Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na +/H + exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury

Novel benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na +/H + exchanger inhibitors. Most of them possess significant cardioprotective effects. A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and s...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (9), p.2430-2433
Main Authors: Zhang, Rui, Lei, Lin, Xu, Yun-Gen, Hua, Wei-Yi, Gong, Guo-Qing
Format: Article
Language:English
Subjects:
Animals
Benzoylguanidine derivatives
Biological and medical sciences
Blood Platelets - drug effects
Cardiovascular system
Chemistry, Pharmaceutical - methods
Drug Design
Drug Evaluation, Preclinical
Guanidines - chemistry
Guanidines - pharmacology
Imidazoles - chemistry
Imidazoles - pharmacology
Inhibitory Concentration 50
Medical sciences
Miscellaneous
Models, Chemical
Molecular Conformation
Myocardial ischemic-reperfusion injury
Na +/H + exchanger
Na +/H + exchanger inhibitors
Pharmacology. Drug treatments
Rats
Reperfusion Injury - drug therapy
Sodium-Hydrogen Exchangers - chemistry
Synthesis
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Summary:Novel benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na +/H + exchanger inhibitors. Most of them possess significant cardioprotective effects. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.02.035