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Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens.
Nguyen, Nghi; Wilson, Danny W; Nagalingam, Gayathri; Triccas, James A; Schneider, Elena K; Li, Jian; Velkov, Tony; Baell, Jonathan.
Afiliación
  • Nguyen N; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences Monash University, VIC, 3052, Australia.
  • Wilson DW; Research Centre for Infectious Diseases, School of Biological Sciences, University of Adelaide, Adelaide 5005, Australia; Macfarlane Burnet Institute for Medical Research and Public Health, Melbourne, Victoria 3004, Australia.
  • Nagalingam G; Microbial Pathogenesis and Immunity Group, Discipline of Infectious Diseases and Immunology, Sydney Medical School, University of Sydney, Sydney, NSW, Australia.
  • Triccas JA; Microbial Pathogenesis and Immunity Group, Discipline of Infectious Diseases and Immunology, Sydney Medical School, University of Sydney, Sydney, NSW, Australia.
  • Schneider EK; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences Monash University, VIC, 3052, Australia.
  • Li J; Monash Biomedicine Discovery Institute, Department of Microbiology, Monash University, VIC, 3800, Australia.
  • Velkov T; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences Monash University, VIC, 3052, Australia. Electronic address: Tony.Velkov@monash.edu.
  • Baell J; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences Monash University, VIC, 3052, Australia; School of Pharmaceutical Sciences, Nanjing Tech University, No. 30 South Puzhu Road, Nanjing 211816, People's Republic of China. Electronic address: Jonathan.Baell@monash.edu.
Eur J Med Chem ; 148: 507-518, 2018 Mar 25.
Article en En | MEDLINE | ID: mdl-29269132
ABSTRACT
In this study, a structure-activity relationship (SAR) compound series based on the NDH-2 inhibitor diphenyleneiodonium (DPI) was synthesised. Compounds were evaluated primarily for in vitro efficacy against Gram-positive and Gram-negative bacteria, commonly responsible for nosocomial and community acquired infections. In addition, we also assessed the activity of these compounds against Mycobacterium tuberculosis (Tuberculosis) and Plasmodium spp. (Malaria). This led to the discovery of highly potent compounds active against bacterial pathogens and malaria parasites in the low nanomolar range, several of which were significantly less toxic to mammalian cells.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Compuestos Onio / Bacterias / Malaria / Mycobacterium tuberculosis Límite: Animals Idioma: En Revista: Eur J Med Chem Año: 2018 Tipo del documento: Article País de afiliación: Australia
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Compuestos Onio / Bacterias / Malaria / Mycobacterium tuberculosis Límite: Animals Idioma: En Revista: Eur J Med Chem Año: 2018 Tipo del documento: Article País de afiliación: Australia