New Trifluoromethyl Triazolopyrimidines as Anti-Plasmodiumfalciparum Agents

N Boechat, LCS Pinheiro, TS Silva, ACC Aguiar… - Molecules, 2012 - mdpi.com
According to the World Health Organization, half of the World's population, approximately
3.3 billion people, is at risk for developing malaria. Nearly 700,000 deaths each year are …

Discovery of new hit-molecules targeting Plasmodium falciparum through a global SAR study of the 4-substituted-2-trichloromethylquinazoline antiplasmodial scaffold

J Desroches, C Kieffer, N Primas, S Hutter… - European journal of …, 2017 - Elsevier
From 4 antiplasmodial hit-molecules identified in 2-trichloromethylquinazoline series, we
conducted a global Structure-Activity relationship (SAR) study involving 26 compounds and …

Design, synthesis and antimalarial evaluation of novel thiazole derivatives

JM Bueno, M Carda, B Crespo, AC Cuñat… - Bioorganic & medicinal …, 2016 - Elsevier
As part of our medicinal chemistry program's ongoing search for compounds with
antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study …

Synthesis and structure–activity relationship of 3-phenylquinoxaline 1, 4-di-N-oxide derivatives as antimalarial agents

E Vicente, LM Lima, E Bongard, S Charnaud… - European journal of …, 2008 - Elsevier
As a continuation of our research and with the aim of obtaining new antimalarial agents, new
series of 3-phenylquinoxaline 1, 4-di-N-oxide derivatives have been synthesized following …

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice

R Gujjar, A Marwaha, F El Mazouni… - Journal of medicinal …, 2009 - ACS Publications
Plasmodium falciparum causes 1− 2 million deaths annually. Yet current drug therapies are
compromised by resistance. We previously described potent and selective …

Synthesis, in silico experiments and biological evaluation of 1, 3, 4-trisubstituted pyrazole derivatives as antimalarial agents

AA Bekhit, MN Saudi, AMM Hassan, SM Fahmy… - European journal of …, 2019 - Elsevier
Abstract New 1, 3, 4-trisubstituted pyrazole derivatives were synthesized and evaluated for
their antiplasmodial activity. Compounds 4b, 4c, 7a and 7d were the most potent …

2-aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure–activity relationship and mode of action studies

K Singh, H Kaur, K Chibale, J Balzarini, S Little… - European journal of …, 2012 - Elsevier
2-Aminopyrimidine based 4-aminoquinolines were synthesized using an efficacious
protocol. Some of the compounds showed in vitro anti-plasmodial activity against drug …

Synthesis, antiplasmodial activity, and β-hematin inhibition of hydroxypyridone–chloroquine hybrids

WA Andayi, TJ Egan, J Gut, PJ Rosenthal… - ACS Medicinal …, 2013 - ACS Publications
A series of noncytotoxic 4-aminoquinoline-3-hydroxypyridin-4-one hybrids were synthesized
on the basis of a synergistic in vitro combination of a precursor N-alkyl-3-hydroxypyridin-4 …

Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives

M Xu, J Zhu, Y Diao, H Zhou, X Ren… - Journal of Medicinal …, 2013 - ACS Publications
Taking the emergence of drug resistance and lack of effective antimalarial vaccines into
consideration, it is of significant importance to develop novel antimalarial agents for the …

Synthesis and in vitro evaluation of novel 8-aminoquinoline–pyrazolopyrimidine hybrids as potent antimalarial agents

M Kannan, AV Raichurkar, FRN Khan… - Bioorganic & Medicinal …, 2015 - Elsevier
In the search of novel chemotherapeutic agents for emerging drug resistant parasites, the
hybridization approaches have successfully emerged as an efficient tool in malarial …