Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies

AC Pippione, S Sainas, P Goyal, I Fritzson… - European journal of …, 2019 - Elsevier
Plasmodium falciparum dihydroorotate dehydrogenase (Pf DHODH) has been clinically
validated as a target for antimalarial drug discovery, as a triazolopyrimidine class inhibitor …

Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase

M Maetani, N Kato, VAP Jabor, FA Calil… - ACS Medicinal …, 2017 - ACS Publications
Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine
biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of …

Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

PB Madrid, J Sherrill, AP Liou, JL Weisman… - Bioorganic & medicinal …, 2005 - Elsevier
A simple two-step synthesis method was used to make 51 B-ring-substituted 4-
hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth …

Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors

F Kayamba, T Malimabe, IK Ademola, OJ Pooe… - European Journal of …, 2021 - Elsevier
Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of
Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant …

Novel antimalarial chloroquine-and primaquine-quinoxaline 1, 4-di-N-oxide hybrids: Design, synthesis, Plasmodium life cycle stage profile, and preliminary toxicity …

L Bonilla-Ramirez, A Rios, M Quiliano… - European Journal of …, 2018 - Elsevier
Emergence of drug resistance and targeting all stages of the parasite life cycle are currently
the major challenges in antimalarial chemotherapy. Molecular hybridization combining two …

Synthesis and evaluation of new diaryl ether and quinoline hybrids as potential antiplasmodial and antimicrobial agents

A Mishra, H Batchu, K Srivastava, P Singh… - Bioorganic & Medicinal …, 2014 - Elsevier
Synthesis and bioevaluation of new diaryl ether hybridized quinoline derivatives as
antiplasmodial, antibacterial and antifungal agents is reported. It was encouraging to …

4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ‐Sensitive and CQ‐Resistant Strains of Plasmodium falciparum

S Manohar, SI Khan, DS Rawat - Chemical biology & drug …, 2013 - Wiley Online Library
A systematic chemical modification in the triazine moiety covalently attached via suitable
linkers to 4‐amino‐7‐chloroquinolines yielded a series of new 7‐chloro‐4‐aminoquinoline …

Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines

P Verhaeghe, N Azas, S Hutter… - Bioorganic & medicinal …, 2009 - Elsevier
To identify a new safe antiplasmodial molecular scaffold, an original series of 2-
trichloromethylquinazolines, functionalized in position 4 by an alkyl-or arylamino substituent …

Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase

T Heikkilä, C Ramsey, M Davies, C Galtier… - Journal of medicinal …, 2007 - ACS Publications
Pyrimidine biosynthesis presents an attractive drug target in malaria parasites due to the
absence of a pyrimidine salvage pathway. A set of compounds designed to inhibit the …

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 …