Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.
Microwave-promoted rhodium-catalyzed arylation of heterocycles through C-H bond activation
Performance-enhancing ligands: Two new bridged bicyclic phosphines 1a,b based on the "phoban" skeleton (see structures of their naphth-2-ylmethyl bromide salts; P yellow, Br brown, C white) are central to a practical catalytic method for the direct arylation of a variety of nitrogen heterocycles using aryl bromides. Broad functional-group tolerance was observed, and the use of microwave radiation allowed for short reaction times. (Chemical Equation Presented)
Lewis, Jared C.,Wu, Jessica Y.,Bergman, Robert G.,Ellman, Jonathan A.
p. 1589 - 1591
(2008/02/01)
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