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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
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Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.

机译:杂环脂族羧am作为诱导型一氧化氮合酶的抑制剂; (2R)-2-吡咯烷羧am作为强效和选择性的血红素配位抑制剂的鉴定。

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摘要

Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC(50)=0.12 muM) and selective iNOS inhibitor (>100-fold vs both eNOS and nNOS), with probable binding to the key anchoring glutamate residue and co-ordination to the haem iron.
机译:合成杂环脂族car并评估其为一氧化氮合酶的抑制剂。特别是(2R)-2-吡咯烷甲box在体外具有很强的作用(IC(50)= 0.12μM)和选择性iNOS抑制剂(相对于eNOS和nNOS而言> 100倍),并且可能与关键锚固谷氨酸残基并与血红素铁配位。

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