Time-dependence and preliminary SAR studies in inhibition of nitric oxide synthase isoforms by homologues of thiocitrulline.

@article{Goodyer2003TimedependenceAP,
  title={Time-dependence and preliminary SAR studies in inhibition of nitric oxide synthase isoforms by homologues of thiocitrulline.},
  author={Claire L M Goodyer and Edwin C. Chinje and Mohammed Jaffar and Ian James Stratford and Michael D. Threadgill},
  journal={Bioorganic & medicinal chemistry letters},
  year={2003},
  volume={13 21},
  pages={3679-80}
}
Treatment of N(alpha)-Cbz-N(epsilon)-(2-hydroxyethylaminothiocarbonyl)-L-lysine N-(2-hydroxyethyl)amide with boiling hydrochloric acid gave N(epsilon)-(4,5-dihydrothiazol-2-yl)-L-lysine. This was a weak and non-isoform selective inhibitor of NOS, whereas N(epsilon)-aminothiocarbonyl-L-lysine and its methyl ester were potent, with IC(50)=13 and 18 microM… CONTINUE READING