Results 31 to 40 of about 1,117 (151)

Bedaquiline: A Novel Diarylquinoline for Multidrug-Resistant Pulmonary Tuberculosis

Cureus, 2022
A new drug Bedaquiline, a diarylquinoline agent has been approved by the Food and Drug Administration for the treatment of pulmonary multidrug-resistant tuberculosis. It has been given approval for use along with the basic regimen with only conditional access through the National Program for tuberculosis in India.
Deshkar, Anuradha T, Shirure, Prashant A
openaire   +2 more sources

The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis

New England Journal of Medicine, 2009
The diarylquinoline TMC207 offers a new mechanism of antituberculosis action by inhibiting mycobacterial ATP synthase. TMC207 potently inhibits drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro and shows bactericidal activity in patients who have drug-susceptible pulmonary tuberculosis.In the first stage of a two-stage, phase 2 ...
Diacon, A. H., Pym, A., Grobusch, M., Patientia, R., Rustomjee, R., Page-Shipp, L., Pistorius, C., Krause, R., Bogoshi, M., Churchyard, G., Venter, A., Allen, J., Palomino, J. C., De Marez, T., van Heeswijk, R. P. G., Lounis, N., Meyvisch, P., Verbeeck, J., Parys, W., de Beule, K., Andries, K., McNeeley, D. F.   +21 more
openaire   +5 more sources

Genetic Basis for Natural and Acquired Resistance to the Diarylquinoline R207910 in Mycobacteria [PDF]

Antimicrobial Agents and Chemotherapy, 2006
ABSTRACT The atpE gene encoding the subunit c of the ATP synthase of Mycobacterium tuberculosis , the target of the new diarylquinoline drug R207910, has been sequenced from in vitro mutants resistant to the drug.
Petrella, Stephanie, Cambau, Emmanuelle, Chauffour, Aurélie, Andries, Koen, Jarlier, Vincent, Sougakoff, Wladimir   +5 more
openaire   +3 more sources

Direct One-Pot Synthesis of Primary 4-Amino-2,3-diaryl-quinolines via Suzuki-Miyaura Cross-Coupling of 2-Aryl-4-azido-3-iodoquinolines with Arylboronic Acids

Molecules, 2011
Palladium-catalyzed Suzuki-Miyaura cross-coupling of 2-aryl-4-azido-3-iodo-quinolines with arylboronic acids afforded the corresponding primary 4-amino-2,3-diarylquinolines in a single-pot operation along with symmetrical biaryls and traces of the 2,3 ...
Mamasegare Mabel Mphahlele, Malose Jack Mphahlele   +1 more
doaj   +1 more source

Mycobacterium tuberculosis: Pathogenesis and therapeutic targets

MedComm, Volume 4, Issue 5, October 2023., 2023
In this review, we summarize the pathogenesis of TB infection, therapeutic targets, and corresponding modulators, including first‐line medications, current clinical trial drugs and molecules in preclinical assessment. Our review provides valuable insights for future antituberculosis drug development efforts.
Jiaxing Yang, Laiying Zhang, Wenliang Qiao, Youfu Luo   +3 more
wiley   +1 more source

Recent Progress in Arylmetalative Cyclization/Annulation of Functionalized Alkynes with Organoboranes

Asian Journal of Organic Chemistry, Volume 12, Issue 5, May 2023., 2023
In this review, a comprehensive summary that focusing on the arylative metalation of functionalized alkynes with organoboranes towards the substantial developments in the stereoselective capture of the resulted vinyl metal complex with a pendent electrophile is systemized to helpful to find the gaps to discover novel transformations in arylative ...
Manda Rajesh, Gadi Ranjith Kumar
wiley   +1 more source

Antibiotic‐Derived Radiotracers for Positron Emission Tomography: Nuclear or “Unclear” Infection Imaging?

Angewandte Chemie, Volume 134, Issue 45, November 7, 2022., 2022
This Review provides summary and critical evaluation, including the challenges and pitfalls, of antibiotic‐derived positron emission tomographic radiopharmaceutical development efforts aimed at infection imaging either considered for radiotracer development for infection imaging or radio‐antibiotic PET imaging supplementing other tools for ...
Arno Christiaan Gouws, Hendrik Gerhardus Kruger, Olivier Gheysens, Jan Rijn Zeevaart, Thavendran Govender, Tricia Naicker, Thomas Ebenhan   +6 more
wiley   +1 more source

A new class of antimycobacterial drugs: the diarylquinolines [PDF]

Thorax, 2005
▴ Andries K, Verhasselt P, Guillemont J, et al . A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science2005;307:223–7 [OpenUrl][1][Abstract/FREE Full Text][2] Over three million people die from tuberculosis (TB) every year, and drug resistance is an increasing problem.
openaire   +1 more source

Probing the Interaction of the Diarylquinoline TMC207 with Its Target Mycobacterial ATP Synthase [PDF]

PLoS ONE, 2011
Infections with Mycobacterium tuberculosis are substantially increasing on a worldwide scale and new antibiotics are urgently needed to combat concomitantly emerging drug-resistant mycobacterial strains. The diarylquinoline TMC207 is a highly promising drug candidate for treatment of tuberculosis. This compound kills M. tuberculosis by binding to a new
Haagsma, Anna C., Podasca, Ioana, Koul, Anil, Andries, Koen, Guillemont, Jerome, Lill, Holger, Bald, Dirk   +6 more
openaire   +5 more sources

Therapy for Mycobacterium kansasii Infection: Beyond 2018

Frontiers in Microbiology, 2018
The current standard of care therapy for pulmonary Mycobacterium kansasii infection is isoniazid (300 mg/day), rifampin (600 mg/day), and ethambutol (15 mg/kg/day) for 12 months after achieving sputum culture negativity.
Michelle S. DeStefano, Carolyn M. Shoen, Michael H. Cynamon, Michael H. Cynamon   +3 more
doaj   +1 more source