Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and. alpha.- …

…, MF Rafferty, RT Borchardt, P Krass

Index: Grunewald, Gary L.; Monn, James A.; Rafferty, Michael F,; Borchardt, Ronald T.; Krass, Polina Journal of Medicinal Chemistry, 1982 , vol. 25, # 10 p. 1248 - 1250

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Citation Number: 8

Abstract

A series of w-substituted analogues of amphetamine and a-methylbemylamine were prepared and evaluated as inhibitors of norepinephrine N-methyltransferase (NMT). These included several alkyl side chain extended analogues (14, as well as the terminally hydroxylated derivatives phenylalanol (6a) and phenylglycinol (7a). None of the alkylsubstituted derivatives displayed appreciable activity as inhibitors; however, the ...