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 …

Carboxylic acid bioisosteres in medicinal chemistry: synthesis and properties

K Bredael, S Geurs, D Clarisse… - Journal of …, 2022 - Wiley Online Library
Lead optimization represents the tedious process of fine‐tuning lead compounds from
biologically active hits to suitable drug candidates for clinical trials. By chemically modifying …

Diversity of AMPA receptor ligands: Chemotypes, binding modes, mechanisms of action, and therapeutic effects

EA Golubeva, MI Lavrov, EV Radchenko, VA Palyulin - Biomolecules, 2022 - mdpi.com
L-Glutamic acid is the main excitatory neurotransmitter in the central nervous system (CNS).
Its associated receptors localized on neuronal and non-neuronal cells mediate rapid …

Click 1, 2, 3-triazoles in drug discovery and development: From the flask to the clinic?

M Serafini, T Pirali, GC Tron - Advances in Heterocyclic Chemistry, 2021 - Elsevier
After 20 years since its conception, click chemistry has come of age and we believe the time
has come to evaluate if the copper-catalyzed azide alkyne cycloaddition (CuCAAC) reaction …

Structure property relationships of N-acylsulfonamides and related bioisosteres

KR Francisco, C Varricchio, TJ Paniak… - European journal of …, 2021 - Elsevier
The N-acylsulfonamide functional group is a feature of the pharmacophore of several
biologically active molecules, including marketed drugs. Although this acidic moiety …

Effective deploying of a novel DHODH inhibitor against herpes simplex type 1 and type 2 replication

A Luganini, G Sibille, B Mognetti, S Sainas… - Antiviral Research, 2021 - Elsevier
Emergence of drug resistance and adverse effects often affect the efficacy of nucleoside
analogues in the therapy of Herpes simplex type 1 (HSV-1) and type 2 (HSV-2) infections …

Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-a]pyridine Scaffold …

S Sainas, M Giorgis, P Circosta… - Journal of Medicinal …, 2021 - ACS Publications
The connection with acute myelogenous leukemia (AML) of dihydroorotate dehydrogenase
(h DHODH), a key enzyme in pyrimidine biosynthesis, has attracted significant interest from …

[HTML][HTML] Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer

AC Pippione, S Kovachka, C Vigato, L Bertarini… - European Journal of …, 2024 - Elsevier
AKR1C3 is an enzyme that is overexpressed in several types of radiotherapy-and
chemotherapy-resistant cancers. Despite AKR1C3 is a validated target for drug …

New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold

AC Pippione, Z Kilic-Kurt, S Kovachka, S Sainas… - European Journal of …, 2022 - Elsevier
The aldo-keto reductase 1C3 (AKR1C3) enzyme is considered an attractive target in
Castration Resistant Prostate Cancer (CRPC) because of its role in the biosynthesis of …

Synthesis and photophysics of benzazole based triazoles with amino acid-derived pendant units. Multiparametric optical sensors for BSA and CT-DNA in solution

NP Debia, JJP Rodríguez, CH da Silveira… - Journal of Molecular …, 2020 - Elsevier
Herein we report the synthesis of a series of amino acid-derived triazoles by an
organocatalytic cycloaddition reaction between azides and carbonyl compounds, catalyzed …