Abstract:
Based on the current structure-activity relationship of apixaban, keeping P
1 portions unchanged and replace
δ-valerolactam in P
4 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.