beta-Lactamase inhibitors: Synthesis and in vitro evaluation of 6-[(1-substituted-1,2,3-triazol-4-yl)methylene]-penicillanic acid sulfones

A series of 6-[(1-substituted 1,2,3-triazol-4-yl)methylene]penicillanic acid sulfones were synthesized and tested for beta-lactamase inhibitory activity. The (6Z)-isomers were over 100 times more potent than the (6E)-isomers against cell-free beta-lactamases and were synergistic with ampicillin agai...

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Bibliographic Details
Published inHeterocycles Vol. 42; no. 2; pp. 653 - 668
Main Authors Eby, P, Cummings, MD, Phillips, OA, Czajkowski, DP, Singh, MP, Spevak, P, Micetich, RG, Maiti, SN
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.01.1996
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
BRL-42715
RESISTANCE
SPECTRUM
PENAM SULFONES
DERIVATIVES
KLEBSIELLA-PNEUMONIAE
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Summary:A series of 6-[(1-substituted 1,2,3-triazol-4-yl)methylene]penicillanic acid sulfones were synthesized and tested for beta-lactamase inhibitory activity. The (6Z)-isomers were over 100 times more potent than the (6E)-isomers against cell-free beta-lactamases and were synergistic with ampicillin against a variety of beta-lactamase producing bacteria.
ISSN:0385-5414
DOI:10.3987/com-95-s62