Polyfluorinated scaffolds in drug discovery

F Pertusati, M Serpi, E Pileggi - Fluorine in Life Sciences: Pharmaceuticals …, 2019 - Elsevier
The introduction of fluorine in drug-like compounds is now a well-accepted and very efficient
strategy in drug discovery, encouraged by the extensive synthetic methodologies available …

Blood schizontocidal activity of WR 238605 (Tafenoquine) against Plasmodium cynomolgi and Plasmodium fragile infections in rhesus monkeys

SK Puri, GP Dutta - Acta tropica, 2003 - Elsevier
A new 8-aminoquinoline antimalarial WR 238605 (Tafenoquine), developed initially as a
primaquine alternative for prevention of Plasmodiumvivax relapses was evaluated for blood …

tBu4NCl/K2S2O8 System Induced C‐2 Functionalization of 8‐Aminoquinoline Amides with Primary Alcohols

K Zhang, J Xu, J Xiao, R Zhong… - European Journal of …, 2023 - Wiley Online Library
A metal and light‐free Minisci‐type acylation approach of 8‐aminoquinoline amides with
general primary alcohols was demonstrated under tBu4NCl/K2S2O8 system …

Clinical development of new prophylactic antimalarial drugs after the 5th Amendment to the Declaration of Helsinki

GS Dow, AJ Magill, C Ohrt - Therapeutics and clinical risk …, 2008 - Taylor & Francis
Malaria is of continuing concern in nonimmune traveling populations. Traditionally,
antimalarial drugs have been developed as agents for dual indications (treatment and …

Copper-catalyzed remote CH monofluoromethylation of 8-aminoquinolines with dimethyl phosphonate as reductant

S Han, Q Wu, L Mele, L Ding, J Li, D Zou, Y Wu, Y Wu - Tetrahedron Letters, 2019 - Elsevier
A simple and efficient copper-catalyzed monofluoromethylation of 8-aminoquinolines with 2-
bromo-2-fluoroacetate has been described with HPO (OMe) 2 (dimethyl phosphonate) as …

Effect of Fluorescent Dyes on In Vitro-Differentiated, Late-Stage Plasmodium falciparum Gametocytes

T Gebru, B Mordmüller, J Held - Antimicrobial Agents and …, 2014 - Am Soc Microbiol
Plasmodium falciparum gametocytes are not associated with clinical symptoms, but they are
responsible for transmitting the pathogen to mosquitoes. Therefore, gametocytocidal …

Chloroquine and primaquine: combining old drugs as a new weapon against falciparum malaria?

TJ Egan - Trends in Parasitology, 2006 - cell.com
A recent publication has shown that primaquine, a drug used to clear liver-stage
Plasmodium vivax infection, acts as a chloroquine-resistance reversing agent for …

Efficacy of a 3-day pretravel schedule of tafenoquine for malaria chemoprophylaxis: a network meta-analysis

N Islam, S Wright, CL Lau, SAR Doi… - Journal of Travel …, 2021 - academic.oup.com
Background Chemoprophylaxis with weekly doses of tafenoquine (200 mg/day for 3 days
before departure [loading dose], 200 mg/week during travel and 1-week post-travel …

Novel approaches in antimalarial drug discovery

J Held, A Kreidenweiss… - Expert opinion on drug …, 2013 - Taylor & Francis
Introduction: The development of new antimalarial drugs remains of the utmost importance,
since Plasmodium falciparum has developed resistance against nearly all …

Strategic use of antimalarial drugs that block falciparum malaria parasite transmission to mosquitoes to achieve local malaria elimination

R Abdul-Ghani, JC Beier - Parasitology research, 2014 - Springer
The ultimate aim of malaria chemotherapy is not only to treat symptomatic infection but also
to reduce transmission potential. With the absence of clinically proven vaccines, drug …