Recent advances of imidazole-containing derivatives as anti-tubercular agents

YL Fan, XH Jin, ZP Huang, HF Yu, ZG Zeng… - European journal of …, 2018 - Elsevier
Tuberculosis still remains one of the most common, communicable, and leading deadliest
diseases known to mankind throughout the world. Drug-resistance in Mycobacterium …

Hit generation in TB drug discovery: from genome to granuloma

T Yuan, NS Sampson - Chemical reviews, 2018 - ACS Publications
Current tuberculosis (TB) drug development efforts are not sufficient to end the global TB
epidemic. Recent efforts have focused on the development of whole-cell screening assays …

Lead Optimization of a Novel Series of Imidazo[1,2-a]pyridine Amides Leading to a Clinical Candidate (Q203) as a Multi- and Extensively-Drug-Resistant Anti …

S Kang, RY Kim, MJ Seo, S Lee, YM Kim… - Journal of medicinal …, 2014 - ACS Publications
A critical unmet clinical need to combat the global tuberculosis epidemic is the development
of potent agents capable of reducing the time of multi-drug-resistant (MDR) and extensively …

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 …

[HTML][HTML] Application of Mycobacterium smegmatis as a surrogate to evaluate drug leads against Mycobacterium tuberculosis

N Lelovic, K Mitachi, J Yang, MR Lemieux, Y Ji… - The Journal of …, 2020 - nature.com
Discovery of new anti-tuberculosis (TB) drugs is a time-consuming process due to the slow-
growing nature of Mycobacterium tuberculosis (Mtb). A requirement of biosafety level 3 (BSL …

Advancement of Imidazo[1,2-a]pyridines with Improved Pharmacokinetics and nM Activity vs. Mycobacterium tuberculosis

GC Moraski, LD Markley, J Cramer… - ACS medicinal …, 2013 - ACS Publications
A set of 14 imidazo [1, 2-a] pyridine-3-carboxamides was synthesized and screened against
Mycobacterium tuberculosis H37Rv. The minimum inhibitory concentrations of 12 of these …

Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

R van der Westhuyzen, S Winks… - Journal of Medicinal …, 2015 - ACS Publications
High-throughput screening of a library of small polar molecules against Mycobacterium
tuberculosis led to the identification of a phthalimide-containing ester hit compound (1) …

Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents

J Tang, B Wang, T Wu, J Wan, Z Tu… - ACS Medicinal …, 2015 - ACS Publications
A series of pyrazolo [1, 5-a] pyridine-3-carboxamide derivatives were designed and
synthesized as new anti-Mycobacterium tuberculosis (Mtb) agents. The compounds exhibit …

Hybrid imidazole (benzimidazole)/pyridine (quinoline) derivatives and evaluation of their anticancer and antimycobacterial activity

D Mantu, V Antoci, C Moldoveanu… - Journal of enzyme …, 2016 - Taylor & Francis
The design, synthesis, structure, and in vitro anticancer and antimycobacterial activity of new
hybrid imidazole (benzimidazole)/pyridine (quinoline) derivatives are described. The …

Arrival of Imidazo[2,1-b]thiazole-5-carboxamides: Potent Anti-tuberculosis Agents That Target QcrB

GC Moraski, N Seeger, PA Miller, AG Oliver… - ACS Infectious …, 2016 - ACS Publications
Increasing interest in the potent anti-tuberculosis activity and the novel target (QcrB) of
imidazo [1, 2-a] pyridine-3-carboxamides encouraged extended structure–activity …