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Bioisosteric replacement strategy for the synthesis of 1-azacyclic compounds with high affinity for the central nicotinic cholinergic receptors

Preben H. Olesen - No affiliation found

2000/06/01 Full-length article DOI: 10.1016/S0968-0896(00)00063-8 Journal: Bioorganic & Medicinal Chemistry

Abstract:

AbstractBioisosteric 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>1000 nM) labeled by [3H]methylcarbamylcholine. Additionally, further support of an important distance parameter for high-affinity nicotinic compounds has been provided.