Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-substituted 1, 2, 3, 4-tetrahydroisoquinolines

…, FW Chapin, GR Girard, C Kaiser, AJ Krog…

Index: Bondinell; Chapin; Girard; Kaiser; Krog; Pavloff; Schwartz; Silvestri; Vaidya; Lam; Wellman; Pendleton Journal of Medicinal Chemistry, 1980 , vol. 23, # 5 p. 506 - 511

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Citation Number: 35

Abstract

In a search for inhibitors of epinephrine biosynthesis as potential therapeutic agents, a series of 13 ring-chlorinated 1, 2, 3, 4-tetrahydroisoquinolines was prepared. These compounds were tested initially for their ability to inhibit rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) in vitro. Enzyme-inhibitor dissociation constants, determined for the six most potent members of the series, indicated the following order of decreasing ...