A new pyridazine series of GABAA α5 ligands

…, S Malpas, K Maubach, R Newman…

文献索引：Van Niel, Monique B.; Wilson, Kevin; Adkins, Charles H.; Atack, John R.; Castro, Jose L.; Clarke, Dawn E.; Fletcher, Stephen; Gerhard, Ute; Mackey, Mark M.; Malpas, Sallie; Maubach, Karen; Newman, Robert; O'Connor, Desmond; Pillai, Gopalan V.; Simpson, Peter B.; Thomas, Steven R.; MacLeod, Angus M. Journal of Medicinal Chemistry, 2005 , vol. 48, # 19 p. 6004 - 6011

全文：HTML全文

被引用次数: 18

摘要

Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor ...