The preparation and evaluation of novel aryl urea analogs as broad-spectrum antibacterial agents is described. Numerous compounds showed low micromolar minimum inhibitory concentrations (MIC) against both Gram-positive and Gram-negative bacteria. Selected analogs also exhibited in vivo efficacy in a lethal murine model of bacterial septicemia.
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http://dx.doi.org/10.1016/j.bmcl.2004.08.059 | DOI Listing |
Chem Asian J
December 2024
Birla Institute of Technology and Science - Pilani Campus: Birla Institute of Technology & Science Pilani, Chemistry, Vidya Vihar, 333031, Pilani, INDIA.
Phys Chem Chem Phys
December 2024
Department of Chemistry and Pharmaceutical Sciences, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.
The hydrogen-bond donor strength of ureas, widely used in hydrogen-bond donor catalysis, molecular recognition, and self-assembly, can be enhanced by increasing the size of the chalcogen X in the CX bond from O to S to Se and by introducing more electron-withdrawing substituents because both modifications increase the positive charge on the NH groups which become better hydrogen-bond donors. However, in 1,3-diaryl X-ureas, a steric mechanism disrupts the positive additivity of these two tuning factors, as revealed by our quantum-chemical analyses. This leads to an enhanced hydrogen-bond donor strength, despite a lower NH acidity, for 1,3-diaryl substituted O-ureas compared to the S- and Se-urea analogs.
View Article and Find Full Text PDFEur J Med Chem
February 2025
Department of Pediatrics, University of California San Francisco, San Francisco, CA, USA. Electronic address:
Pendrin (SLC26A4) is an anion exchanger expressed in epithelial cells of kidney and lung. Pendrin inhibition is a potential treatment approach for edema, hypertension and inflammatory lung diseases. We have previously identified first-in-class pendrin inhibitors by high-throughput screening, albeit with low potency for pendrin inhibition (IC ∼10 μM).
View Article and Find Full Text PDFBioorg Chem
December 2024
Pharmacognosy Department, Pharmaceutical and Drug Industry Institute, National Research Centre, 12622 Dokki, Egypt.
To investigate the therapeutic potential of 5-Fluorouracil-based analogues, a straightforward synthetic technique was employed to synthesize a novel series of 5-arylurea uracil derivatives (AUFU01-03) and aryl-urea derivatives bearing perfluorophenyl (AUPF01-03). Reliable tools such as infrared (IR), Nuclear Magnetic Resonance (NMR) spectra, and elemental analyses were utilized to confirm the chemical structures and purity of these compounds. In comparison to healthy noncancerous control skin fibroblast cells (BJ-1), we examined the antiproliferative efficacy of compounds (AUFU01-03) and (AUPF01-03) against specific human malignant cell lines of the breast (MCF-7), and colon (HCT-116).
View Article and Find Full Text PDFInt J Biol Macromol
November 2024
Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P. O. Box 31441, Dammam, Saudi Arabia.
Urease catalyzes the hydrolysis of urea, leading to an increase in stomach pH and supporting Helicobacter pylori survival, which is linked to several gastrointestinal disorders. In this study, thiazine-based Schiff bases were explored as promising urease inhibitors. Various spectroscopic techniques characterized the synthetic library of thiazine Schiff bases 2-36 and also evaluated for their inhibitory activities against urease.
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