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Synthesis and Evaluation of Novel Nitric Oxide-Donating Ligustrazine Derivatives as Potent Antiplatelet Aggregation Agents.
Li, Han-Xu; Tian, Jian-Hui; Li, Hua-Yu; Wan, Xin; Zou, Yu.
Afiliación
  • Li HX; Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
  • Tian JH; Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
  • Li HY; Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
  • Wan X; Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
  • Zou Y; Institute of Pharmaceutical Process, Hubei Province Key Laboratory of Occupationl Hazard Identification and Control, School of Medicine, Wuhan University of Science and Technology, Wuhan 430065, China.
Molecules ; 28(8)2023 Apr 11.
Article en En | MEDLINE | ID: mdl-37110589
Antiplatelet aggregation agents have demonstrated clinical benefits in the treatment of ischemic stroke. In our study, a series of novel nitric oxide (NO)-donating ligustrazine derivatives were designed and synthesized as antiplatelet aggregation agents. They were evaluated for the inhibitory effect on 5'-diphosphate (ADP)-induced and arachidonic acid (AA)-induced platelet aggregation in vitro. The results showed that compound 15d displayed the best activity in both ADP-induced and AA-induced assays, and compound 14a also showed quite better activity than ligustrazine. The preliminary structure-activity relationships of these novel NO-donating ligustrazine derivatives were discussed. Moreover, these compounds were docked with the thromboxane A2 receptor to study the structure-activity relationships. These results suggested that the novel NO-donating ligustrazine derivatives 14a and 15d deserve further study as potent antiplatelet aggregation agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Agregación Plaquetaria / Óxido Nítrico Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Suiza
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Agregación Plaquetaria / Óxido Nítrico Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Suiza