Discovery of novel trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems |
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| Authors: | Imamura H Ohtake N Shimizu A Sato H Sugimoto Y Sakuraba S Nagano R Nakano M Abe S Suzuki-Sato C Nishimura I Kojima H Tsuchiya Y Yamada K Hashizume T Morishima H |
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| Institution: | Banyu Tsukuba Research Institute, Ibaraki, Japan. imamrahk@banyu.co.jp |
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| Abstract: | Novel trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems were designed and synthesized to provide J-111,347 (1a) as the first example of an exceptionally broad-spectrum antibiotic, showing activity against methicillin-resistant Staphyloccocus aureus (MRSA) as well as Pseudomonas aeruginosa. Further derivation of 1a afforded J-111,225 (2a), J-114,870 (3a), and J-114,871 (3b). which showed improved safety profiles and retained broad-spectrum antibacterial activities. |
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