Synthesis and pharmacology of benzoxazines as highly selective antagonists at M4 muscarinic receptors

…, CE Augelli-Szafran, H Hallak, T Pugsley…

Index: Boehme, Thomas M.; Augelli-Szafran, Corinne E.; Hallak, Hussein; Pugsley, Thomas; Serpa, Kevin; Schwarz, Roy D. Journal of Medicinal Chemistry, 2002 , vol. 45, # 14 p. 3094 - 3102

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Citation Number: 136

Abstract

Previously, we reported on PD 102807 (41) as being the most selective synthetic M4 muscarinic antagonist identified to date. Synthesized analogues of 41 showed no improvement in affinity and selectivity at that time. However, several newly synthesized compounds exhibit a 7-fold higher affinity at M4 receptors and demonstrate a selectivity of at least 100-fold over all other muscarinic receptor subtypes. For example, compound 28 ...