Results 11 to 20 of about 1,117 (151)

Comprehensive Assessment of the Safety of a New Antituberculosis Drug from the Diarylquinolines Group

Journal Biomed, 2021
The safety of the new anti-tuberculosis drug Tiozonide was studied by bioinformatics and preclinical methods using laboratory animals and with the participation of healthy volunteers. The absence of toxic effects on the main life support systems of mammals predicted by QSAR models was confi rmed by the results of acute, subchronic and chronic toxicity ...
A. Yu. Savchenko, G. V. Ramenskaya, V. G. Kukes, M. S. Burenkov, B. V. Shilov   +4 more
openaire   +3 more sources

Extrapolation of lung pharmacokinetics of bedaquiline across species using physiologically-based pharmacokinetic modelling. [PDF]

Br J Clin Pharmacol
Aims Bedaquiline (BDQ) is a first‐in‐class diarylquinoline (DARQ) and a potent anti‐tuberculosis drug, vital in combating multi‐drug resistant tuberculosis (TB). Understanding its lung pharmacokinetics (PK) across species is crucial for effective clinical translation.
Karakitsios E, Della Pasqua O, Dokoumetzidis A.   +2 more
europepmc   +2 more sources

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
In this study, different assortments of 2-arylquinolines and 2,6-diarylquinolines have been developed. Recently, we have developed a new series of 6,7-dimethoxy-4-alkoxy-2-arylquinolines as Topoisomerase I (TOP1) inhibitors with potent anticancer ...
Mostafa M. Elbadawi, Wagdy M. Eldehna, Amer Ali Abd El-Hafeez, Warda R. Somaa, Amgad Albohy, Sara T. Al-Rashood, Keli K. Agama, Eslam B. Elkaeed, Pradipta Ghosh, Yves Pommier, Manabu Abe   +10 more
doaj   +2 more sources

The Kinetics of Bedaquiline Diffusion in Tuberculous Cavities Open a Window for the Emergence of Resistance. [PDF]

J Infect Dis
Background Cavitary tuberculosis is difficult to cure and constitutes a site of relapse. Bedaquiline has been a wonder drug in the treatment of multidrug-resistant tuberculosis, but emergence of resistance threatens the sustainability of its success.
Bustion AE, Ernest JP, Kaya F, Silva C, Sarathy J, Blanc L, Imperial M, Gengenbacher M, Xie M, Zimmerman MD, Robertson GT, Weiner D, Via LE, Barry CE, Savic RM, Dartois V.   +15 more
europepmc   +2 more sources

NTM-host matched infection models for the classification of drug efficacy against rapid and slow growing nontuberculous mycobacteria species [PDF]

Scientific Reports
Nontuberculous mycobacteria (NTM) are increasingly recognized as major causes of pulmonary disease worldwide. However, progress in identifying effective clinical treatments is difficult because standardized, high-burden preclinical models that enable ...
Vincent E. Guglielmi, Jason E. Cummings, Nicholas J. Whittel, Erik A. Langland, Richard A. Slayden   +4 more
doaj   +2 more sources

Bedaquiline, pretomanid, linezolid, and moxifloxacin (BPaLM) for multidrug- or rifampin-resistant tuberculosis: a systematic review [PDF]

Jornal Brasileiro de Pneumologia
Objective: To evaluate the available evidence comparing the use of the bedaquiline, pretomanid, linezolid, and moxifloxacin (BPaLM) regimen for 6 months with that of standard-of-care regimens for patients with multidrug-resistant or rifampin-resistant ...
Denise Rossato Silva, Flávia Fonseca Fernandes, Juliana Carvalho Ferreira, Wanderley Bernando, Margareth Maria Pretti Dalcolmo, Fernanda Dockhorn Costa Johansen, Fernanda Carvalho de Queiroz Mello   +6 more
doaj   +2 more sources

Synthesis, anti-tuberculosis activity and QSAR study of 2,4-diarylquinolines and analogous polycyclic derivatives

Arabian Journal of Chemistry, 2019
The multicomponent syntheses of 2,4-di-aryl-quinolines and analogous polycyclic derivatives as anti-tuberculosis agents were described. They were prepared via Beyer and Friedlander methods under microwave irradiation in short reaction times and good ...
Gisela C Muscia, Graciela Y Buldain, Juan J Casal   +2 more
exaly   +2 more sources

Bioenergetics of Mycobacterium: An Emerging Landscape for Drug Discovery

Pathogens, 2018
Mycobacterium tuberculosis (Mtb) exhibits remarkable metabolic flexibility that enables it to survive a plethora of host environments during its life cycle.
Iram Khan Iqbal, Sapna Bajeli, Ajit Kumar Akela, Ashwani Kumar   +3 more
doaj   +2 more sources

6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

ACS Medicinal Chemistry Letters, 2017
Bedaquiline (1) is a new drug for tuberculosis and the first of the diarylquinoline class. It demonstrates excellent efficacy against TB but induces phospholipidosis at high doses, has a long terminal elimination half-life (due to its high lipophilicity), and exhibits potent hERG channel inhibition, resulting in clinical QTc interval prolongation.
Amy S. T. Tong, Peter J. Choi, Adrian Blaser, Hamish S. Sutherland, Sophia K. Y. Tsang, Jerome Guillemont, Magali Motte, Christopher B. Cooper, Koen Andries, Walter Van den Broeck, Scott G. Franzblau, Anna M. Upton, William A. Denny, Brian D. Palmer, Daniel Conole   +14 more
openaire   +4 more sources

Exploring novel antitubercular agents: Innovative design of 2,3-diaryl-quinoxalines targeting DprE1 for effective tuberculosis treatment

Open Chemistry
The rising instances of drug resistance in Mycobacterium tuberculosis strains pose a significant global health challenge. Conventional tuberculosis (TB) treatments, which typically involve multiple antibiotics, face hurdles like drug resistance, reduced ...
Sharma Kirti, Sharma Atul, Sanduja Mohit, Jogpal Vikas, Mishra Asim Kumar, Kumar Girish, Virmani Tarun, Noman Omar M., Alhalmi Abdulsalam   +8 more
doaj   +2 more sources