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Hydrogen sulphide (H2S) is emerging as an important endogenous modulator, which exhibits the beneficial effects of nitric oxide (NO) on the cardiovascular (CV) system, without producing toxic metabolites.[1] H2S is biosynthesized in mammalian tissues by cystathionine--synthase and cystathionine--lyase. H2S exhibits the antioxidant properties of inorganic and organic sulphides, behaving as a scavenger of reactive oxygen species. H2S trigger other important effects and the activation of ATP-sensitive potassium channel (KATP) accounts for its vasorelaxing and cardioprotective effects. Furthermore, H2S inhibits smooth muscle proliferation and platelet aggregation. In non-CV systems, H2S regulates the functions of the central nervous system, as well as respiratory, gastroenteric, and endocrine systems. Conversely, H2S deficiency contributes to the pathogenesis of hypertension.Likewise, impairment of H2S biosynthesis is involved in CV complications associated with diabetes mellitus. There is also evidence of a cross-talk between the H2S and the endothelial NO pathways. In particular, recent observations indicate a possible pathogenic link between deficiencies of H2S activity and the progress of endothelial dysfunction. These biological aspects of endogenous H2S have led several authors to look at this mediator as ‘‘the new NO’’ that has given attractive opportunities to develop innovative classes of drugs.
In this study, we report the synthesis and the pharmacological evaluation of a series of new thioamide derivatives of general formula I and II as H2S donor.