Results 121 to 130 of about 1,117 (151)

A Diarylquinoline Drug Active on the ATP Synthase of Mycobacterium tuberculosis

Science, 2005
The incidence of tuberculosis has been increasing substantially on a worldwide basis over the past decade, but no tuberculosis-specific drugs have been discovered in 40 years. We identified a diarylquinoline, R207910, that potently inhibits both drug-sensitive and drug-resistant Mycobacterium tuberculosis
Koen, Andries, Peter, Verhasselt, Jerome, Guillemont, Hinrich W H, Göhlmann, Jean-Marc, Neefs, Hans, Winkler, Jef, Van Gestel, Philip, Timmerman, Min, Zhu, Ennis, Lee, Peter, Williams, Didier, de Chaffoy, Emma, Huitric, Sven, Hoffner, Emmanuelle, Cambau, Chantal, Truffot-Pernot, Nacer, Lounis, Vincent, Jarlier   +17 more
openaire   +2 more sources

Ionic Liquid and Sc(OTf)3 as a Sustainable Combo for Photochemical One‐Pot Aza‐Diels‐Alder Reaction to Access 2,4‐Diarylquinolines

ChemistrySelect
A sustainable photochemical methodology has been developed to synthesize biologically active 2,4‐diarylquinolines by aza‐Diels‐Alder reaction (Povarov reaction) using [BMIM][BF4] and Sc(OTf)3 under organic solvent‐free conditions.
B. Bala, Shivasankar Krishnamoorthy, M. Meyyappan, M. Vinothkumar, B. Sridhar, Ramesh L Gardas, G. Sekar   +6 more
semanticscholar   +1 more source

Bedaquiline

Annals of Pharmacotherapy, 2013
Objective: To review the chemistry, pharmacology, microbiology, pharmacokinetics, pharmacodynamics, clinical efficacy, safety, dosage, and administration of bedaquiline, a novel oral diarylquinoline antimycobacterial agent approved by the Food and Drug Administration for the treatment of adults with pulmonary multidrug-resistant tuberculosis (MDR-TB ...
Chahine, Elias B., Karaoui, Lamis R., Mansour, Hanine   +2 more
openaire   +3 more sources

Uncatalyzed and Solvent‐Free Process for the Synthesis of 1,4‐Diarylquinoline Derivatives

Synthetic Communications, 2008
Abstract The uncatalyzed and three‐component reaction of arylaldehyde, malonodinitrile, and 3‐arylamino‐5,5‐dimethylcyclohex‐2‐enone at 160 °C under solvent‐free conditions gave 1,4‐diarylquinoline derivatives in high yields.
Xiang‐Shan Wang, Mei‐Mei Zhang, Hong Jiang, Chang‐Sheng Yao, Shu‐Jiang Tu   +4 more
openaire   +1 more source

p -TSA·H 2 O-Catalyzed Synthesis of 2,3-Diarylquinoline Derivatives via One-Pot Three-Component Reaction

Synthesis, 2023
An environmentally benign synthesis of 2,3-diarylquinolines is reported via a one-pot three-component reaction from arylamines, benzaldehyde, and styrene oxide in the presence of 20 mol% p-TSA·H2O at 120 °C. This protocol does not require metal catalysts,
Simra Faraz, A. Khan
semanticscholar   +1 more source

An explorative study on diarylquinoline-based inhibitor targeting Enterococcus faecium MurF

Structural Chemistry, 2020
Enterococcus faecium MurF (EfMurF) enzyme catalyzes the addition of d-alanyl-d-alanine to form murein UDP-N-acetylmuramoyl-pentapeptide. This is the last cytoplasmic step of peptidoglycan synthesis and is essential for bacterial cell wall integrity.
Mohammed Afzal Azam, Vyshaag Chembakam veetil Manoj   +1 more
openaire   +1 more source

Bactericidal activity of the diarylquinoline TMC207 against Mycobacterium tuberculosis outside and within cells

Tuberculosis, 2010
The bactericidal activities of the diarylquinoline TMC207 in a liquid culture medium started with a bacteriostatic phase lasting about 7 days and then continued with a dose-related bactericidal phase. In comparison, its intra-cellular activity in primary mouse peritoneal macrophages (PM) and in the J774 macrophage-like cell line had little or no static
Dhillon, Jasvir, Andries, Koen, Philips, Patrick, Mitchison, Denis A.   +3 more
openaire   +3 more sources

A Clean Synthesis of 1,4‐Diarylquinoline Derivatives Catalyzed by TEBAC in Aqueous Media

Journal of the Chinese Chemical Society, 2007
AbstractA series of 1,4‐diarylquinoline derivatives were synthesized by the reaction of arylmethylidenemalononitriles or 2‐cyano‐3‐aryl‐1‐acrylate and 3‐arylamino‐5,5‐dimethylcyclohex‐2‐enone in aqueous media at 100 °C catalyzed by TEBAC. Meanwhile, the water medium was chosen as green solvent.
Xiang‐Shan Wang, Mei‐Mei Zhang, Hong Jiang, Da‐Qing Shi, Shu‐Jiang Tu   +4 more
openaire   +1 more source

Environmentally benign synthesis of 2,4-diarylquinolines under metal- & solvent-free conditions

Tetrahedron Letters, 2023
Simra Faraz, Sabina Yashmin, Mayura Dilip Marathe, Abu Taleb Khan   +3 more
semanticscholar   +1 more source

Ion mobility-mass spectrometry analysis of diarylquinoline diastereomers: Drugs used for tuberculosis treatment

European Journal of Mass Spectrometry, 2018
Mycobacterium tuberculosis infection results in more than two million deaths per year and is the leading cause of mortality in people infected with HIV. A new structural class of antimycobacterials, the diarylquinolines, has been synthesized and is being highly effective against both M. tuberculosis and multidrug-resistant tuberculosis.
Domalain, Virginie, Hubert-Roux, Marie, Quéguiner, Laurence, Jeanne Dit Fouque, Dany, Arnoult, Eric, Speybrouck, David, Guillemont, Jérôme, Afonso, Carlos   +7 more
openaire   +3 more sources