New series of 3-phenylquinoxaline 1,4-di-N-oxide with selective activity against Mycobacterium tuberculosis have been prepared and evaluated. Thirty-four of the seventy tested compounds showed an MIC value less than 0.2 microg/mL, a value on the order of the MIC of rifampicin. Furthermore, 45% of the evaluated derivatives showed a good in vitro activity/toxicity ratio. The most active and selective compounds carry a fluorine atom in the quinoxaline 7-position or in the phenyl substituent para-position. In conclusion, the potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for synthesizing new analogues, particularly compound 7-methyl-3-(4'-fluoro)phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide (MIC <0.2 microg/mL and SI > 500).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmc.2008.10.086 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Dopamine genetic risk scores and psychiatric symptoms: Interacting risk factors for impulse control behaviours in de novo Parkinson's disease.
J Neuropsychol
January 2025
Department of Health, Medical and Neuropsychology, Leiden University, Leiden, The Netherlands.
Up to 45% of patients with Parkinson's disease (PD) experience impulse control disorders (ICDs), characterized by a loss of voluntary control over impulses, drives or temptations. This study aimed to investigate whether previously identified genetic and psychiatric risk factors interact towards the development of ICDs in PD. A total of 278 de novo PD patients (ICD-free at enrollment) were selected from the Parkinson's Progression Markers Initiative database.
View Article and Find Full Text PDFThe AhR pathway regulation in phthalates-induced cancer promotion, progression and metastasis: a scoping review.
Cancer Cell Int
January 2025
Department of Toxicology, Faculty of Medical Science, Tarbiat Modares University, Tehran, Iran.
Background: Cancer remains a leading cause of death worldwide. Environmental factors, specifically endocrine-disrupting chemicals (EDCs), like phthalates, are increasingly being linked to cancer development. Phthalates, widely used in consumer products, can activate the aryl hydrocarbon receptor (AhR).
View Article and Find Full Text PDFA randomised controlled implementation trial of the feasibility and effectiveness of school staff delivery of a selective substance use and mental health program during the COVID-19 pandemic.
BMC Public Health
January 2025
The Matilda Centre for Research in Mental Health and Substance Use, The University of Sydney, Level 6, Jane Foss Russell Building, Sydney, NSW, 2006, Australia.
Background: Preventure is a selective school-based personality-targeted program that has shown long-term benefits in preventing student alcohol use, internalising and externalising problems when delivered by psychologists. In this first Australian randomised controlled trial of school staff implementation of Preventure, we aimed to examine i) acceptability, feasibility, and fidelity and ii) effectiveness of Preventure on student alcohol use, internalising, and externalising symptoms.
Methods: A cluster-randomised controlled implementation trial was conducted in Sydney, Australia and was guided by the RE-AIM framework (Glasgow et al.
Physical literacy among chinese elementary school students: the mediating role of physical knowledge and physical competency.
BMC Public Health
January 2025
School of Health Management Policy, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 46 Xizongbu Hutong, Dongcheng District, Beijing, 100730, People's Republic of China.
Background: Physical literacy (PL) is pivotal for improving sedentary behaviors, enhancing intrinsic motivation for physical activity, and supporting the growth and development of adolescents. This study aims to measure the current situation and internal pathway of PL among Chinese elementary school students.
Methods: This study was conducted from June to July 2022 and used multistage cluster sampling to select the study subjects.
Decision-making behavior of blood glucose management and its influencing factors in pregnant women with gestational diabetes mellitus.
BMC Pregnancy Childbirth
January 2025
Department of Obstetrics, the Affiliated Hospital of Qingdao University, Qingdao, China.
Background: Currently, most studies only focus on the glucose management level and self- management behavior of pregnant women with gestational diabetes mellitus, but lack analysis and discussion on their decision-making behavior and influencing factors during glucose management.
Aim: This study aimed to investigate the decision-making behavior of blood glucose management and its influencing factors among pregnant women with gestational diabetes mellitus in China.
Methods: This was a prospective study.
Want 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!