title: Synthesis and evaluation of nitric oxide-releasing derivatives of 3-n-butylphthalide as anti-platelet agents.
abstract: Most ischemic stroke results from brain blood vessel blockage by platelet-mediated thrombus, and anti-platelet therapy has been demonstrated clinical benefits in the treatment of this disease. In the present work, novel nitric oxide (NO)-releasing derivatives of an anti-ischemic stroke drug 3-n-butylphthalide (NBP) were synthesized. Compounds 7a and 7c exhibited more potent anti-platelet activity than NBP and aspirin, and released a moderate amount of NO, which is beneficial in improving cardiovascular and cerebral circulation. These findings provide an alternative approach to the development of drugs more potent than NBP for the intervention of ischemic stroke.
authors.affiliation: Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.forename: Xuliang
authors.initials: X
authors.lastname: Wang
authors.forename: Rong
authors.initials: R
authors.lastname: Fu
authors.forename: Wenying
authors.initials: W
authors.lastname: Yu
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Wang
authors.forename: Yisheng
authors.initials: Y
authors.lastname: Lai
authors.forename: Sixun
authors.initials: S
authors.lastname: Peng
authors.forename: Yihua
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000244:Adenosine Diphosphate / Q000494:pharmacology; D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects*; D002109:Caffeic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009566:Nitrates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009569:Nitric Oxide / Q000378:metabolism*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits
chemical_list: D001565:Benzoates; D001572:Benzofurans; D002109:Caffeic Acids; D009566:Nitrates; D010975:Platelet Aggregation Inhibitors; D009569:Nitric Oxide; D000244:Adenosine Diphosphate; C027125:3-n-butylphthalide