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1.
Microorganisms ; 10(5)2022 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-35630446

RESUMEN

Pseudomonas aeruginosa is a dominant cause of respiratory infection in individuals with cystic fibrosis (CF), leading to significant morbidity and mortality. Detection of P. aeruginosa is conducted by culture of respiratory samples but this process may occasionally be compromised due to overgrowth by other bacteria and fungi. We aimed to evaluate a novel chromogenic medium, Pseudomonas aeruginosa chromogenic agar (PACA), for culture of P. aeruginosa from respiratory samples, from patients with CF. A total of 198 respiratory samples were cultured onto PACA and three other media: CHROMID® P. aeruginosa, CHROMagar™ Pseudomonas and MacConkey agar. P. aeruginosa was recovered from 66 samples (33%), using a combination of all media. After 72 h incubation, the sensitivity of the four chromogenic media was as follows: 91% for PACA and CHROMagar™ Pseudomonas, 85% for CHROMID® P. aeruginosa and 83% for MacConkey agar. For the three chromogenic media, the positive predictive value after 72 h was as follows: 95% for PACA, 56% for CHROMagar™ Pseudomonas and 86% for CHROMID® P. aeruginosa. PACA proved to be a highly effective culture medium for the isolation and specific detection of P. aeruginosa from respiratory samples.

2.
J Med Chem ; 59(6): 2780-93, 2016 Mar 24.
Artículo en Inglés | MEDLINE | ID: mdl-26907951

RESUMEN

Novel pyrroles have been designed, synthesized, and evaluated against mycobacterial strains. The pyrroles have originally been designed as hybrids of the antitubercular drugs BM212 (1) and SQ109 (2), which showed common chemical features with very similar topological distribution. A perfect superposition of the structures of 1 and 2 revealed by computational studies suggested the introduction of bulky substituents at the terminal portion of the pyrrole C3 side chain and the removal of the C5 aryl moiety. Five compounds showed high activity toward Mycobacterium tuberculosis, while 9b and 9c were highly active also against multidrug-resistant clinical isolates. Compound 9c showed low eukaryotic cell toxicity, turning out to be an excellent lead candidate for preclinical trials. In addition, four compounds showed potent inhibition (comparable to that of verapamil) toward the whole-cell drug efflux pump activity of mycobacteria, thus turning out to be promising multidrug-resistance-reversing agents.


Asunto(s)
Adamantano/análogos & derivados , Antituberculosos/síntesis química , Antituberculosos/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Etilenodiaminas/síntesis química , Etilenodiaminas/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Piperazinas/síntesis química , Piperazinas/farmacología , Pirroles/síntesis química , Pirroles/farmacología , Adamantano/síntesis química , Adamantano/farmacología , Proteínas Portadoras/efectos de los fármacos , Línea Celular , Supervivencia Celular/efectos de los fármacos , Biología Computacional , Diseño de Fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Mycobacterium/efectos de los fármacos , Preparaciones Farmacéuticas/metabolismo , Relación Estructura-Actividad
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