Quinolone: a versatile therapeutic compound class

PS Dube, LJ Legoabe, RM Beteck - Molecular Diversity, 2023 - Springer
The discovery of nalidixic acid is one pinnacle in medicinal chemistry, which opened a new
area of research that has led to the discovery of several life-saving antimicrobial agents …

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 …

Comparing and Validating Machine Learning Models for Mycobacterium tuberculosis Drug Discovery

T Lane, DP Russo, KM Zorn, AM Clark… - Molecular …, 2018 - ACS Publications
Tuberculosis is a global health dilemma. In 2016, the WHO reported 10.4 million incidences
and 1.7 million deaths. The need to develop new treatments for those infected with …

The present state of the tuberculosis drug development pipeline

MDJ Libardo, HIM Boshoff, CE Barry III - Current opinion in pharmacology, 2018 - Elsevier
Tuberculosis now ranks as the leading cause of death in the world due to a single infectious
agent. Current standard of care treatment can achieve very high cure rates for drug-sensitive …

Identification of 2-aryl-quinolone inhibitors of cytochrome bd and chemical validation of combination strategies for respiratory inhibitors against Mycobacterium …

LN Jeffreys, A Ardrey, TA Hafiz, LA Dyer… - ACS Infectious …, 2023 - ACS Publications
Mycobacterium tuberculosis cytochrome bd quinol oxidase (cyt bd), the alternative terminal
oxidase of the respiratory chain, has been identified as playing a key role during chronic …

Bioenergetic Inhibitors: Antibiotic Efficacy and Mechanisms of Action in Mycobacterium tuberculosis

EJ Hasenoehrl, TJ Wiggins, M Berney - Frontiers in cellular and …, 2021 - frontiersin.org
Development of novel anti-tuberculosis combination regimens that increase efficacy and
reduce treatment timelines will improve patient compliance, limit side-effects, reduce costs …

Recent advancements and developments in search of anti-tuberculosis agents: a quinquennial update and future directions

TM Dhameliya, KA Bhakhar, ND Gajjar, KA Patel… - Journal of Molecular …, 2022 - Elsevier
Tuberculosis (TB) has been considered as the highly chronic, contagious and infectious
disorder caused by Mycobacterium tuberculosis (Mtb). Every year more than 10 million …

Plasticity of Mycobacterium tuberculosis NADH dehydrogenases and their role in virulence

C Vilchèze, B Weinrick, LW Leung… - Proceedings of the …, 2018 - National Acad Sciences
Worldwide control of the tuberculosis (TB) epidemic has not been achieved, and the latest
statistics show that the TB problem might be more endemic than previously thought …

Tricyclic SpiroLactams kill mycobacteria in vitro and in vivo by inhibiting type II NADH dehydrogenases

S Dam, S Tangara, C Hamela, T Hattabi… - Journal of Medicinal …, 2022 - ACS Publications
It is critical that novel classes of antituberculosis drugs are developed to combat the
increasing burden of infections by multidrug-resistant strains. To identify such a novel class …

Bioenergetics of Mycobacterium: An Emerging Landscape for Drug Discovery

IK Iqbal, S Bajeli, AK Akela, A Kumar - Pathogens, 2018 - mdpi.com
Mycobacterium tuberculosis (Mtb) exhibits remarkable metabolic flexibility that enables it to
survive a plethora of host environments during its life cycle. With the advent of bedaquiline …