adrenergic (Adrenoceptor)
J Med Chem 2000 May 4;43(9):1699-1704
2-Amino-2-oxazolines as Subtype Selective alpha(2) Adrenoceptor Agonists.
Wong WC, Sun W, Cui W, Chen Y, Forray C, Vaysse PJ, Branchek TA, Gluchowski C
Deparments of Chemistry, Pharmacology, and Cell Biology, Synaptic Pharmaceutical Corporation, 215 College Road, Paramus, New Jersey 07652.
Cyclohexylamino oxazoline 1 (AGN 190837), an analogue of 2 (Bay a6781), is a potent alpha(2) adrenoceptor agonist. On the basis of a design generated by receptor-ligand modeling, a number of cyclohexyl and norbornyl analogues were synthesized wherein the propyl group of 1 was replaced by phenylalkyl subsituents. This resulted in compound 6 being an alpha(2c) selective agonist, as well as 7 and 9 being alpha(2a)/alpha(2c) selective.
PMID: 10794687
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