Muscarinic M 3 receptor antagonists with (2R)-2-[(1R)-3, 3-Difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2

…, T Kimura, T Fujikawa, T Hasegawa, K Noguchi…

文献索引：Ogino, Yoshio; Ohtake, Norikazu; Kobayashi, Kensuke; Kimura, Toshifumi; Fujikawa, Toru; Hasegawa, Takuro; Noguchi, Kazuhito; Mase, Toshiaki Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 13 p. 2167 - 2172

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被引用次数: 12

摘要

Optimization of the amine part of our original muscarinic M3 receptor antagonist 1 was performed to identify M3 receptor antagonists that are superior to 1. Compounds carrying a variety of diamine moieties without hydrophobic substituent on the nitrogen atom were screened against the binding affinity for the M3 receptor and the selectivity for M3 over the M1 and M2 receptors. This process led to a 4-aminopiperidinamide (2l) with a Ki value of ...