Design, Synthesis and Bioactivity Evaluation of Ag(I)‐, Au(I)‐ and Au(III)‐Quinoxaline‐Wingtip N‐Heterocyclic Carbene Complexes Against Antibiotic Resistant Bacterial Pathogens

ChemMedChem, Journal Year: 2024, Volume and Issue: 19(20)

Published: June 27, 2024

Intending to homogenize the biological activities of both quinoxaline and imidazole moieties, proligand, 1-methyl-3-quinoxaline-imidazolium hexaflurophosphate (1.HPF

Language: Английский

Antileishmanial and Antitrypanosomal Trends of Synthetic Tetralone Derivatives

Drug Development Research, Journal Year: 2025, Volume and Issue: 86(1)

Published: Jan. 29, 2025

ABSTRACT Leishmaniasis and trypanosomiasis are parasitic diseases that closely linked to poverty, pose significant local burdens, common in tropical subtropical regions. Various synthetic tetralone derivatives were studied as potential scaffolds for antileishmanial antitrypanosomal activities. The compounds their effectiveness against multiple kinetoplastid protozoan pathogens: Leishmania major , mexicana, bloodstream trypomastigotes of Trypanosoma brucei . Two different strains T. b. used. first strain was the wild‐type (s427‐WT), second multidrug resistant (MDR) B48, which produced by deleting TbAT1 gene from s427WT subsequent adaptation high levels resistance diamidines organo‐arsenical drugs. Compounds 4c, 7c, 9b 11b showed activity two species, establishing them versatile leads with broad anti‐kinetoplastid activity. Compound 4c a derivative bromo‐containing trimethoxybenzylidene moiety methyl‐substituted cyclohexanone ring, identified most potent inhibitor both strains, EC 50 values 0.19 0.22 µM WT respectively, showing absence cross‐resistance diamidine arsenical trypanocide classes. In addition, compound exhibited more potency than controls, eflornithine pentamidine, MDR strain. We conclude derivates could be valuable starting point discovery new antiparasitic

Language: Английский

Anti-Biofilm Action of Cineole and Hypericum perforatum to Combat Pneumonia-Causing Drug-Resistant P. aeruginosa

Antibiotics, Journal Year: 2024, Volume and Issue: 13(8), P. 689 - 689

Published: July 24, 2024

Hospital-acquired antibiotic-resistant pneumonia is one of the major causes mortality around world that pose a catastrophic threat.

Language: Английский