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Citation: Yi Li, Bilan Luo, Juqin Zhao, Yong Li, Yi Zhang, Lei Tang, Lingling Fan. Design, Synthesis and Anti-Platelet Aggregation Activity of Piperido[2, 3-b]piperazine Derivatives[J]. Chemistry, ;2021, 84(2): 162-166. shu

Design, Synthesis and Anti-Platelet Aggregation Activity of Piperido[2, 3-b]piperazine Derivatives

Yi Li ¹ ,
Bilan Luo ¹ ,
Juqin Zhao ¹ ,
Yong Li ¹ ,
Yi Zhang ¹ ,
Lei Tang ^{1, 2} ,
Lingling Fan ^1,,

1.
School of Pharmacy, Guizhou Medical University, Guiyang, 550004
2.
Guizhou Chemical Drug Research and Development Engineering Technical Center, Guizhou Medical University, Guiyang, 550004

Corresponding author: Lingling Fan, fanling1025@126.com
Received Date: 6 August 2020
Accepted Date: 17 August 2020

Figures(2)

Using 2, 3-diaminopyridine and 2, 3-butanedione as the starting material, ten new piperido [2, 3-b]piperazine derivatives (3a~3j) were synthesized by cyclization, catalytic hydrogenation and nucleophilic substitution reaction. Their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The in vitro antiplatelet aggregation activity study showed that compounds 3d, 3e, 3g, 3h and 3j had a certain antiplatelet aggregation effect, and the activity of compound 3h (IC₅₀=1.24 mmol/L) was significantly better than that of the lead compound ligustrazine (IC₅₀=3.96 mmol/L) and the positive drug aspirin (IC₅₀=2.41 mmol/L).
- Piperido[2, 3-b]piperazine,
- Synthesis,
- Anti-platelet aggregation activity
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