50710-44-6Relevant articles and documents
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1
Bender, Aaron M.,Blobaum, Anna L.,Boutaud, Olivier,Cho, Hyekyung P.,Engers, Darren W.,Jeffrey Conn, P.,Lindsley, Craig W.,Luscombe, Vincent B.,Niswender, Colleen M.,Rodriguez, Alice L.,Spearing, Paul K.
, (2021)
This Letter describes the synthesis and optimization of a series of heteroaryl-pyrrolidinone positive allosteric modulators (PAMs) of the muscarinic acetylcholine receptor M1 (mAChR M1). Through the continued optimization of M1 PAM tool compound VU0453595, with a focus on replacement of the 6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one with a wide variety of alternative 4,5-dihydropyrrolo-fused heteroaromatics, the generation of M1 PAMs with structurally novel chemotypes is disclosed. Two compounds from these subseries, 8b (VU6005610) and 20a (VU6005852), show robust selectivity for the M1 mAChR, and no M1 agonism. Both compounds have favorable preliminary PK profiles in vitro; 8b additionally demonstrates high brain exposure in a rodent IV cassette model.
α,25-Dihydroxyvitamin D3 analogs featuring aromatic and heteroaromatic rings: Design, synthesis, and preliminary biological testing
Posner,Li,White,Vinader,Takeuchi,Guggino,Dolan,Kensler
, p. 4529 - 4537 (2007/10/03)
Aromatic compounds 2a-c, analogs of 1α,25-dihydroxyvitamin (calcitriol, 1), and heteroaromatic compounds 4a-c and 5a-c, analogs of 19-nor-1α,25- dihydroxyvitamin D3 (3), were designed to simulate the topology of their biologically potent parent
