Substituted pentacyclic carbazolones as novel muscarinic allosteric agents: synthesis and structure-affinity and cooperativity relationships

P Gharagozloo, S Lazareno, M Miyauchi…

文献索引：Gharagozloo, Parviz; Lazareno, Sebastian; Miyauchi, Masao; Popham, Angela; Birdsall, Nigel J. M. Journal of Medicinal Chemistry, 2002 , vol. 45, # 6 p. 1259 - 1274

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被引用次数: 19

摘要

Two series of pentacyclic carbazolones, 22 and 23, have been synthesized utilizing a facile intramolecular Diels-Alder reaction and are allosteric modulators at muscarinic acetylcholine receptors. Their affinities and cooperativities with acetylcholine and the antagonist N- methylscopolamine (NMS) at M1-M4 receptors have been analyzed and compared. All of the synthesized compounds are negatively cooperative with acetylcholine. In contrast, the ...