Effect of Ring Size or an Additional Heteroatom on the Potency and Selectivity of Bicyclic Benzylamine-Type Inhibitors of Phenylethanolamine N-Methyltransferase1a

GL Grunewald, VH Dahanukar, P Ching…

文献索引：Grunewald, Gary L.; Dahanukar, Vilas H.; Ching, Piao; Criscione, Kevin R. Journal of Medicinal Chemistry, 1996 , vol. 39, # 18 p. 3539 - 3546

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被引用次数: 73

摘要

In the search for potent and selective inhibitors of the enzyme phenylethanolamine N- methyltransferase (PNMT; EC 2.1. 1.28), we examined the effect of ring size or an additional heteroatom in the conformationally-restricted benzylamine-type PNMT inhibitors. Based on semiempirical calculations (MNDO) and molecular modeling studies, PNMT-inhibitory activity of these compounds seemed to be dependent on (a) the torsion angle between the ...