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Synthesis of steroidal inhibitors for Mycobacterium tuberculosis.
Churchman, Luke R; Beckett, James R; Tan, Lendl; Woods, Kyra; Doherty, Daniel Z; Ghith, Amna; Bernhardt, Paul V; Bell, Stephen G; West, Nicholas P; De Voss, James J.
Affiliation
  • Churchman LR; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • Beckett JR; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • Tan L; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • Woods K; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • Doherty DZ; Department of Chemistry, University of Adelaide, Adelaide, South Australia 5005, Australia.
  • Ghith A; Department of Chemistry, University of Adelaide, Adelaide, South Australia 5005, Australia.
  • Bernhardt PV; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • Bell SG; Department of Chemistry, University of Adelaide, Adelaide, South Australia 5005, Australia.
  • West NP; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia.
  • De Voss JJ; School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, Brisbane, Queensland 4072, Australia. Electronic address: j.devoss@uq.edu.au.
J Steroid Biochem Mol Biol ; 239: 106479, 2024 05.
Article in En | MEDLINE | ID: mdl-38346478
ABSTRACT
Oxidised derivatives of cholesterol have been shown to inhibit the growth of Mycobacterium tuberculosis (Mtb). The bacteriostatic activity of these compounds has been attributed to their inhibition of CYP125A1 and CYP142A1, two metabolically critical cytochromes P450 that initiate degradation of the sterol side chain. Here, we synthesise and characterise an extensive library of 28 cholesterol derivatives to develop a structure-activity relationship for this class of inhibitors. The candidate compounds were evaluated for MIC with virulent Mtb and in binding studies with CYP125A1 and CYP142A1 from Mtb.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Mycobacterium tuberculosis Language: En Journal: J Steroid Biochem Mol Biol Journal subject: BIOLOGIA MOLECULAR / BIOQUIMICA Year: 2024 Document type: Article Affiliation country: Country of publication:
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Mycobacterium tuberculosis Language: En Journal: J Steroid Biochem Mol Biol Journal subject: BIOLOGIA MOLECULAR / BIOQUIMICA Year: 2024 Document type: Article Affiliation country: Country of publication: