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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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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container_end_page 1040
container_issue 9
container_start_page 1030
container_title Journal of antibiotics
container_volume 47
creator IM, CHAEUK
MAITI, SAMARENDRA N.
MICETICH, RONALD G.
DANESHXALAB, MOHSEN
ATCHISON, KEVIN
PHILLIPS, OLUDOTUN A.
KUNUGITA, CHIEKO
description 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.
doi_str_mv 10.7164/antibiotics.47.1030
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ispartof The Journal of Antibiotics, 1994/09/25, Vol.47(9), pp.1030-1040
issn 0021-8820
1881-1469
language eng
recordid cdi_proquest_miscellaneous_16758113
source J-STAGE
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
title SYNTHESIS AND β-LACTAMASE INHIBITORY ACTIVITY OF 6-[(1-HETEROARYLTHIOETHYL-1, 2, 3-TRIAZOL-4-YL)-METHYLENE]PENAM SULFONES
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