N-Heteroaryl glycinamides and glycinamines as potent NPY5 antagonists

…, A Joshi, MR Marzabadi, V Jubian, K Andersen…

文献索引：Wu, Lingyun; Lu, Kai; Desai, Mahesh; Packiarajan, Mathivanan; Joshi, Amita; Marzabadi, Mohammad R.; Jubian, Vrej; Andersen, Kim; Chandrasena, Gamini; Boyle, Noel J.; Walker, Mary W. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5573 - 5576

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被引用次数: 3

摘要

Subtype specific ligands are needed to evaluate the therapeutic potential of modulating the brain's neuropeptide Y system. The benzothiazepine glycinamide 1a was identified as an NPY5 antagonist lead. While having acceptable solubility, the compound was found to suffer from high clearance and poor exposure. Optimization efforts are described targeting improvements in potency, microsomal stability, and PK properties. The low microsomal ...