Platelet aggregation inhibiting and anticoagulant effects of oligoamines, XXII: Bisoxazol-, bisimidazol-, bisthiazol- and oligo-1,2,4-thiadiazolimines.
One mesoionic 4,4'-propylene-bis-oxazol-5-imine (5), two 2,2'-m-phenylene-bis-imidazol-4-imines (9a,b), five 4,4'-benzene-bis-(and tris)-thiazol-2-amines (13a,b, 14a-c) and 14 3,3'-benzene-bis-(and tris)-1,2,4-thiadiazolimines (18a-o) were synthesized and assayed for their antiplatelet and anticoagulant activities. The most potent compound was the tris-thiadiazole derivative 18m which inhibited the aggregation of platelets induced by collagen at a concentration of 10 mumol/L by 50 percent (Born-test). No anticoagulant effects (Quick-test) were observed up to 400 mumol/L. In the thiazolamine series combined antiplatelet and anticoagulant activities were seen.
Rehse
K
K
Institut für Pharmazie, Freien Universität Berlin.
Martens
A
A
D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007097:Imines / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000925:Anticoagulants; D007097:Imines; D010975:Platelet Aggregation Inhibitors; D013830:Thiadiazoles