Objective To study the effect of electronic isosteric substitution with acidic tetrazolium groups on the coagulation promoting activity of dencichine.Methods Three analogues of dencichine were synthesized by reacting N2-Fmoc-L-2,3-diaminoalanine with 2H-1,2,3-triazole-2-acetic acid,1H-1,2,4-triazol-1-acetic acid,1H-tetrazol-5-acetic acid,respectively.The structures of the resulting compounds were confirmed by 1H NMR,13C NMR and MS.Results Three analogues,including 3-(2-(2H-1,2,3-triazol-2-yl)acetamido)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)propanoic acid(Ⅰ),3-(2-(1H-1,2,4-triazol-1-yl)acetamido)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)propanoic acid(Ⅱ)and 3-(2-(2H-tetrazol-5-yl)acetamido)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)propanoic acid(Ⅲ)were obtained.Four items of blood coagulation tests(APTT,PT,TT and FIB)and plasma recalcification time test indicated that derivative Ⅲ had better procoagulant properties than Ⅰ and Ⅱ.Conclusion Electron isosteric substitution with acidic tetrazolium groups on dencichine molecule has a certain enhancing effect on its procoagulant activity.
dencichineanaloguefour items of blood coagulation testsplasma recalcification timeprocoagulant activity
维普
万方数据
