Results 41 to 50 of about 1,117 (151)

Early Bactericidal Activity and Pharmacokinetics of the Diarylquinoline TMC207 in Treatment of Pulmonary Tuberculosis [PDF]

Antimicrobial Agents and Chemotherapy, 2008
ABSTRACT Tibotec Medicinal Compound 207 (TMC207) is a novel diarylquinoline with a unique mode of action that targets mycobacterial ATP synthase. TMC207 exhibits high in vitro activity against mycobacterial strains either susceptible or resistant to all first-line and many second-line drugs, including fluoroquinolones, and has ...
R, Rustomjee, A H, Diacon, J, Allen, A, Venter, C, Reddy, R F, Patientia, T C P, Mthiyane, T, De Marez, R, van Heeswijk, R, Kerstens, A, Koul, K, De Beule, P R, Donald, D F, McNeeley   +13 more
openaire   +2 more sources

New treatment options for multidrug-resistant tuberculosis

Therapeutic Advances in Respiratory Disease, 2012
Despite the development of effective treatments, tuberculosis (TB) remains a major health problem. TB continues to infect new victims and kills nearly 2 million people annually.
Stephen K. Field, Dina Fisher, Julie M. Jarand, Robert L. Cowie   +3 more
doaj   +1 more source

Cytotoxicity and Antimicrobial Activity of GaMF1 Analogs

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
GaMF1 is a reported, highly potent inhibitor of mycobacterial ATP synthase. Structural modification of this scaffold significantly changes biological activity. We present GaMF1 analogues with strong antiparasitic effects, potential antiproliferative properties, and discuss the selectivity limitations of the parent compound and its analogues.
Jan Chasák, Petr Vyvlečka, Ivan Nemec, An Matheeussen, Natascha Van Pelt, Paul Cos, Guy Caljon, Vladimír Kryštof, Lucie Brulíková   +8 more
wiley   +1 more source

Discovery of 1,3,4‐Oxadiazin‐5‐One Derivative CJ1‐34 as a Partial ATP Synthase Inhibitor for CNS Applications

Chemistry – A European Journal, Volume 31, Issue 24, April 25, 2025.
Novel structural scaffolds for targeting ATP synthase with appropriate properties to cross blood‐brain barrier were designed, synthesised, and evaluated by in vitro assays. CJ1‐34 was identified as a partial ATP synthase inhibitor with a determined IC50 of 394 nM in isolated bovine mitochondria, which can be further explored as a potential CNS drug for
Caitlin V. M. L. Jie, Aro Delparente, Lisa Reichert, Manuela Albrecht, Kenneth Atz, Gisbert Schneider, Roger Schibli, Linjing Mu   +7 more
wiley   +1 more source

Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research

Angewandte Chemie International Edition, Volume 64, Issue 10, March 3, 2025.
This article provides an overview over antibacterial drugs investigated in the past three decades. Aspects of the compound's origins, their cellular targets, the antibacterial spectrum and proof‐of‐concept in animal studies are covered and current trends are highlighted.
Roderich D. Süssmuth, Marcel Kulike‐Koczula, Peng Gao, Simone Kosol   +3 more
wiley   +1 more source

Metal free synthesis of 2,4-diarylquinoline derivatives with enamides and imines

RSC Advances, 2015
A simple and efficient way to construct quinoline derivatives using enamides and imines in metal free condition.
Yamin Li, Xiaoqiang Zhou, Zhaoyang Wu, Jinhui Cao, Chaowei Ma, Yongqin He, Guosheng Huang   +6 more
openaire   +2 more sources

Tuberculosis: An Update for the Clinician

Respirology, Volume 30, Issue 3, Page 196-205, March 2025.
ABSTRACT Tuberculosis (TB) remains a significant global health threat with high mortality and efforts to meet WHO End TB Strategy milestones are off‐track. It has become clear that TB is not a dichotomous infection with latent and active forms but presents along a disease spectrum.
Saskia Janssen, Melissa Murphy, Caryn Upton, Brian Allwood, Andreas H. Diacon   +4 more
wiley   +1 more source

Novel Pharmacological Approaches for Multidrug‐Resistant Tuberculosis: Review

Advances in Pharmacological and Pharmaceutical Sciences, Volume 2025, Issue 1, 2025.
Background Due to its resistance to common anti‐TB drugs, multidrug‐resistant tuberculosis (MDR‐TB) presents substantial treatment problems. Optimizing therapeutic outcomes requires individualized treatment plans that take into account patient comorbidities, medication susceptibility profiles, and past treatment history.
Kassahun Dires Ayenew, Habtemariam Alekaw Habteweld, Abate Wondesen Tsige, Yihenew Sewale Bizu, Koteshwara Mudigonda   +4 more
wiley   +1 more source

Unraveling Drug Resistance in Mycobacterium leprae: Exploring Genetic Mutations to Enhance Treatment Strategies for Human Leprosy—A Narrative Review

International Journal of Microbiology, Volume 2025, Issue 1, 2025.
Leprosy, one of the oldest diseases, is caused by Mycobacterium leprae and Mycobacterium lepromatosis and continues to pose a significant global public health challenge despite decades of control efforts and the widespread use of multidrug therapy. Clinical manifestations range from tuberculoid to severe lepromatous forms, often accompanied by immune ...
Gayathri Perera, Maheshi Thilakarathna, Ishani Aluthgamage, Sakuni Sathsarani, Pasan C. Fernando, Sharini Samaranayake, Nazif Ullah, Bhagya Deepachandi, Abdelwahab Omri   +8 more
wiley   +1 more source

One-Pot Synthesis of 2,3,4-Triarylquinolines via Suzuki-Miyaura Cross-Coupling of 2-Aryl-4-chloro-3-iodoquinolines with Arylboronic Acids

Molecules, 2010
Palladium–catalyzed Suzuki cross-coupling of 2-aryl-4-chloro-3-iodoquinolines with excess arylboronic acids (2.5 equiv.) in the presence of tricyclohexylphosphine afforded the 2,3,4-triarylquinolines in one-pot operation.
Malose Jack Mphahlele, Mamasegare Mabel Mphahlele   +1 more
doaj