Evaluation of 7-arylaminopyrazolo [1, 5-a] pyrimidines as anti-Plasmodium falciparum, antimalarial, and Pf-dihydroorotate dehydrogenase inhibitors

LFSP Azeredo, JP Coutinho, VAP Jabor… - European Journal of …, 2017 - Elsevier
Malaria remains one of the most serious global infectious diseases. An important target for
antimalarial chemotherapy is the enzyme dihydroorotate dehydrogenase from Plasmodium …

Lead Optimization of Aryl and Aralkyl Amine-Based Triazolopyrimidine Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity …

R Gujjar, F El Mazouni, KL White, J White… - Journal of medicinal …, 2011 - ACS Publications
Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability
to maintain effective therapy to combat the illness is continually challenged by the …

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective …

S Kokkonda, X Deng, KL White… - Journal of Medicinal …, 2016 - ACS Publications
Malaria persists as one of the most devastating global infectious diseases. The pyrimidine
biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) has been identified as a new …

The development of novel compounds against malaria: quinolines, triazolpyridines, pyrazolopyridines and pyrazolopyrimidines

L CS Pinheiro, L M. Feitosa, M O. Gandi, F F. Silveira… - Molecules, 2019 - mdpi.com
Based on medicinal chemistry tools, new compounds for malaria treatment were designed.
The scaffolds of the drugs used to treat malaria, such as chloroquine, primaquine …

Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitors with Potent and Selective Activity against the Malaria Parasite Plasmodium falciparum

MA Phillips, R Gujjar, NA Malmquist… - Journal of medicinal …, 2008 - ACS Publications
A Plasmodium falciparum dihydroorotate dehydrogenase (Pf DHODH) inhibitor that is potent
(KI= 15 nM) and species-selective (> 5000-fold over the human enzyme) was identified by …

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 …

Comparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH …

FF Silveira, JO de Souza, LVB Hoelz… - European Journal of …, 2021 - Elsevier
In this work, we designed and synthesized 35 new triazolopyrimidine, pyrazolopyrimidine
and quinoline derivatives as P. falciparum inhibitors (3D7 strain). Thirty compounds …

Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria

S Kokkonda, X Deng, KL White… - Journal of medicinal …, 2020 - ACS Publications
Malaria puts at risk nearly half the world's population and causes high mortality in sub-
Saharan Africa, while drug resistance threatens current therapies. The pyrimidine …

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 …

Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model

ML Booker, CM Bastos, ML Kramer, RH Barker… - Journal of Biological …, 2010 - ASBMB
Plasmodium falciparum, the causative agent of the most deadly form of human malaria, is
unable to salvage pyrimidines and must rely on de novo biosynthesis for survival …