Hauptmann J, Hoffmann J, Markwardt F
Acta Biol Med Ger. 1976;35(5):635-44.
The effect of the aromatic diamidine derivative 2,6-bis (4-amidinobenzyl)-cyclohexanon-(1) on blood coagulation and fibrinolysis in vitro and in vivo was compared with that of the benzamidine derivative 4-amidinophenyl pyruvic acid and the aromatic diamidine derivative 4,4'-diamidinophenoxypentane. 2,6-Bis(4-amidinobenzyl)-cyclohexanon-(1) was found to be a strong inhibitor of the clotting enzyme thrombin. Because of the toxic side effects and pharmacokinetic properties of both diamidine derivatives their in vivo use as anticoagulants is limited.
将芳香二脒衍生物2,6-双(4-脒基苄基)-环己酮-(1)在体外和体内对血液凝固和纤维蛋白溶解的作用,与苯甲脒衍生物4-脒基苯基丙酮酸以及芳香二脒衍生物4,4'-二脒基苯氧基戊烷的作用进行了比较。发现2,6-双(4-脒基苄基)-环己酮-(1)是凝血酶的强效抑制剂。由于这两种二脒衍生物都有毒副作用和药代动力学特性,它们在体内作为抗凝剂的应用受到限制。