Biological activity of oxadiazole and thiadiazole derivatives

UA Atmaram, SM Roopan - Applied Microbiology and Biotechnology, 2022 - Springer
The 5-membered oxadiazole and thiadiazole scaffolds are the most privileged and well-
known heterocycles, being a common and essential feature of a variety of natural products …

Mycobacterial cell wall biosynthesis: a multifaceted antibiotic target

KA Abrahams, GS Besra - Parasitology, 2018 - cambridge.org
Mycobacterium tuberculosis (Mtb), the etiological agent of tuberculosis (TB), is recognized
as a global health emergency as promoted by the World Health Organization. Over 1 million …

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 …

DprE2 is a molecular target of the anti-tubercular nitroimidazole compounds pretomanid and delamanid

KA Abrahams, SM Batt, SS Gurcha, N Veerapen… - Nature …, 2023 - nature.com
Mycobacterium tuberculosis is one of the global leading causes of death due to a single
infectious agent. Pretomanid and delamanid are new antitubercular agents that have …

Drug discovery in tuberculosis. New drug targets and antimycobacterial agents

A Campaniço, R Moreira, F Lopes - European journal of medicinal …, 2018 - Elsevier
Tuberculosis (TB) remains a major health problem worldwide. The infectious agent,
Mycobacterium tuberculosis, has a unique ability to survive within the host, alternating …

Overview of the development of DprE1 inhibitors for combating the menace of tuberculosis

RV Chikhale, MA Barmade, PR Murumkar… - Journal of medicinal …, 2018 - ACS Publications
Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), a vital enzyme for cell wall
synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It …

Recent Advances of DprE1 Inhibitors against Mycobacterium tuberculosis: Computational Analysis of Physicochemical and ADMET Properties

PSM Amado, C Woodley, MLS Cristiano, PM O'Neill - ACS omega, 2022 - ACS Publications
Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) is a critical flavoenzyme in
Mycobacterium tuberculosis, catalyzing a vital step in the production of lipoarabinomannan …

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 …

High-throughput screening for the discovery of enzyme inhibitors

MD Lloyd - Journal of Medicinal Chemistry, 2020 - ACS Publications
Enzymes are common targets in high-throughput screening and related campaigns. An
analysis of papers published between 1990 and 2018 showed that kinases were the most …

N-methylation of a bactericidal compound as a resistance mechanism in Mycobacterium tuberculosis

T Warrier, K Kapilashrami, A Argyrou… - Proceedings of the …, 2016 - National Acad Sciences
The rising incidence of antimicrobial resistance (AMR) makes it imperative to understand the
underlying mechanisms. Mycobacterium tuberculosis (Mtb) is the single leading cause of …