4-Thiophenoxy-2-trichloromethyquinazolines display in vitro selective antiplasmodial activity against the human malaria parasite Plasmodium falciparum

P Verhaeghe, A Dumètre, C Castera-Ducros… - Bioorganic & medicinal …, 2011 - Elsevier
A series of original quinazolines bearing a 4-thiophenoxy and a 2-trichloromethyl group was
synthesized in a convenient and efficient way and was evaluated toward its in vitro …

Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria

RT Skerlj, CM Bastos, ML Booker… - ACS medicinal …, 2011 - ACS Publications
Inhibition of dihydroorotate dehydrogenase (DHODH) for P. falciparum potentially
represents a new treatment option for malaria, since DHODH catalyzes the rate-limiting step …

4-Aminoquinolines: chloroquine, amodiaquine and next-generation analogues

PM O'Neill, VE Barton, SA Ward, J Chadwick - Treatment and Prevention …, 2012 - Springer
For several decades, the 4-aminoquinolines chloroquine (CQ) and amodiaquine (AQ) were
considered the most important drugs for the control and eradication of malaria. The success …

Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents

S Pandey, P Agarwal, K Srivastava… - European journal of …, 2013 - Elsevier
A series of novel tetrazole derivatives of 4-aminoquinoline were synthesized and screened
for their antimalarial activities against both chloroquine-senstive (3D7) and chloroquine …

Quinoline hybrids and their antiplasmodial and antimalarial activities

YQ Hu, C Gao, S Zhang, L Xu, Z Xu, LS Feng… - European Journal of …, 2017 - Elsevier
Malaria, in particular infection with P. falciparum (the most lethal of the human malaria
parasite species, responsible for nearly one million deaths every year), is one of the most …

Synthesis of 4‐aminoquinoline‐1, 2, 3‐triazole and 4‐aminoquinoline‐1, 2, 3‐triazole‐1, 3, 5‐triazine Hybrids as Potential Antimalarial Agents

S Manohar, SI Khan, DS Rawat - Chemical Biology & Drug …, 2011 - Wiley Online Library
We report herein synthesis of a series of 4‐aminoquinoline‐1, 2, 3‐triazole and 4‐
aminoquinoline‐1, 2, 3‐triazole‐1, 3, 5‐triazine hybrids and evaluate their antimalarial …

Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure–Activity and Structure–Property …

R Neelarapu, JR Maignan, CL Lichorowic… - Journal of medicinal …, 2018 - ACS Publications
Malaria deaths have been decreasing over the last 10–15 years, with global mortality rates
having fallen by 47% since 2000. While the World Health Organization (WHO) recommends …

4-aminoquinolines active against chloroquine-resistant Plasmodium falciparum: basis of antiparasite activity and quantitative structure-activity relationship analyses

SJ Hocart, H Liu, H Deng, D De… - Antimicrobial agents …, 2011 - Am Soc Microbiol
Chloroquine (CQ) is a safe and economical 4-aminoquinoline (AQ) antimalarial. However,
its value has been severely compromised by the increasing prevalence of CQ resistance …

Recent developments in antimalarial drug discovery

AA Joshi, CL Viswanathan - Anti-Infective Agents in Medicinal …, 2006 - ingentaconnect.com
Malaria with 1 million deaths and about 500 million new cases reported annually is a
challenge to drug therapy and discovery. Drug resistance accompanied by lack of progress …

Quinolines and structurally related heterocycles as antimalarials

K Kaur, M Jain, RP Reddy, R Jain - European journal of medicinal …, 2010 - Elsevier
The quinoline scaffold is prevalent in a variety of pharmacologically active synthetic and
natural compounds. The discovery of chloroquine, the most famous drug containing this …