Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens

Nghi Nguyen, Danny W. Wilson, Gayathri Nagalingam, James A. Triccas, Elena K. Schneider, Jian Li, Tony Velkov, Jonathan Baell

Research output: Contribution to journalArticleResearchpeer-review

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.

LanguageEnglish
Pages507-518
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Volume148
DOIs
StatePublished - 25 Mar 2018

Keywords

  • Diphenyleneiodonium
  • Gram-negative
  • Malaria
  • Plasmodium
  • Type II NADH-quinone oxidoreductase

Cite this

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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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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.

In: European Journal of Medicinal Chemistry, Vol. 148, 25.03.2018, p. 507-518.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens

AU - Nguyen,Nghi

AU - Wilson,Danny W.

AU - Nagalingam,Gayathri

AU - Triccas,James A.

AU - Schneider,Elena K.

AU - Li,Jian

AU - Velkov,Tony

AU - Baell,Jonathan

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KW - Plasmodium

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