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 …

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 …

Synthesis, anti-plasmodial activities, and mechanistic insights of 4-aminoquinoline-triazolopyrimidine hybrids

S Chowdhary, Shalini, J Mosnier, I Fonta… - ACS Medicinal …, 2022 - ACS Publications
In the search of new antiplasmodial agents, a multitargeted approach was used in the
synthesis of triazolopyrimidine-and 4-aminoquinolines-based hybrids. In vitro antiplasmodial …

Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity

S Manohar, UC Rajesh, SI Khan… - ACS medicinal …, 2012 - ACS Publications
A class of hybrid molecules consisting of 4-aminoquinoline and pyrimidine were synthesized
and tested for antimalarial activity against both chloroquine (CQ)-sensitive (D6) and …

N-cinnamoylated chloroquine analogues as dual-stage antimalarial leads

BC Pérez, C Teixeira, IS Albuquerque… - Journal of Medicinal …, 2013 - ACS Publications
The control of malaria is challenged by drug resistance, and new antimalarial drugs are
needed. New drug discovery efforts include consideration of hybrid compounds as potential …

Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum

KV Sashidhara, SR Avula, GR Palnati, SV Singh… - Bioorganic & medicinal …, 2012 - Elsevier
The control of malaria has been complicated with increasing resistance of malarial parasite
against existing antimalarials. Herein, we report the synthesis of a new series of chloroquine …

[HTML][HTML] Introducing new antimalarial analogues of chloroquine and amodiaquine: a narrative review

AR Parhizgar, A Tahghighi - Iranian journal of medical sciences, 2017 - ncbi.nlm.nih.gov
Antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs,
chloroquine (CQ) and amodiaquine (AQ), have been used to prevent and treat malaria for …

Design, synthesis, and in silico-in vitro antimalarial evaluation of 1, 2, 3-triazole-linked dihydropyrimidinone quinoline hybrids

RA Adigun, FP Malan, MO Balogun, N October - Structural Chemistry, 2023 - Springer
In response to the malaria parasite's resistance towards quinoline-based antimalarial drugs,
we have employed quinoline-containing compounds in combination with …

New quinoline-5, 8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain

H Hussain, S Specht, SR Sarite, A Hoerauf… - European journal of …, 2012 - Elsevier
We report on the design, synthesis, and in vitro evaluation of new quinoline-5, 8-dione and
hydroxynaphthoquinone derivatives. The synthesized compounds were evaluated for in vitro …

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 …