Design, synthesis and evaluation of hydrogen sulfide-releasing derivatives of ring opening 3-<i>n</i>-butylphthalide as novel platelet aggregation inhibitors

WANG Xiaoli; WANG Zhaoya; WANG Linna; JI Hui; ZHANG Yihua; YIN Jian

doi:10.11665/j.issn.1000-5048.20160205

Journal of China Pharmaceutical University > 2016 > 47(2): 158-162. > DOI: 10.11665/j.issn.1000-5048.20160205

WANG Xiaoli, WANG Zhaoya, WANG Linna, JI Hui, ZHANG Yihua, YIN Jian. Design, synthesis and evaluation of hydrogen sulfide-releasing derivatives of ring opening 3-n-butylphthalide as novel platelet aggregation inhibitors[J]. Journal of China Pharmaceutical University, 2016, 47(2): 158-162. DOI: 10.11665/j.issn.1000-5048.20160205

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Design, synthesis and evaluation of hydrogen sulfide-releasing derivatives of ring opening 3-n-butylphthalide as novel platelet aggregation inhibitors

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Abstract

A series of hydrogen sulfide-releasing derivatives of open ring 3-n-butylphthalide( 5a - 5f )were designed, synthesized, and their structures were confirmed by MS and ¹H NMR. The inhibitory activity of the target compounds against adenosine diphosphate(ADP)and arachidonic acid(AA)-induced platelet aggregation was evaluated in vitro by Born′s turbidimetric assay. In comparison with 3-n-butylphthalide(NBP), compound 5e possessed better antiplatelet aggregation activity. Therefore, it may be utilized as a lead compound for further investigation.
- 3-n-butylphthalide,
- hydrogen sulfide,
- hydrogen sulfide donors,
- synthesis,
- antiplatelet aggregation activity

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Design, synthesis and evaluation of hydrogen sulfide-releasing derivatives of ring opening 3-n-butylphthalide as novel platelet aggregation inhibitors

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