Recent advances on patents of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors as antimalarial agents

P Gehlot, VK Vyas - Expert Opinion on Therapeutic Patents, 2023 - Taylor & Francis
Introduction Pyrimidine nucleotides are essential for the parasite's growth and replication.
Parasites have only a de novo pathway for the biosynthesis of pyrimidine nucleotides …

Dihydroorotate dehydrogenase: a drug target for the development of antimalarials

A Singh, M Maqbool, M Mobashir, N Hoda - European Journal of Medicinal …, 2017 - Elsevier
Malaria is a critical human disease with extensive exploration yet unestablished due to
occurrence of frequent drug resistance. This aspect of malaria pharmacology calls for the …

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 …

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 …

Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases

PTP Bedingfield, D Cowen, P Acklam… - Journal of medicinal …, 2012 - ACS Publications
The de novo pyrimidine biosynthesis enzyme dihydroorotate dehydrogenase is an emerging
drug target for the treatment of malaria. In this context a key property of Plasmodium …

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 …

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 …

High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase

J Baldwin, CH Michnoff, NA Malmquist, J White… - Journal of Biological …, 2005 - ASBMB
Plasmodium falciparum is the causative agent of the most serious and fatal malarial
infections, and it has developed resistance to commonly employed chemotherapeutics. The …

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 …

Plasmodium Falciparum Dihydroorotate Dehydrogenase: A Drug Target against Malaria

LVB Hoelz, FA Calil, MC Nonato… - Future Medicinal …, 2018 - Taylor & Francis
Malaria remains one of the most lethal infectious diseases worldwide, and the most severe
form is caused by Plasmodium falciparum. In recent decades, the major challenge to …