Targeting mycobacterial membranes and membrane proteins: Progress and limitations

G Kumar, S Kapoor - Bioorganic & medicinal chemistry, 2023 - Elsevier
Among the various bacterial infections, tuberculosis continues to hold center stage. Its
causative agent, Mycobacterium tuberculosis, possesses robust defense mechanisms …

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 …

The anti-mycobacterial activity of the cytochrome bcc inhibitor Q203 can be enhanced by small-molecule inhibition of cytochrome bd

P Lu, AH Asseri, M Kremer, J Maaskant, R Ummels… - Scientific reports, 2018 - nature.com
Mycobacterial energy metabolism currently attracts strong attention as new target space for
development of anti-tuberculosis drugs. The imidazopyridine Q203 targets the cytochrome …

Quinoline: an attractive scaffold in drug design

LFE Moor, TRA Vasconcelos… - Mini Reviews in …, 2021 - benthamdirect.com
Quinoline and its derivatives comprise an important group of heterocyclic compounds that
exhibits a wide range of pharmacological properties such as antibacterial, antiviral …

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 …

Small organic molecules targeting the energy metabolism of Mycobacterium tuberculosis

M Urban, V Šlachtová, L Brulikova - European Journal of Medicinal …, 2021 - Elsevier
Causing approximately 10 million incident cases and 1.3–1.5 million deaths every year,
Mycobacterium tuberculosis remains a global health problem. The risk is further …

Arylvinylpiperazine amides, a new class of potent inhibitors targeting QcrB of Mycobacterium tuberculosis

CS Foo, A Lupien, M Kienle, A Vocat, A Benjak… - MBio, 2018 - Am Soc Microbiol
New drugs are needed to control the current tuberculosis (TB) pandemic caused by infection
with Mycobacterium tuberculosis. We report here on our work with AX-35, an …

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 …

An open-access dashboard to interrogate the genetic diversity of Mycobacterium tuberculosis clinical isolates

J Phelan, K Van den Heede, S Masyn, R Verbeeck… - Scientific reports, 2024 - nature.com
Tuberculosis (TB) remains one of the leading infectious disease killers in the world. The
ongoing development of novel anti-TB medications has yielded potent compounds that often …

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 …