Research on Synthesis and Procoagulant Activity of Dencichine Analogues
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
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