Journal of Medicinal Chemistry p. 1432 - 1437 (1981)
Update date:2022-08-03
Topics:
DeMarinis, R. M.
Bryan, W. M.
Shah, D. H.
Hieble, J. P.
Pendleton, R. G.
A series of phenylethylamines related to methoxamine has been prepared and evaluated for direct α1-receptor agonist activity.It has been observed that for open-chain compounds such as methoxamine, in which the amine-containing portion is free to adopt numerous conformations, an hydroxyl group is necessary for direct α1-adrenergic activity.When the hydroxyl is removed, however, the direct component of activity is greatly reduced unless the amine is incorporated into a more sterically defined structure.From our studies we have concluded that in order for a phenylethylamine to be active as a direct α1-receptor agonist it should have a β nitrogen in a fully extended conformation relative to a substituted phenyl ring.For optimum potency, the nitrogen should be exocyclic to a saturated six-membered ring.It may be further incorporated exocyclic or endocyclic into an additional ring so long as the amine occupies a well-defined region of space relative to the aromatic portion of a molecule.The ED50 values of some of the more potent compounds as α1-receptor agonists are on the order of 1 * 10-7 M.
View MoreMS( MAOSHENG )Chemical CO.,LTD
Contact:+86-519-82726678.82726378
Address:TAOXI INDUSTRY ZONE JINTAN
Contact:+31-24-3886056
Address:Binderskampweg 29 Unit 36
SHAANXI TOP PHARM CHEMICAL CO.LTD
Contact:+86-029-85733403
Address:No.108 ,west sector,south er huan,xi'an,china
AllyChem Co., Ltd., Dalian, China(BBChem)
Contact:+86-411-62313318/62313328
Address:No.5 of Jinbin Road, Jinzhou New District, Dalian City, Liaoning Province, P.R.China
Contact:(86) 731 88718666
Address:Room 1222, Unit 4, Building B, Shangcheng, No.47, Kaiyuan East Road.
Doi:10.1021/ja00410a052
(1981)Doi:10.1021/jm0311036
(2004)Doi:10.1021/jm00144a014
(1981)Doi:10.1021/jo00339a048
(1981)Doi:10.1016/j.tet.2004.08.024
(2004)Doi:10.1016/S0957-4166(01)00030-1
(2001)