Platelet aggregation inhibiting and anticoagulant effects of oligoamines, XXI: 4,4'-Alkylene-bis-sydnone imines.
Two methylene-, seven ethylene-, eleven propylene- and two 4,4'-butylene-bis-sydnone imines have been synthesized and tested for their antiplatelet (Born-test, collagen) and anticoagulant (Quick-test) activity in vitro. The most active compounds were found in the ethylene and propylene series. The most favourable substituents in 3-position of the sydnone were hexyl to octyl or phenylethyl to phenylbutyl groups. Six compounds exhibit an IC50 < or = 10 mumol/L against platelet aggregation. Three compounds showed an IC75 < or = 200 mumol/L concerning the fibrin formation (Quick delta t > or = 7 s).
Rehse
K
K
Institut für Pharmazie, Freien Universität Berlin.
Martens
A
A
D000925:Anticoagulants / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013558:Sydnones / Q000138:chemical synthesis* / Q000494:pharmacology
D000925:Anticoagulants; D010975:Platelet Aggregation Inhibitors; D013558:Sydnones