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• W2051215183 abstract "Setting: Because of widespread emergence of resistant Mycobacterium tuberculosis and the high incidence of opportunistic infection caused by M. avium complex (MAC) in AIDS patients, there is an urgent need for new drugs against these organisms.Objective: To evaluate the activity of newly synthesized 2′2-bipyridyl analogues against MAC and M. tuberculosis.Design: Susceptibility of MAC and M. tuberculosis to VUF-8514 and VUF-8842 were determined by both tube dilution method using 7H9 broth and radiometric (BACTEC) method using 14C-palmitic acid.Results and Conclusions: The MICs of 8514 against MAC and M. tuberculosis wee 1 μg/ml and 0.5 μg/ml respectively, while for 8842 the respective values were 8 μg/ml and 2 μg/ml. In general, the MBC values for both drugs were two-fold higher than their corresponding MIC values. However, both drugs exhibited high bactericidal activities against both organisms. The MICs of clinical isolates of both organisms were in the same range as reference strains; furthermore, two isolates of M. tuberculosis that showed resistance to rifampicin were found to be susceptible to 8514. Thus, these two bipyridyl analogues show great promise in chemotherapy of tuberculosis and M. avium infection.Cadre: L'émergence étendue de formes résistantes de Mycobacterium tuberculosis, ainsi que l'incidence élevée d'infections opportunistes dues au complexe M. avium (MAC) chez des malades atteints de SIDA, soulignent la nécessité urgente de trouver de nouveaux médicaments contre ces organismes.Objet: Evaluer l'activité des analogues du 2,2′-bipyridyl récemment synthétisés contre MAC et M. tuberculosis. Schéma: La sensibilité de MAC et M. tuberculosis vis à vis de VUF-8514 et VUF-8842 a étéévaluée utilisant les méthodes de dilution en tubes, avec le milieu 7H9, et de radiométrie (BACTEC), avec l'acide 14C-palmitique.Résultats et Conclusions: Les concentrations minimales inhibitrices (CMI) de VUF-8514 contre MAC et M. tuberculosis étaient de 1 μg/ml et 0,5 μg/ml respectivement, tandis que pour VUF-8842 les valeurs respectives étaient de 8 μg/ml et 2 μg/ml. En général les valeurs CMB (concentration minimale bactéricide) pour les deux drogues étaient 2 fois plus élevées que leurs valeurs CMI correspondantes. Toutefois les deux composés ont montré une activité bactéricide puissante contre les deux organismes. Les CMI des isolats cliniques des deux organismes se trouvaient dans les mêmes zones que les souches de référence ; d'ailleurs deux isolats de M. tuberculosis qui ont montré une résistance à la rifampicine ont été sensibles à 8514. Ainsi ces deux analogues bipyridil sont prometteurs pour la chimiothérapie de tuberculose et de l'infection due à M. avium.Marco de referencia: La amplitud de la aparición de formas resistentes de Mycobacterium tuberculosis y la incidencia elevada de infecciones oportunistas causadas por el complejo M. avium (MAC) en los enfermos con SIDA, ponen en evidencia la necesidad urgente de encontrar nuevos medicamentos contra estos microorganismos.Objetivo: Evaluar la actividad contra MAC y M. tuberculosis de los análogos del 2,2′-bipiridil, recientemente sintetizados.Método: Se determinó la sensibilidad de MAC y M. tuberculosis a VUF-8514 y VUF-8842 por los métodos de dilución en tubos, usando el medio 7119 y de radiometría (BACTEC) usando el ácido 14C-palmítico.Resultados y conclusión: Las concentraciones inhibidoras mínimas (CIM) de VUF-8514 contra MAC y M. tuberculosis eran de 1 μg/ml y de 0,5 μg respectivamente, mientras que para VUF-8842 los valores respectivos eran de 8 μg/ml y 2 μg/ml. En general los valores de la concentratión bactericida minima (CBM) para ambas drogas eran dos veces más elevados que los valores CIM correspondientes. Sin embargo, ambas drogas mostraron una elevada actividad bactericida contra ambos microorganismos. Las CIM de los aislados clínicos de ambos microorganismos se encontraban dentro de los mismos márgenes que las de las cepas de referencia; además, dos aislados de M. tuberculosis que mostraron una resistencia a la rifampicina eran sensibles a VUF8514. Así, estos dos análogos de bipiridil son prometedores para la quimioterapia de la tuberculosis y de la infección con M. avium." @default.
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• W2051215183 date "1992-01-01" @default.
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• W2051215183 title "Clinical aspects of mycobacterial infections in HIV infection" @default.
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• W2051215183 doi "https://doi.org/10.1016/0923-2508(92)90049-t" @default.
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