SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 2-AZETIDINONE-1-SULFONIC ACID DERIVATIVES WITH A HETEROATOM-BOUND SUBSTITUENT AT THE 4-POSITION

SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 2-AZETIDINONE-1-SULFONIC ACID DERIVATIVES WITH A HETEROATOM-BOUND SUBSTITUENT AT THE 4-POSITION

The synthesis and antibacterial activity of 3-[(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)-acetamido]-2-azetidinone-1-sulfonic acid derivatives with a heteroatom-bound substituent at the 4-position are described. The effect of various 4-substituents on the antibacterial activity was examined. Some of...

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Veröffentlicht in:Journal of antibiotics 1985, Vol.38(10), pp.1387-1400
Hauptverfasser: NOGUCHI, NORIYOSHI, MASUYA, HIROTOMO, SUGAWARA, TOHORU, KAWANO, YASUHIKO, MATSUO, TAISUKE, OCHIAI, MICHIHIKO
Format: Artikel
Sprache:eng
Schlagworte:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Bacteria - drug effects
Chemistry
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms
Lactams - chemical synthesis
Lactams - pharmacology
Organic chemistry
Preparations and properties
Structure-Activity Relationship
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Zusammenfassung:The synthesis and antibacterial activity of 3-[(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)-acetamido]-2-azetidinone-1-sulfonic acid derivatives with a heteroatom-bound substituent at the 4-position are described. The effect of various 4-substituents on the antibacterial activity was examined. Some of these compounds showed excellent antibacterial activity especially against Gram-negative bacteria, including β-lactamase-producing strains.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.38.1387