novel and orally bioavailable inducible nitric oxide synthase inhibitors. synthesis and evaluation...

2005 Organo-selenium compounds

Organo-selenium compoundsS 0130 Novel and Orally Bioavailable Inducible Nitric Oxide Synthase Inhibitors. Syn-

thesis and Evaluation of Optically Active 4,5-Dialkyl-2-iminoselenazolidine De-rivatives. — A series of novel optically active 4,5-dialkyl-2-iminoselenazolidine de-rivatives (VII) and (VIII) is synthesized by two synthetic methods. The pathway via the chromatographic separation of the isomers (V) and (VI) is also used for the synthesis of the enantiomers of (VII) and (VIII). All compounds are examined for their in vitro and in vivo inhibitory activity against iNOS. (VII) shows the best selectivity for iNOS and strong inhibitory activity. — (UEDA*, S.; TERAUCHI, H.; SUZUKI, K.; YANO, A.; MATSUMOTO, M.; KUBO, T.; MINATO, H.; ARAI, Y.; TSUJI, J.-I.; WATANABE, N.; Bioorg. Med. Chem. Lett. 15 (2005) 5, 1361-1366; Chem. Res. Lab., Dainippon Pharm. Co., Ltd., Suita, Osaka 564, Japan; Eng.) — H. Haber

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