Fluorine and fluorinated motifs in the design and application of bioisosteres for drug design

NA Meanwell - Journal of medicinal chemistry, 2018 - ACS Publications
The electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …

An insight on medicinal attributes of 1, 2, 4-triazoles

R Aggarwal, G Sumran - European journal of medicinal chemistry, 2020 - Elsevier
The present review aims to summarize the pharmacological profile of 1, 2, 4-triazole, one of
the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant …

Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or …

A Llanos-Cuentas, M Casapia… - The Lancet Infectious …, 2018 - thelancet.com
Background DSM265 is a novel, long-duration inhibitor of plasmodium dihydroorotate
dehydrogenase (DHODH) with excellent selectivity over human DHODH and activity against …

The dihydroorotate dehydrogenases: past and present

RAG Reis, FA Calil, PR Feliciano, MP Pinheiro… - Archives of biochemistry …, 2017 - Elsevier
The flavoenzyme dihydroorotate dehydrogenase catalyzes the stereoselective oxidation of
(S)-dihydroorotate to orotate in the fourth of the six conserved enzymatic reactions involved …

MalDA, accelerating malaria drug discovery

T Yang, S Ottilie, ES Istvan, KP Godinez-Macias… - Trends in …, 2021 - cell.com
The Malaria Drug Accelerator (MalDA) is a consortium of 15 leading scientific laboratories.
The aim of MalDA is to improve and accelerate the early antimalarial drug discovery process …

1, 2, 4-Triazolo [1, 5-a] pyrimidines in drug design

K Oukoloff, B Lucero, KR Francisco, KR Brunden… - European journal of …, 2019 - Elsevier
Abstract The 1, 2, 4-triazolo [1, 5-a] pyrimidine (TP) heterocycle, in spite of its relatively
simple structure, has proved to be remarkably versatile as evidenced by its use in many …

[HTML][HTML] Quinoline derivatives as possible lead compounds for anti-malarial drugs: Spectroscopic, DFT and MD study

B Sureshkumar, YS Mary, CY Panicker, S Suma… - Arabian Journal of …, 2020 - Elsevier
In this work we report spectroscopic characterization and reactivity study by density
functional theory (DFT) and molecular dynamics (MD) simulations of two quinoline …

[HTML][HTML] The molecular basis of antimalarial drug resistance in Plasmodium vivax

LE Buyon, B Elsworth, MT Duraisingh - International Journal for …, 2021 - Elsevier
Plasmodium vivax is the most geographically widespread cause of human malaria and is
responsible for the majority of cases outside of the African continent. While great progress …

Dihydroorotate dehydrogenase inhibitors in anti-infective drug research

D Boschi, AC Pippione, S Sainas, ML Lolli - European journal of medicinal …, 2019 - Elsevier
Pyrimidines are essential for the cell survival and proliferation of living parasitic organisms,
such as Helicobacter pylori, Plasmodium falciparum and Schistosoma mansoni, that are …

The development process for discovery and clinical advancement of modern antimalarials

TD Ashton, SM Devine, JJ Mohrle, B Laleu… - Journal of Medicinal …, 2019 - ACS Publications
Malaria is a devastating disease caused by Plasmodium parasites, resulting in
approximately 435000 deaths in 2018. The impact of malaria is compounded by the …