SYNTHESIS AND BETA-LACTAMASE INHIBITORY PROPERTIES OF 2-BETA-[(1,2,3-TRIAZOL-1-YL)METHYL]-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACID 1,1-DIOXIDE AND RELATED TRIAZOLYL DERIVATIVES
SYNTHESIS AND BETA-LACTAMASE INHIBITORY PROPERTIES OF 2-BETA-[(1,2,3-TRIAZOL-1-YL)METHYL]-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACID 1,1-DIOXIDE AND RELATED TRIAZOLYL DERIVATIVES
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DOI：
10.1021/jm00391a032
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发表时间：
1987-08-01
影响因子：
7.3
通讯作者：
OGAWA, K
中科院分区：
文献类型：
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作者：
MICETICH, RG;MAITI, SN;OGAWA, K
Benzhydryl 2.beta.-[(1,2,3-triazol-1-yl)methyl]-2.alpha.-methylpenam-3.alpha.-carboxylate 1,1-dioxide was prepared by heating benzhydryl 2.beta.-(azidomethyl)-2.alpha.-methylpenam-3.alpha.-carboxylate 1,1-dioxide with (trimethylsilyl)acetylene. The ester group was removed by hydrogenolysis to give sodium 2.beta.-[(1,2,3-triazol-1-yl)methyl]-2.alpha.-methylpenam-3.alpha.-carboxylate 1,1-dioxide (3i YTR-830), which was found to be a potent inhibitor of various bacterial .beta.-lactamases. A series of related compounds was prepared in a similar way, and all of these compounds show excellent .beta.-lactamase inhibitory properties.
