Strong In Vitro Activities of Two New Rifabutin Analogs against Multidrug-Resistant Mycobacterium tuberculosis-Reference-Cited by-同舟云学术

Strong In Vitro Activities of Two New Rifabutin Analogs against Multidrug-Resistant Mycobacterium tuberculosis

Published:2010-12 Issue:12 Volume:54 Page:5363-5365
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

García Ana-Belén¹,Palacios Juan J.²,Ruiz María-Jesús³,Barluenga José¹,Aznar Fernando¹,Cabal María-Paz¹,García José María⁴,Díaz Natalia⁵

Affiliation:

1. Instituto Universitario de Química Organometálica Enrique Moles, Unidad Asociada al C.S.I.C., Universidad de Oviedo, c/ Julián Clavería 8, 33006 Oviedo, Spain

2. Unidad de Referencia Regional de Micobacterias, Hospital Universitario Central de Asturias, c/ Doctor Bellmunt s/n, 33006 Oviedo, Spain

3. Servicio de Microbiología Clínica, Hospital General Universitario Gregorio Marañón, c/ Dr. Esquerdo 46, 28007 Madrid, Spain

4. Servicio de Neumología, Hospital San Agustín, Camino de Heros 4, 33400 Avilés, Spain

5. Departamento de Química Física y Analítica, Universidad de Oviedo, c/ Julián Clavería 8, 33006 Oviedo, Spain

Abstract

ABSTRACT Two new rifabutin analogs, RFA-1 and RFA-2, show high in vitro antimycobacterial activities against Mycobacterium tuberculosis . MIC values of RFA-1 and RFA-2 were ≤0.02 μg/ml against rifamycin-susceptible strains and 0.5 μg/ml against a wide selection of multidrug-resistant strains, compared to ≥50 μg/ml for rifampin and 10 μg/ml for rifabutin. Molecular dynamic studies indicate that the compounds may exert tighter binding to mutants of RNA polymerase that have adapted to the rifamycins.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00149-10

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