title: Synthesis, structure and antiaggregatory effects of some N-(4,5-dihydro-1H-imidazol-2-yl)indoles.
abstract: A series of 1-(4,5-dihydro-1H-imidazol-2-yl)indole derivatives was prepared in order to evaluate their antiaggregatory activity in human platelets. The compounds 4a-m were prepared by reacting N-aryl-N-(4,5-dihydro-1H-imidazol-2-yl)hydroxylamines (2a-d) with monosubstituted acetylene derivatives 3a-b. Imidazoline derivatives 4 were further acetylated or sulfonylated to give amides 5a-c and sulfonamides 6a-c and 7a-c, respectively. Eight compounds were taken as representative aryliminoimidazoline analogs. Among them only one, 4m, showed a good concentration-dependent action against the primary or alpha 2-adrenoreceptor mediated phase of noradrenaline-induced aggregation in platelets.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Poland. saczew@farmacja.amg.gda.pl
authors.forename: F
authors.initials: F
authors.lastname: Saczewski
authors.forename: T
authors.initials: T
authors.lastname: Debowski
authors.forename: J
authors.initials: J
authors.lastname: Petrusewicz
authors.forename: M
authors.initials: M
authors.lastname: Gdaniec
authors.forename: R K
authors.initials: RK
authors.lastname: Dabrowski
authors.forename: E
authors.initials: E
authors.lastname: Nowakowska
mesh_terms: D018360:Crystallography, X-Ray; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007211:Indoles; D010975:Platelet Aggregation Inhibitors