阿哌沙班衍生物的合成及Ⅹa因子抑制活性

基金项目: 国家“重大新药创制”科技重大专项资助项目(No.2013ZX09301303-002)；江苏省产学研联合创新资金-前瞻性联合研究项目资助(No.BY2011158)；中央高校基本科研业务费专项基金资助项目(No.JKY2011092)

Synthesis and factor Xa inhibitory activity of apixaban derivatives

摘要: 在阿哌沙班的结构基础上，保持其P₁部分不变，对其P₄部分进行结构改造，用一系列芳香酰胺基团代替2-氮己酮，合成了一系列未见报道的吡唑并吡啶酮类化合物。所合成化合物结构均经IR，¹H NMR和MS确证，并对这些化合物的Ⅹa因子抑制活性进行了测定，结果表明所有化合物均表现出一定的Ⅹa因子抑制活性，但活性均低于阳性药阿哌沙班。
- 阿哌沙班 /
- 衍生物 /
- 合成 /
- Ⅹa因子抑制剂
Abstract: Based on the current structure-activity relationship of apixaban, keeping P₁ portions unchanged and replace δ-valerolactam in P₄ portions with aromatic amide group, a series of dihydropyrazolopyridinones not reported were designed and synthesized. The structures of all the synthesized derivatives were identified by IR, ¹H NMR and MS. And then their anti-factor Xa activity was tested. The results showed that all the tested compounds exhibited factor Xa inhibitory activity, but with less potency than that of apixaban.
- apixaban /
- derivatives /
- synthesis /
- factor Xa inhibitors