Research on New β-Lactam Antibiotics ; Penem and Carbapenem

In the research of penems, a versatile intermediate 2-thioxopenam was synthesized, from which many penem derivatives were obtained. The structure-activity relationship analysis of the synthesized penens showed that cyclic amine side chain was most effective one as a substituent of 2-thiopenems. Seve...

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Published inYAKUGAKU ZASSHI Vol. 107; no. 3; pp. 175 - 191
Main Authors SUGIMURA, YUKIO, HIRAOKA, TETSUO
Format Journal Article
LanguageJapanese
Published The Pharmaceutical Society of Japan 25.03.1987
Subjects
2-oxocarbapenam
2-thioxopenam
carbapenem
penem
thienamycin
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Summary:In the research of penems, a versatile intermediate 2-thioxopenam was synthesized, from which many penem derivatives were obtained. The structure-activity relationship analysis of the synthesized penens showed that cyclic amine side chain was most effective one as a substituent of 2-thiopenems. Several carbapenems with the same side chain as penems at 2-position were synthesized, one of the compounds was RS-533. Some effective methods for carbapenem synthesis were also discussed.
ISSN:0031-6903
1347-5231
DOI:10.1248/yakushi1947.107.3_175