Journal of Medicinal Chemistry p. 1248 - 1250 (1982)
Update date:2022-07-31
Topics:
Grunewald, Gary L.
Monn, James A.
Rafferty, Michael F,
Borchardt, Ronald T.
Krass, Polina
A series of ω-substituted analogues of amphetamine and α-methylbenzylamine were prepared and evaluated as inhibitors of norepinephrine N-methyltransferase (NMT).These included several alkyl side chain extended analogues (1-5), as well as the terminally hydroxylated derivatives phenylalanol (6a) and Phenylglycinol (7a).None of the alkyl-substituted derivatives displayed appreciable activity as inhibitors; however, the hydroxylated analogues were up to twofold more potent than the parent compounds.The positive contribution of the side-chain hydroxy suggests that theterminal methyl group of the lead compounds is situated close to a hydrophilic area or hydrogen bonding functional group within the active site.
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Doi:10.1021/jm00358a003
(1983)Doi:10.1007/BF00513435
(1982)Doi:10.1134/S107042801706001X
(2017)Doi:10.1016/0040-4039(81)89010-7
(1981)Doi:10.1055/s-1982-30011
(1982)Doi:10.1016/S0022-328X(00)86917-X
(1982)