Abstract:
:Endothelial dysfunction and consequent reduction of biosynthesis of endogenous nitric oxide (NO) play an important pathogenetic role in the cardiovascular complications associated with type II diabetes. In this work, the hybrid drugs 3a and 3b, nitrooxymethylbenzoate-derivatives of 1 (which is a hydroxylated active metabolite of glibenclamide 2), are reported. The pharmacodynamic characterization of 3b showed that its hypoglycaemic activity is enriched with additional NO-donor effects, conferring vasorelaxing and anti-platelet properties of potentially great usefulness for diabetes-related cardiovascular disorders.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Calderone V,Rapposelli S,Martelli A,Digiacomo M,Testai L,Torri S,Marchetti P,Breschi MC,Balsamo Adoi
10.1016/j.bmc.2009.06.049subject
Has Abstractpub_date
2009-08-01 00:00:00pages
5426-32issue
15eissn
0968-0896issn
1464-3391pii
S0968-0896(09)00617-8journal_volume
17pub_type
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