponding (aryloxy)propanolamine still proved to be a very potent β-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.
View MoreShanghai Harvest Chemical Ind. Co., Ltd.
Contact:021-51385350
Address:ROOM 806-807, AI LI CHEN BUILDING, No.333 JINGXIANG ROAD, PUDONG DISTRICT, 201206, SHANGHAI
Contact:+86 021-51698675
Address:1701, Jielong Plaza, No.618 Pingliang Rd, ShangHai,China
WUXI KINGHAN BIO-MEDICAL&CHEMICAL INC.
Contact:13861062998
Address:Room 1316,No.1619 Huishan Avenue,Wuxi,China
Shandong Yuanli Science and Technology Co., Ltd.
Contact:86-0536-6777557
Address:Zhuliu Industiral Park,Changle County
Zhejiang Chemicals Import & Export Corporation
Contact:86-571-87043088
Address:No.37,Qingchun Road,Hangzhou,China
Doi:10.1021/acsmedchemlett.9b00394
(2019)Doi:10.1016/j.tetlet.2004.09.003
(2004)Doi:10.1039/c39860001417
(1986)Doi:10.1021/ja00412a024
(1981)Doi:10.1016/S0022-328X(00)92605-6
(1981)Doi:10.1016/j.bmcl.2006.04.091
(2006)