CHEMICAL MODIFICATION OF TAZOBACTAM - SYNTHESIS OF 2-BETA-[(4-SUBSTITUTED)-1,2,3-TRIAZOL-1-YL]METHYL PENICILLANIC ACID SULFONE DERIVATIVES

Citation
El. Setti et al., CHEMICAL MODIFICATION OF TAZOBACTAM - SYNTHESIS OF 2-BETA-[(4-SUBSTITUTED)-1,2,3-TRIAZOL-1-YL]METHYL PENICILLANIC ACID SULFONE DERIVATIVES, Journal of antibiotics, 48(11), 1995, pp. 1320-1329
Citations number
19
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
ISSN journal
00218820
Volume
48
Issue
11
Year of publication
1995
Pages
1320 - 1329
Database
ISI
SICI code
0021-8820(1995)48:11<1320:CMOT-S>2.0.ZU;2-U
Abstract
A series of 2 beta-[(4-substituted)-1,2,3-triazol-1-yl]methyl penicill anic acid sulfones was synthesized as P-lactamase inhibitors. Many of these compounds showed good in vitro inhibitory activity against penic illinase, cefotaximase and plasmid-mediated class III TEM enzymes, but exhibited weaker cephalosporinase inhibition. One member in this seri es-2 1,2,3-triazol-1-yl]methyl-6,6-dihydropenicillanate 1,1-dioxide (1 2a), when tested in combination with piperacillin, showed excellent sy nergistic activity against microorganisms producing plasmid-mediated e nzymes, but had insufficient activity against microorganisms producing chromosomally mediated class I enzymes.