Compound 64716, 1-ethyl-4 (1H)-oxo-[1,3]dioxolo[4,5-g]cinnoline-3-carboxylic acid, is a new synthetic antibacterial agent. The antibacterial spectrum of this compound includes gram-negative bacteria that are most frequently isolated from urinary tract infections. Minimal inhibitory concentration values of 64716 for isolates of Escherichia coli and Proteus sp. ranged from 2 to 4 and 2 to 8 mug/ml, respectively, and the compound was bactericidal at concentrations close to the minimal inhibitory concentration values. In vivo, doses required for successful therapy of experimental mouse infections were comparable to those for nalidixic acid. After oral administration of 40 mg/kg, peak concentrations of this compound in mouse blood reached 19.2 mug/ml. Within 30 min after doses of 20 mg/kg, bacteriologically active drug concentrations of 64716, nalidixic acid, and oxolinic acid in mouse urine were >1,000, 170, and <1.5 mug/ml, respectively. Resistant bacteria were not selected when bacteria were exposed to 500 mug/ml of 64716. Compound 64716 was less bound by human serum proteins than was nalidixic acid. Equivalent antibacterial activity along with superior pharmacological properties of 64716 when compared with nalidixic acid lead to the conclusion that this new compound is a promising antibacterial agent.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC444569 | PMC |
| http://dx.doi.org/10.1128/AAC.4.4.415 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Groundwater antibiotics contamination in an alluvial-pluvial fan, North China Plain: Occurrence, sources, and risk assessment.
Environ Res
October 2023
Institute of Hydrogeology and Environmental Geology, Chinese Academy of Geological Sciences, Shijiazhuang, 050061, China; Hebei Key Laboratory of Groundwater Remediation, Shijiazhuang, 050061, China. Electronic address:
Antibiotics in groundwater have received widespread concern because high levels of them harm aquatic ecosystems and human health. This study aims to investigate the concentration, distribution, ecological and human health risks as well as potential sources of antibiotics in groundwater in the Hutuo River alluvial-pluvial fan, North China Plain. A total of 84 groundwater samples and nine surface water samples were collected, and 35 antibiotics were analyzed using ultra-performance liquid chromatography-tandem mass spectrometry.
View Article and Find Full Text PDFPrioritization, sources, and ecological risk of typical antibiotics in the Huai River, a Chinese major river: a warning about aquaculture.
Environ Sci Pollut Res Int
May 2023
Anhui Provincial Engineering Laboratory of Water and Soil Pollution Control and Remediation, School of Ecology and Environment, Anhui Normal University, Wuhu, Anhui, 241002, People's Republic of China.
This is the first comprehensive report on antibiotics in the Huai River, a major Chinese river. To illuminate the concentrations, prioritization, spatial distributions, sources, and ecological risks of antibiotics, surface water samples were collected and three types of most widely used antibiotics (16 sulfonamides, 8 tetracyclines, and 14 quinolones) were analyzed. The results indicated that concentrations of ∑quinolones (86 ± 31 ng/L) > ∑tetracyclines (20 ± 13 ng/L) > ∑sulfonamides (11 ± 3.
View Article and Find Full Text PDFStoichiometry-Selective Antagonism of α4β2 Nicotinic Acetylcholine Receptors by Fluoroquinolone Antibiotics.
ACS Chem Neurosci
June 2022
Division of Biosciences, University College London, London WC1E 6BT, United Kingdom.
Quinolone antibiotics disrupt bacterial DNA synthesis by interacting with DNA gyrase and topoisomerase IV. However, in addition, they have been shown to act as inhibitors of pentameric ligand-gated ion channels such as GABA receptors and the α7 nicotinic acetylcholine receptor (nAChR). In the present study, we have examined the effects of quinolone antibiotics on the human α4β2 nAChR, an important subtype that is widely expressed in the central nervous system.
View Article and Find Full Text PDFValidation of two UHPLC-MS/MS methods for fast and reliable determination of quinolone residues in honey.
Food Addit Contam Part A Chem Anal Control Expo Risk Assess
May 2021
Department of R&D, Altıparmak Food Industry and Trade Inc, Istanbul, Turkey.
Antibiotic usage for beekeeping, including quinolones, can lead to residues in honey and these residues usually result from the drugs used in the treatment of American or European foulbrood diseases. Residues in honey may cause allergic reactions as well as increased antibiotic resistance. Within this study, rapid and breakthrough analysis methods were developed using UHPLC-ESI-MS/MS and sample preparation processes were minimised.
View Article and Find Full Text PDFTranscriptomic analysis of key genes and pathways in human bronchial epithelial cells BEAS-2B exposed to urban particulate matter.
Environ Sci Pollut Res Int
February 2021
Department of Infectious Diseases, Zhongshan Hospital, Fudan University, 180 Fenglin Road, Shanghai, 200032, China.
Urban particulate matter (PM), a great danger to public health, is associated with increasing risk of pulmonary diseases. However, the involved key genes and signaling pathways mediating the cellular responses to urban PM are largely unknown. In this study, human bronchial epithelial cells BEAS-2B was exposed to Standard reference material (SRM) 1649b, followed by RNA-sequencing (RNA-seq) and a combination of different bioinformatics analysis.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!