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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.
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Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.

机译:口服生物利用型诱导型一氧化氮合酶抑制剂的设计与合成。第1部分:二氢吡啶-2-亚胺的合成和生物学评估。

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摘要

Dihydropyridin-2-imines were synthesized and biologically evaluated both in vitro and in vivo using a nitric oxide inhibition assay. Compounds 1, 4, 5 and 7-11 exhibited potent activity in the inducible nitric oxide (iNOS) inhibition assay. Of these 5, 6, 9 and 10 showed 5- to 11-fold increases in isoform selectivity. Compounds 1, 5, 9 and 10 showed potent inhibitory activity in the NOx accumulation assay in mice. Compounds 1 and 5 also showed good bioavailability (BA) when given orally.
机译:合成二氢吡啶-2-亚胺,并使用一氧化氮抑制试验在体内和体外进行生物学评估。化合物1、4、5和7-11在诱导型一氧化氮(iNOS)抑制试验中表现出强大的活性。在这些5、6、9和10中,同工型选择性提高了5到11倍。化合物1、5、9和10在小鼠的NOx积累测定中显示出有效的抑制活性。口服时,化合物1和5也显示出良好的生物利用度(BA)。

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