Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071

Herein we report the discovery and SAR of a novel series of M-1 agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M-1 agonist with high selectivity, clean ancillary pharmacology and enantiospecific activity. (C) 2011 Elsevier Ltd. All rights reserved.