title: 2-amino-2-oxazolines as subtype selective alpha(2) adrenoceptor agonists.
abstract: 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.
authors.affiliation: Deparment of Chemistry, Synaptic Pharmaceutical Corporation, 215 College Road, Paramus, New Jersey 07652, USA. WAI.WONG.B@BAYER.COM
authors.forename: W C
authors.initials: WC
authors.lastname: Wong
authors.forename: W
authors.initials: W
authors.lastname: Sun
authors.forename: W
authors.initials: W
authors.lastname: Cui
authors.forename: Y
authors.initials: Y
authors.lastname: Chen
authors.forename: C
authors.initials: C
authors.lastname: Forray
authors.forename: P J
authors.initials: PJ
authors.lastname: Vaysse
authors.forename: T A
authors.initials: TA
authors.lastname: Branchek
authors.forename: C
authors.initials: C
authors.lastname: Gluchowski
mesh_terms: D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D003001:Cloning, Molecular; D006801:Humans; D007202:Indicators and Reagents; D008958:Models, Molecular; D009010:Monte Carlo Method; D010080:Oxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D000959:Antihypertensive Agents; D007202:Indicators and Reagents; D010080:Oxazoles; C409962:cyclohexylamino oxazoline; C003822:BAY-a 6781