Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A

Z Zhang, X Lu, J Xu, J Rothfuss, RH Mach…

Index: Zhang, Zhanbin; Lu, Xiaoxia; Xu, Jinbin; Rothfuss, Justin; MacH, Robert H.; Tu, Zhude European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 3986 - 3995

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Citation Number: 5

Abstract

A series of analogues were synthesized by optimizing the structure of papaverine. The in vitro PDE10A binding affinity (IC50) values for these new analogues were measured; for compounds that have IC50 value less than 60 nM for PDE10A, the binding affinities (IC50 value) for PDE3A and PDE3B were tested. Of these analogues, compounds 6a, 6b, 6n, 8b, 8c and 11 displayed relatively higher PDE10A potency with IC50 value in the range of 28– ...