SYNTHESIS AND β-LACTAMASE INHIBITORY ACTIVITY OF 6-[(1-HETEROARYLTHIOETHYL-1, 2, 3-TRIAZOL-4-YL)-METHYLENE]PENAM SULFONES

The synthesis of β-lactamase inhibitory activity of a series of sodium 6-[(1-heteroarylthioethyl-1, 2, 3-triazol-4-yl)methylene]pemcillanate 1, 1-dioxides are described. Their activity was compared with tazobactam and sulbactam. The Z-isomers were more active than the E-isomers. The in vitro activit...

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Bibliographic Details
Published in:Journal of antibiotics 1994/09/25, Vol.47(9), pp.1030-1040
Main Authors: IM, CHAEUK, MAITI, SAMARENDRA N., MICETICH, RONALD G., DANESHXALAB, MOHSEN, ATCHISON, KEVIN, PHILLIPS, OLUDOTUN A., KUNUGITA, CHIEKO
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
beta-Lactamase Inhibitors
Biological and medical sciences
Drug Synergism
Medical sciences
Molecular Structure
Penicillanic Acid - analogs & derivatives
Penicillanic Acid - chemical synthesis
Penicillanic Acid - pharmacology
Pharmacology. Drug treatments
Structure-Activity Relationship
Sulbactam - pharmacology
Tazobactam
Thiadiazoles - chemical synthesis
Thiadiazoles - pharmacology
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Summary:The synthesis of β-lactamase inhibitory activity of a series of sodium 6-[(1-heteroarylthioethyl-1, 2, 3-triazol-4-yl)methylene]pemcillanate 1, 1-dioxides are described. Their activity was compared with tazobactam and sulbactam. The Z-isomers were more active than the E-isomers. The in vitro activity of the Z-isomers of the phenylthiadiazole derivatives (13a and 15a) was better than sulbactam against the tested β-lactamases and comparable to tazobactam especially against TEM-2 and cephalosporinase. But their synergistic activity with five antibiotics was inferior to tazobactam.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.47.1030