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Synthesis and biological evaluation of 2,4-diaminopteridine derivatives as nitric oxide synthase inhibitor
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2009-04-01 , DOI: 10.1016/j.cclet.2008.12.012 Fei Ma , Gang Lü , Wei Fen Zhou , Qiu Juan Wang , Yi Hua Zhang , Qi Zheng Yao
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2009-04-01 , DOI: 10.1016/j.cclet.2008.12.012 Fei Ma , Gang Lü , Wei Fen Zhou , Qiu Juan Wang , Yi Hua Zhang , Qi Zheng Yao
Abstract A series of novel 2,4-diamino-pteridines ( 9a–l ) were synthesized and evaluated as inhibitors of inducible nitric oxide synthase (iNOS) in vitro . It was found that 9a , 9d , 9e , 9h , 9i and 9l showed potent inhibitory activities similar to that of methotrexate (MTX), while the activities of 9b , 9c , 9f , 9 g , 9j and 9k are stronger than MTX.
中文翻译:
一氧化氮合酶抑制剂2,4-二氨基蝶啶衍生物的合成及生物学评价
摘要合成了一系列新颖的2,4-二氨基-哌啶类化合物(9a–l),并在体外作为诱导型一氧化氮合酶(iNOS)的抑制剂进行了评估。发现9a,9d,9e,9h,9i和9l表现出与甲氨蝶呤(MTX)相似的有效抑制活性,而9b,9c,9f,9g,9j和9k的抑制作用强于MTX。
更新日期:2009-04-01
中文翻译:
一氧化氮合酶抑制剂2,4-二氨基蝶啶衍生物的合成及生物学评价
摘要合成了一系列新颖的2,4-二氨基-哌啶类化合物(9a–l),并在体外作为诱导型一氧化氮合酶(iNOS)的抑制剂进行了评估。发现9a,9d,9e,9h,9i和9l表现出与甲氨蝶呤(MTX)相似的有效抑制活性,而9b,9c,9f,9g,9j和9k的抑制作用强于MTX。