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…

Index: 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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Citation Number: 12

Abstract

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 ...