FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and Gram-negative bacteria. A series of o-hydroxybenzylamines 1-16 and its corresponding new urea derivatives 17-32 were synthesized and fully characterized by spectroscopic methods and elemental analysis. This new urea derivatives class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 1-(5-bromo-2-hydroxybenzyl)-1-(4-fluorophenyl)-3-phenylurea (18) and 1-(5-bromo-2-hydroxybenzyl)-1-(4-chlorophenyl)-3-phenylurea (20) were potent inhibitors of E. coli FabH.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2011.06.049DOI Listing

Publication Analysis

Top Keywords

urea derivatives
12
coli fabh
8
design synthesis
4
synthesis biological
4
biological evaluation
4
evaluation urea
4
derivatives o-hydroxybenzylamines
4
o-hydroxybenzylamines phenylisocyanate
4
phenylisocyanate potential
4
fabh
4

Similar Publications

Molecular Mechanism for the Unprecedented Metal-Independent Hydroxyl Radical Production from Thioureas and HO.

Environ Sci Technol

January 2025

State Key Laboratory of Environmental Chemistry and Ecotoxicology, Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing 100085, P. R. China.

The most well-known hydroxyl radical (OH)-generating system is the classic iron-mediated Fenton reaction. Thiourea has been considered as an efficient OH scavenger and is frequently used to study the role of OH in various biochemical and medical research studies. Here we found that the highly reactive OH can be produced from thiourea and HO through a metal-independent pathway, as measured by electron spin resonance (ESR) secondary radical spin-trapping and fluorescent methods.

View Article and Find Full Text PDF

In this research, we report a simple fluorescent probe designed to detect thallium(iii) ions (Tl) in artificial urine samples. The Tl signaling probe (TP-1) was readily prepared from 2-acetyl-6-methoxynaphthalene and hydrazine. In a pH 4.

View Article and Find Full Text PDF

Objective: In the context of acute cardiogenic pulmonary edema (ACPE), a frequently encountered medical emergency associated with high early mortality rates, there is a need to predict short-term outcomes for risk stratification.Our aim was to derive and validate a model, a simple clinical scoring system using baseline vital signs, clinical and presenting characteristics, and readily available laboratory tests, that allows accurate prediction of short-term mortality in individuals experiencing ACPE.

Methods: This retrospective cohort study included 1088 patients with ACPE from six health centers.

View Article and Find Full Text PDF

Wool Fabric with an Improved Durable Biological Resistance Using a Coumarin Derivative.

ACS Appl Bio Mater

January 2025

Proteinic and Man-made Fibres Department, Textile Research and Technology Institute, National Research Centre, Cairo, Dokki, 12622, Egypt.

Wool is the most widely used proteinic natural fiber in the clothing industry by virtue of its versatile properties. Unfortunately, wool, as a natural fiber, is more susceptible to attack by microorganisms and moths, which may cause harm to the fiber and human health. That is why the antimicrobial and mothproof finishing of natural textiles is of prime importance to the textile and clothing industry.

View Article and Find Full Text PDF

This study aimed to evaluate the effect of autolyzed yeast (obtained from culture of Saccharomyces cerevisiae in sugarcane derivatives) supplementation on diet digestibility, feeding behavior, levels of blood metabolites associated with protein and energy metabolism, and performance of Dorper × Santa Ines lambs finished in feedlot. Twenty-four non-castrated male lambs with an average age of 4 months and a body weight (BW) of 19.49 ± 3.

View Article and Find Full Text PDF

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!