SwePub
Sök i LIBRIS databas

  Utökad sökning

AMNE:(MEDICAL AND HEALTH SCIENCES)
 

Sökning: AMNE:(MEDICAL AND HEALTH SCIENCES) > Design, synthesis, ...

Design, synthesis, and evaluation of novel Δ2-thiazolino 2-pyridone derivatives that potentiate isoniazid activity in an isoniazid-resistant mycobacterium tuberculosis mutant

Sarkar, Souvik (författare)
Umeå universitet,Kemiska institutionen
Mayer Bridwell, Anne E. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Good, James A. D., 1985- (författare)
Umeå universitet,Kemiska institutionen
visa fler...
Wang, Erin R. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
McKee, Samuel R. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Valenta, Joy (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Harrison, Gregory A. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Flentie, Kelly N. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Henry, Frederick L. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Wixe, Torbjörn (författare)
Umeå universitet,Kemiska institutionen
Demirel, Peter (författare)
Umeå universitet,Kemiska institutionen
Vagolu, Siva K. (författare)
Department of Microbiology, University of Oslo, Oslo, Norway
Chatagnon, Jonathan (författare)
University Lille, CNRS, INSERM, CHU Lille, Institut Pasteur de Lille, U1019-UMR 9017-CIIL-Center for Infection and Immunity of Lille, Lille, France
Machelart, Arnaud (författare)
University Lille, CNRS, INSERM, CHU Lille, Institut Pasteur de Lille, U1019-UMR 9017-CIIL-Center for Infection and Immunity of Lille, Lille, France
Brodin, Priscille (författare)
University Lille, CNRS, INSERM, CHU Lille, Institut Pasteur de Lille, U1019-UMR 9017-CIIL-Center for Infection and Immunity of Lille, Lille, France
Tønjum, Tone (författare)
Department of Microbiology, University of Oslo, Oslo, Norway; Oslo University Hospital, Oslo, Norway
Stallings, Christina L. (författare)
Department of Molecular Microbiology, Center for Women’s Infectious Disease Research, Washington University School of Medicine, MO, St. Louis, United States
Almqvist, Fredrik (författare)
Umeå universitet,Kemiska institutionen
visa färre...
 (creator_code:org_t)
American Chemical Society (ACS), 2023
2023
Engelska.
Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 66:16, s. 11056-11077
Relaterad länk:
https://doi.org/10.1...
visa fler...
https://umu.diva-por... (primary) (Raw object)
https://urn.kb.se/re...
https://doi.org/10.1...
visa färre...
  • Tidskriftsartikel (refereegranskat)
Abstract Ämnesord
Stäng  
  • Mycobacterium tuberculosis (Mtb) drug resistance poses an alarming threat to global tuberculosis control. We previously reported that C10, a ring-fused thiazolo-2-pyridone, inhibits Mtb respiration, blocks biofilm formation, and restores the activity of the antibiotic isoniazid (INH) in INH-resistant Mtb isolates. This discovery revealed a new strategy to address INH resistance. Expanding upon this strategy, we identified C10 analogues with improved potency and drug-like properties. By exploring three heterocycle spacers (oxadiazole, 1,2,3-triazole, and isoxazole) on the ring-fused thiazolo-2-pyridone scaffold, we identified two novel isoxazoles, 17h and 17j. 17h and 17j inhibited Mtb respiration and biofilm formation more potently with a broader therapeutic window, were better potentiators of INH-mediated inhibition of an INH-resistant Mtb mutant, and more effectively inhibited intracellular Mtb replication than C10. The (−)17j enantiomer showed further enhanced activity compared to its enantiomer and the 17j racemic mixture. Our potent second-generation C10 analogues offer promise for therapeutic development against drug-resistant Mtb.

Ämnesord

MEDICIN OCH HÄLSOVETENSKAP  -- Klinisk medicin -- Infektionsmedicin (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Clinical Medicine -- Infectious Medicine (hsv//eng)

Publikations- och innehållstyp

ref (ämneskategori)
art (ämneskategori)

Hitta via bibliotek

Till lärosätets databas

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

 
pil uppåt Stäng

Kopiera och spara länken för att återkomma till aktuell vy