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Heteroaromatic-aminomethyl quinolones: Potent and selective iNOS inhibitors

SG Durón, A Lindstrom, C Bonnefous, H Zhang…

文献索引:Duron, Sergio G.; Lindstrom, Andrew; Bonnefous, Celine; Zhang, Hui; Chen, Xiaohong; Symons, Kent T.; Sablad, Marciano; Rozenkrants, Natasha; Zhang, Yan; Wang, Li; Yazdani, Nahid; Shiau, Andrew K.; Noble, Stewart A.; Rix, Peter; Rao, Tadimeti S.; Hassig, Christian A.; Smith, Nicholas D. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 2 p. 1237 - 1241

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被引用次数: 4

摘要

The overproduction of nitric oxide during the biological response to inflammation by the nitric oxide synthase (NOS) enzymes have been implicated in the pathology of many diseases. By removal of the amide core from uHTS-derived quinolone 4, a new series highly potent heteroaromatic-aminomethyl quinolone iNOS inhibitors 8 were identified. SAR studies led to identification of piperazine 22 and pyrimidine 32, both of which reduced plasma nitrates ...