Synthesis and biological evaluation of nitric oxide (NO)-hydrogen sulfide (HS) releasing derivatives of (S)-3-n-butylphthalide as potential antiplatelet agents / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 946-953, 2016.
Article
in English
| WPRIM
| ID: wpr-812536
ABSTRACT
In the present study, a series of novel nitric oxide-hydrogen sulfide releasing derivatives of (S)-3-n-butylphthalide ((S)-NBP) were designed, synthesized, and evaluated as potential antiplatelet agents. Compound NOSH-NBP-5 displayed the strongest activity in inhibiting the arachidonic acid (AA)- and adenosine diphosphate (ADP)-induced platelet aggregation in vitro, with 3.8- and 7.0-fold more effectiveness than (S)-NBP, respectively. Furthermore, NOSH-NBP-5 could release moderate levels of NO and HS, which would be beneficial in improving cardiovascular and cerebral circulation. Moreover, NOSH-NBP-5 could release (S)-NBP when incubated with rat brain homogenate. In conclusion, these findings may provide new insights into the development of novel antiplatelet agents for the treatment of thrombosis-related ischemic stroke.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Thrombosis
/
Benzofurans
/
Platelet Aggregation Inhibitors
/
Molecular Structure
/
Chemistry
/
Platelet Aggregation
/
Rats, Sprague-Dawley
/
Drug Therapy
/
Hydrogen Sulfide
Limits:
Animals
/
Humans
/
Male
Language:
English
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2016
Type:
Article
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