杂环羧脒类化合物作为诱导型一氧化氮合酶抑制剂；（2R）-2-吡咯烷甲脒作为一种有效的、选择性的血红素配位抑制剂的发现。
Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
机构信息
GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):3037-40. doi: 10.1016/j.bmcl.2011.03.038. Epub 2011 Mar 21.
PMID:21482467
Abstract
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 μM) 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.
摘要
杂环羧脒被合成并评估为一氧化氮合酶抑制剂。特别是（2R）-2-吡咯烷甲脒，被证明是一种高效的体外（IC50=0.12 μM）和选择性 iNOS 抑制剂（对 eNOS 和 nNOS 的抑制作用超过 100 倍），可能与关键的锚定谷氨酸残基结合，并与血红素铁配位。
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