Studies on penam sulfones III. Synthesis and β-lactamase inhibitory activity of sodium (6R)-6-(α-hydroxybenzyl)-2β-methoxyiminomethyl-2α-methylpenam-3α-carboxylate 1,1-dioxide and sodium 2β-acyl-2α-methylpenam-3α-carboxylate 1,1-dioxide

The synthesis and in vitro synergies of (6R)-6-(α-hydroxybenzyl)-2β-methoxyiminomethyl-2α-methylpenam-3α-carboxylate 1,1-dioxide ( 4) and 2β-acyl-2α-methylpenam-3α-carboxylate 1,1-dioxide ( 15) are described. Compound 15 showed good in vitro synergy in combination with piperacillin and ceftazidime a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997, Vol.7 (1), p.11-14
Main Authors: Czajkowski, David P, Reddy, Andhe V.N, Setti, Eduardo L, Phillips, Oludotun A, Micetich, Ronald G, Kunugita, Chieko, Maiti, Samarendra N
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Medical sciences
Pharmacology. Drug treatments
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Summary:The synthesis and in vitro synergies of (6R)-6-(α-hydroxybenzyl)-2β-methoxyiminomethyl-2α-methylpenam-3α-carboxylate 1,1-dioxide ( 4) and 2β-acyl-2α-methylpenam-3α-carboxylate 1,1-dioxide ( 15) are described. Compound 15 showed good in vitro synergy in combination with piperacillin and ceftazidime against chromosomally mediated class I cephalosporinase producing organisms including TEM, SHV, and OXA-type enzymes producing microorganisms. The synthesis and in vitro synergies of sodium(6R)-6-(α-hydroxybenzyl)-2β-methoxyiminomethyl-2α-methylpenam-3α-carboxylate 1,1-dioxide( 4) and sodium 2β-acyl-2α-methylpenam-3α-carboxylate 1,1-dioxide ( 15) are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(96)00575-6