6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2, 6-Dimethoxyphenoxy) ethyl] aminomethyl-1, 4-benzodioxane (WB4101): 1 discovery of …

L Fumagalli, M Pallavicini, R Budriesi…

Index: Fumagalli, Laura; Pallavicini, Marco; Budriesi, Roberta; Bolchi, Cristiano; Canovi, Mara; Chiarini, Alberto; Chiodini, Giuseppe; Gobbi, Marco; Laurino, Paola; Micucci, Matteo; Straniero, Valentina; Valoti, Ermanno Journal of Medicinal Chemistry, 2013 , vol. 56, # 16 p. 6402 - 6412

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Citation Number: 13

Abstract

Previous results have shown that replacement of one of the two o-methoxy groups at the phenoxy residue of the potent, but not subtype-selective, α1-AR antagonist (S)-WB4101 [(S)- 1] by phenyl, or by ortho, meta-fused cyclohexane, or especially by ortho, meta-fused benzene preferentially elicits α1D-AR antagonist affinity. Such observations inspired the design of four new analogues of 1 bearing, in lieu of the 2, 6-dimethoxyphenoxy residue, a ...