Tuberculosis drug discovery: challenges and new horizons

GFS Fernandes, AM Thompson… - Journal of Medicinal …, 2022 - ACS Publications
Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious
disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to …

Pyrimidine derivatives with antitubercular activity

V Finger, M Kufa, O Soukup, D Castagnolo… - European Journal of …, 2023 - Elsevier
Small molecules with antitubercular activity containing the pyrimidine motif in their structure
have gained more attention after three drugs, namely GSK 2556286 (GSK-286), TBA-7371 …

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis

K Pethe, P Bifani, J Jang, S Kang, S Park, S Ahn… - Nature medicine, 2013 - nature.com
New therapeutic strategies are needed to combat the tuberculosis pandemic and the spread
of multidrug-resistant (MDR) and extensively drug-resistant (XDR) forms of the disease …

Fueling open‐source drug discovery: 177 small‐molecule leads against tuberculosis

L Ballell, RH Bates, RJ Young… - …, 2013 - Wiley Online Library
With the aim of fuelling open‐source, translational, early‐stage drug discovery activities, the
results of the recently completed antimycobacterial phenotypic screening campaign against …

Lansoprazole is an antituberculous prodrug targeting cytochrome bc1

J Rybniker, A Vocat, C Sala, P Busso, F Pojer… - Nature …, 2015 - nature.com
Better antibiotics capable of killing multi-drug-resistant Mycobacterium tuberculosis are
urgently needed. Despite extensive drug discovery efforts, only a few promising candidates …

Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H) …

X Li, V Hernandez, FL Rock, W Choi… - Journal of medicinal …, 2017 - ACS Publications
There is an urgent need to develop new and safer antitubercular agents that possess a
novel mode of action. We synthesized and evaluated a novel series of 3-aminomethyl 4 …

Recent developments of imidazo [1, 2-a] pyridine analogues as antituberculosis agents

S Samanta, S Kumar, EK Aratikatla… - RSC Medicinal …, 2023 - pubs.rsc.org
Over the past 2000 years, tuberculosis (TB) has killed more people than any other infectious
disease. In 2021, TB claimed 1.6 million lives worldwide, making it the second leading …

Identification of Novel Imidazo[1,2-a]pyridine Inhibitors Targeting M. tuberculosis QcrB

KA Abrahams, JAG Cox, VL Spivey, NJ Loman… - PloS one, 2012 - journals.plos.org
Mycobacterium tuberculosis is a major human pathogen and the causative agent for the
pulmonary disease, tuberculosis (TB). Current treatment programs to combat TB are under …

Discovery of novel oral protein synthesis inhibitors of Mycobacterium tuberculosis that target leucyl-tRNA synthetase

A Palencia, X Li, W Bu, W Choi, CZ Ding… - Antimicrobial agents …, 2016 - Am Soc Microbiol
The recent development and spread of extensively drug-resistant and totally drug-resistant
resistant (TDR) strains of Mycobacterium tuberculosis highlight the need for new …

A genetic strategy to identify targets for the development of drugs that prevent bacterial persistence

JH Kim, KM O'Brien, R Sharma… - Proceedings of the …, 2013 - National Acad Sciences
Antibacterial drug development suffers from a paucity of targets whose inhibition kills
replicating and nonreplicating bacteria. The latter include phenotypically dormant cells …