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 …

Triazole derivatives and their antiplasmodial and antimalarial activities

XM Chu, C Wang, WL Wang, LL Liang, W Liu… - European journal of …, 2019 - Elsevier
Malaria, caused by protozoan parasites of the genus Plasmodium especially by the most
prevalent parasite Plasmodium falciparum, represents one of the most devastating and …

Pharmacological significance of triazole scaffold

R Kharb, PC Sharma, MS Yar - Journal of enzyme inhibition and …, 2011 - Taylor & Francis
The triazole nucleus is one of the most important and well known heterocycles which is a
common and integral feature of a variety of natural products and medicinal agents. Triazole …

[HTML][HTML] Antimalarial drug discovery—approaches and progress towards new medicines

EL Flannery, AK Chatterjee, EA Winzeler - Nature Reviews Microbiology, 2013 - nature.com
Malaria elimination has recently been reinstated as a global health priority but current
therapies seem to be insufficient for the task. Elimination efforts require new drug classes …

Chemical genetics of Plasmodium falciparum

WA Guiguemde, AA Shelat, D Bouck, S Duffy… - Nature, 2010 - nature.com
Malaria caused by Plasmodium falciparum is a disease that is responsible for 880,000
deaths per year worldwide. Vaccine development has proved difficult and resistance has …

Repositioning of acefylline as anti-cancer drug: Synthesis, anticancer and computational studies of azomethines derived from acefylline tethered 4-amino-3-mercapto …

I Shahzadi, AF Zahoor, B Tüzün, A Mansha, MN Anjum… - Plos one, 2022 - journals.plos.org
Novel azomethines derived from acefylline tethered triazole hybrids (7a-k) have been
synthesized and evaluated against human liver cancer cell line (Hep G2) using MTT assay …

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with …

JM Coteron, M Marco, J Esquivias, X Deng… - Journal of medicinal …, 2011 - ACS Publications
Drug therapy is the mainstay of antimalarial therapy, yet current drugs are threatened by the
development of resistance. In an effort to identify new potential antimalarials, we have …

New medicines to improve control and contribute to the eradication of malaria

TNC Wells, PL Alonso, WE Gutteridge - Nature reviews Drug discovery, 2009 - nature.com
Despite being one of the most prevalent tropical diseases, for many years malaria was not a
commercial priority for the pharmaceutical industry. However, in response to the emergence …

On dihydroorotate dehydrogenases and their inhibitors and uses

H Munier-Lehmann, PO Vidalain… - Journal of medicinal …, 2013 - ACS Publications
Proper nucleosides availability is crucial for the proliferation of living entities (eukaryotic
cells, parasites, bacteria, and virus). Accordingly, the uses of inhibitors of the de novo …

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 …