Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds |
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| Authors: | Imamura H Ohtake N Shimizu A Sato H Sugimoto Y Sakuraba S Kiyonaga H Suzuki-Sato C Nakano M Nagano R Yamada K Hashizume T Morishima H |
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| Institution: | Banyu Tsukuba Research Institute, Ibaraki, Japan. |
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| Abstract: | Through further derivatization of J-111,347 (1a), a trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenem, undesired epileptogenicity in a rat intracerebroventricular assay (200 microg/rat) could be eliminated to afford J-111,225 (2a), J-114,870 (3a) and J-114,871 (3b) which preserved comparable broad antimicrobial activity. |
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