Exploring the active site of phenylethanolamine N-methyltransferase: 3-alkyl-7-substituted-1, 2, 3, 4-tetrahydroisoquinoline inhibitors

…, AD Chieu, KJ Fincham, SR Bhat, KR Criscione

Index: Grunewald, Gary L.; Romero, F. Anthony; Chieu, Alex D.; Fincham, Kelcie J.; Bhat, Seema R.; Criscione, Kevin R. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 4 p. 1261 - 1273

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Citation Number: 8

Abstract

A series of 3-alkyl-7-substituted-1, 2, 3, 4-tetrahydroisoquinolines was synthesized and these compounds were evaluated for their PNMT inhibitory potency and affinity for the α2- adrenoceptor. 7-Nitro-, 7-bromo-, 7-aminosulfonyl-, or 7-N-2, 2, 2-trifluoroethylaminosulfonyl- THIQs that possess a 3-alkyl substituent that is longer than a methyl group showed decreased PNMT inhibitory potency, except for 3-propyl-7-aminosulfonyl-THIQ, which ...