Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives |
| |
Authors: | Ueda Shigeo Terauchi Hideo Suzuki Kenji Yano Akihiro Matsumoto Masashi Kubo Taeko Minato Hisao Arai Yukiyo Tsuji Jun-ichi Watanabe Nobuhide |
| |
Affiliation: | Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, Enoki-cho 33-94, Suita, Osaka 564-0053, Japan. shigeo-ueda@dainippon-pharm.co.jp |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|