5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists
…, R Hoffmann, B Didier, V Rybaltchenko…
Index: Rival, Yveline; Hoffmann, Remy; Didier, Bruno; Rybaltchenko, Volodymyr; Bourguignon, Jean-Jacques; Wermuth, Camille G. Journal of Medicinal Chemistry, 1998 , vol. 41, # 3 p. 311 - 317
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Citation Number: 54
Abstract
A conformational analysis, performed on muscarinic M1 agonists, identified four structural features characteristic of the muscarinic M1 pharmacophore:(i) a protonable basic or quaternary nitrogen acting as a cationic head;(ii) an electronegative dipole usually part of a planar mesomeric ester, amide, or amidine function which can be replaced by an ether (muscarine) or a dioxolane (AF 30);(iii) an intercharge distance of 5±0.5 Å between the ...
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