Synthesis and evaluation of L-quebrachitol derivatives against platelet aggregation

Abstract

Thrombosis plays an important role in the occurrence and development of cardiovascular and cerebrovascular diseases that contribute to high mortality and morbidity in patients. L-(-)-Quebrachitol (QCT), a natural product, was first isolated from quebracho bark. It can inhibit PAF receptor and decrease gastric damage induced by indomethacin, as a drug against platelet aggregation. Here, five QCT derivatives were synthesized and investigated for their inhibitory effects on platelet aggregation. Among them, compound 3a showed anticoagulant effects comparable to aspirin, while compound 4b showed dose-independent inhibitory activities in rats that were stronger than aspirin.

Keywords:

• Thrombosis
• L-(-)-Quebrachitol
• gastric damage
• platelet aggregation
• aspirin

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

Project supported by the National Natural Science Foundation of China (No. 82273793), Key Research Project of Department of Education of Liaoning Province (LJKZZ20220108), the China Postdoctoral Science Foundation (No. 2019M661132), the foundation of Liaoning Provincial Department of Education (No. LJKQZ20222351).