Oxidative Phosphorylation—an Update on a New, Essential Target Space for Drug Discovery in Mycobacterium tuberculosis

CSY Foo, K Pethe, A Lupien - Applied Sciences, 2020 - mdpi.com
New drugs with new mechanisms of action are urgently required to tackle the global
tuberculosis epidemic. Following the FDA-approval of the ATP synthase inhibitor …

Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease

CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …

Design, synthesis, and antifungal evaluation of novel quinoline derivatives inspired from natural quinine alkaloids

GZ Yang, JK Zhu, XD Yin, YF Yan… - Journal of agricultural …, 2019 - ACS Publications
Inspired by quinine and its analogues, we designed, synthesized, and evaluated two series
of quinoline small molecular compounds (a and 2a) and six series of quinoline derivatives …

Novel 4-aminoquinolines: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase, antitubercular activity, SAR, and preclinical …

JD Paz, ND de Moura Sperotto, AS Ramos… - European Journal of …, 2023 - Elsevier
Herein a series of 4-aminoquinolines were synthesized in an attempt to optimize and study
the structural features related to LABIO-17 biological activity, a Mycobacterium tuberculosis …

Discovery of novel 2-(trifluoromethyl) quinolin-4-amine derivatives as potent antitumor agents with microtubule polymerization inhibitory activity

K Liu, M Mo, G Yu, J Yu, S Song, S Cheng, H Li… - Bioorganic …, 2023 - Elsevier
In this work, a series of 2-(trifluoromethyl) quinolin-4-amine derivatives were designed and
synthesized through structural optimization strategy as a microtubule-targeted agents …

Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy) acetamide-based antituberculosis agents

AF Borsoi, JD Paz, BL Abbadi, FS Macchi… - European Journal of …, 2020 - Elsevier
Using a classical molecular simplification approach, a series of 36 quinolines were
synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (M …

Advances in drug discovery of new antitubercular multidrug-resistant compounds

GFS Fernandes, C Man Chin, JL Dos Santos - Pharmaceuticals, 2017 - mdpi.com
Tuberculosis (TB), a disease caused mainly by the Mycobacterium tuberculosis (Mtb), is
according to the World Health Organization (WHO) the infectious disease responsible for the …

Terminal respiratory oxidases: a targetables vulnerability of mycobacterial bioenergetics?

S Bajeli, N Baid, M Kaur, GP Pawar… - Frontiers in cellular …, 2020 - frontiersin.org
Recently, ATP synthase inhibitor Bedaquiline was approved for the treatment of multi-drug
resistant tuberculosis emphasizing the importance of oxidative phosphorylation for the …

Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors of Mycobacterium tuberculosis. Structural correction of reported N-(6-(2 …

PJ Choi, GL Lu, HS Sutherland, AC Giddens… - Tetrahedron …, 2022 - Elsevier
During our studies into preparing analogues of pyrazolopyrimidine as ATP synthesis
inhibitors of Mycobacterium tuberculosis, a regiospecific condensation reaction between …

Antitubercular activity of novel 2-(quinoline-4-yloxy) acetamides with improved drug-like properties

AF Borsoi, LM Alice, N Sperotto… - ACS Medicinal …, 2022 - ACS Publications
Using cycloalkyl and electron-donating groups to decrease the carbonyl electrophilicity, a
novel series of 2-(quinoline-4-yloxy) acetamides was synthesized and evaluated as in vitro …