Novel 5-HT3 antagonists. Isoquinolinones and 3-aryl-2-pyridones

…, T Sugiura, H Nakai, S Iguchi, S Shigeoka…

Index: Matsui; Sugiura; Nakai; Iguchi; Shigeoka; Takada; Odagaki; Nagao; Ushio; Ohmoto; Iwamura; Yamazaki; Arai; Kawamura Journal of Medicinal Chemistry, 1992 , vol. 35, # 18 p. 3307 - 3319

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Citation Number: 65

Abstract

Synthesis and pharmacological evaluation of a series of 1, 2-dihydro-l-[(6-methyl-l-imidazo1- 4-yl) methyl]-2-oxopyridine 6-HTS antagonists are described. The key pharmacophoric elementa were defined as a basic nitrogen, a linking group capable of hydrogen bonding interactions, and an aromatic moiety. 1, 2-Dihydro-2-oxopyridine moiety could be a good linking group because of ita nicely planar structure. The steric limitations of the aromatic ...