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  • Title: Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
    Author: Young RJ, Alderton W, Angell AD, Beswick PJ, Brown D, Chambers CL, Crowe MC, Dawson J, Hamlett CC, Hodgson ST, Kleanthous S, Knowles RG, Russell LJ, Stocker R, Woolven JM.
    Journal: Bioorg Med Chem Lett; 2011 May 15; 21(10):3037-40. PubMed ID: 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.
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