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  • Title: Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives.
    Author: Ueda S, Terauchi H, Suzuki K, Yano A, Matsumoto M, Kubo T, Minato H, Arai Y, Tsuji J, Watanabe N.
    Journal: Bioorg Med Chem Lett; 2005 Mar 01; 15(5):1361-6. PubMed ID: 15713387.
    Abstract:
    We have previously reported that (4R,5R)-5-ethyl-2-imino-4-methylthiazolidine (3) strongly inhibits inducible nitric oxide synthase (iNOS). In a successive search for strong and selective iNOS inhibitors, we, herein, describe the synthesis of the selenium analogue of 3 (4: ES-2133) and its related optically active compounds and examine their in vitro and in vivo inhibitory activity against iNOS. In addition, an alternative synthetic method to the selected compound 4 and its pharmacokinetic profile is also reported.
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