Synthesis of 4, 5, 6, 7-tetrahydrothieno [3, 2-c] pyridines and comparison with their isosteric 1, 2, 3, 4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N- …

GL Grunewald, MR Seim, SR Bhat, ME Wilson…

Index: Grunewald, Gary L.; Seim, Mitchell R.; Bhat, Seema R.; Wilson, Marc E.; Criscione, Kevin R. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 1 p. 542 - 559

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Citation Number: 15

Abstract

A series of substituted 4, 5, 6, 7-tetrahydrothieno [3, 2-c] pyridines (THTPs) was synthesized and evaluated for their human phenylethanolamine N-methyltransferase (hPNMT) inhibitory potency and affinity for the α2-adrenoceptor. The THTP nucleus was suggested as an isosteric replacement for the 1, 2, 3, 4-tetrahydroisoquinoline (THIQ) ring system on the basis that 3-thienylmethylamine (18) was more potent as an inhibitor of hPNMT and more ...