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 …

Overview of recent strategic advances in medicinal chemistry

G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …

Identification of hydantoin based Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) inhibitors as antimycobacterial agents using computational tools

SN Mali, A Pandey, RR Bhandare, AB Shaik - Scientific reports, 2022 - nature.com
Tuberculosis (TB) is one of the emerging infectious diseases in the world. DprE1 (
Decaprenylphosphoryl-β-d-ribose 2′-epimerase), an enzyme accountable for …

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 …

Tuberculosis drug discovery: A decade of hit assessment for defined targets

S Oh, L Trifonov, VD Yadav, CE Barry III… - Frontiers in Cellular …, 2021 - frontiersin.org
More than two decades have elapsed since the publication of the first genome sequence of
Mycobacterium tuberculosis (Mtb) which, shortly thereafter, enabled methods to determine …

In Silico Development of Novel Benzofuran-1,3,4-Oxadiazoles as Lead Inhibitors of M. tuberculosis Polyketide Synthase 13

A Irfan, S Faisal, AF Zahoor, R Noreen, SA Al-Hussain… - Pharmaceuticals, 2023 - mdpi.com
Benzofuran and 1, 3, 4-oxadiazole are privileged and versatile heterocyclic
pharmacophores which display a broad spectrum of biological and pharmacological …

Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs

SR Green, SH Davis, S Damerow, CA Engelhart… - Nature …, 2022 - nature.com
Tuberculosis is a major global cause of both mortality and financial burden mainly in low
and middle-income countries. Given the significant and ongoing rise of drug-resistant strains …

Promiscuous targets for antitubercular drug discovery: The paradigm of DprE1 and MmpL3

G Degiacomi, JM Belardinelli, MR Pasca, E De Rossi… - Applied Sciences, 2020 - mdpi.com
The development and spread of Mycobacterium tuberculosis multi-drug resistant strains still
represent a great global health threat, leading to an urgent need for novel anti-tuberculosis …

DprE1 inhibitors: enduring aspirations for future antituberculosis drug discovery

S Yadav, A Soni, O Tanwar, R Bhadane… - …, 2023 - Wiley Online Library
DprE1 is a crucial enzyme involved in the cell wall synthesis of Mycobacterium tuberculosis
and a promising target for antituberculosis drug development. However, its unique structural …

Identification of β-Lactams Active against Mycobacterium tuberculosis by a Consortium of Pharmaceutical Companies and Academic Institutions

B Gold, J Zhang, LL Quezada, J Roberts… - ACS infectious …, 2022 - ACS Publications
Rising antimicrobial resistance challenges our ability to combat bacterial infections. The
problem is acute for tuberculosis (TB), the leading cause of death from infection before …