nuova ( anche nitro-..) aspririna
c'é sempre qualcuno che ci sta lavorando ( anche non solo nitro-.. )
New Nitric Oxide or Hydrogen Sulfide Releasing Asp... [J Med Chem. 2011] - PubMed result
J Med Chem. 2011 Jun 21. [Epub ahead of print]
New Nitric Oxide or Hydrogen Sulfide Releasing Aspirins.
Lazzarato L, Chegaev K,
Marini E, Rolando B, Borretto E, Guglielmo S, Joseph S, Di Stilo A,
Fruttero R,
Gasco A.
Abstract
A new series of (((R-oxy)carbonyl)oxy)methyl esters of Aspirin (ASA), bearing
nitric oxide (NO) or hydrogen sulfide (H2S) releasing groups, was synthesized and the compounds evaluated as new ASA co-drugs. All the products were quite stable in buffered solution at pH 1 and 7.4. Conversely, they were all rapidly metabolized, producing ASA and the
NO/H2S releasing moiety used for their preparation. Consequent on ASA release, the compounds were capable of inhibiting collagen-induced platelet aggregation of human platelet-rich plasma (PRP). The simple
NO/H2S donor substructures were able to relax contracted rat aorta strips, with a NO- and H2S-dependent mechanism, respectively, but they either did not trigger antiaggregatory activity or displayed antiplatelet potency markedly below that of the related co-drug. The new products might provide a safer and improved alternative to the use of ASA principally in its anti-inflammatory and antithrombotic applications.