https://pubs.rsc.org/en/content/articlepdf/2019/NP/C8NP00092A

Marine natural products.

The incidence of tuberculosis has been increasing substantially on a worldwide basis over the past decade, but no tuberculosis-specific drugs have been discovered in 40 years. We identified a diarylquinoline, R207910, that potently inhibits both drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro (minimum inhibitory concentration 0.06 μg/ml). In mice, R207910 exceeded the bactericidal activities of isoniazid and rifampin by at least 1 log unit. Substitution of drugs included in the World Health Organization's first-line tuberculosis treatment regimen (rifampin, isoniazid, and pyrazinamide) with R207910 accelerated bactericidal activity, leading to complete culture conversion after 2 months of treatment in some combinations. A single dose of R207910 inhibited mycobacterial growth for 1 week. Plasma levels associated with efficacy in mice were well tolerated in healthy human volunteers. Mutants selected in vitro suggest that the drug targets the proton pump of adenosine triphosphate (ATP) synthase.

https://science.sciencemag.org/content/sci/307/5707/223.full.pdf

A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.

Advances in the chemistry of tetrahydroquinolines.

Quinolines and structurally related heterocycles as antimalarials

Antituberculosis drugs: ten years of research.

Antimalarials from nature

Ring-substituted quinolines as potential anti-tuberculosis agents.

Malaria caused by protozoa of the genus Plasmodium, because of its prevalence, virulence, and drug resistance, is the most serious and widespread parasitic disease encountered by mankind. The inadequate armory of drugs in widespread use for the treatment of malaria, development of strains resistant to commonly used drugs such as chloroquine, and the lack of affordable new drugs are the limiting factors in the fight against malaria. These factors underscore the continuing need of research for new classes of antimalarial agents, and a re-examination of the existing antimalarial drugs that may be effective against resistant strains. This review provides an in-depth look at the most significant progress made during the past 10 years in antimalarial drug development.

Meenakshi Jain

Papers

Quinolines and structurally related heterocycles as antimalarials

Antimalarials from nature

Ring-substituted quinolines as potential anti-tuberculosis agents.

Recent advances in antimalarial drug development

Synthesis, antimalarial, antileishmanial, and antimicrobial activities of some 8-quinolinamine analogues