189244-06-2Relevant academic research and scientific papers
Bioisosteric replacement strategy for the synthesis of 1-azacyclic compounds with high affinity for the central nicotinic cholinergic receptors
Olesen, Preben H.,Tonder, Janne E.,Hansen, John Bondo,Hansen, Holger C.,Rimvall, Karin
, p. 1443 - 1450 (2000)
Bioisosteric replacement of the isoxazole heterocycle in (3-methyl-5-isoxazolyl)methylene-azacyclic compounds with pyridine, oxadiazole, or an acyl group resulted in ligands with high to moderate affinity for the central nicotinic cholinergic receptors (IC50=2.0 to IC50>1000nM) labeled by [3H]methylcarbamylcholine. Additionally, further support of an important distance parameter for high-affinity nicotinic compounds has been provided. Copyright (C) 2000 Elsevier Science Ltd.
