Investigating the targeting power to brain tissues of intranasal rasagiline mesylate-loaded transferosomal in situ gel for efficient treatment of Parkinson's disease

HN ElShagea, RR Makar, AH Salama, NA Elkasabgy… - Pharmaceutics, 2023 - mdpi.com
Rasagiline mesylate (RSM) is a hydrophilic drug with poor oral bioavailability (36%)
because of hepatic first-pass metabolism. The present study focuses on delivering RSM …

[HTML][HTML] Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues

MM Hassan, YD Li, MW Ma, M Teng, WS Byun… - European Journal of …, 2024 - Elsevier
Chemically induced proximity modalities such as targeted protein degradation (TPD) hold
promise for expanding the number of proteins that can be manipulated pharmacologically …

Propargylamine: an important moiety in drug discovery

A Carneiro, E Uriarte, F Borges… - Future Medicinal …, 2023 - Taylor & Francis
Propargylamine is a chemical moiety whose properties have made it a widely distributed
group within the fields of medicinal chemistry and chemical biology. Its particular reactivity …

Superiority of the Triple-Acting 5-HT6R/5-HT3R Antagonist and MAO-B Reversible Inhibitor PZ-1922 over 5-HT6R Antagonist Intepirdine in Alleviation of Cognitive …

K Grychowska, U López-Sánchez… - Journal of Medicinal …, 2023 - ACS Publications
The multifactorial origin and neurochemistry of Alzheimer's disease (AD) call for the
development of multitarget treatment strategies. We report a first-in-class triple acting …

Resveratrol analogues as dual inhibitors of monoamine oxidase b and carbonic anhydrase vii: a new multi-target combination for neurodegenerative diseases?

S Carradori, M Fantacuzzi, A Ammazzalorso, A Angeli… - Molecules, 2022 - mdpi.com
Neurodegenerative diseases (NDs) are described as multifactorial and progressive
syndromes with compromised cognitive and behavioral functions. The multi-target-directed …

N-substituted benzimidazole acrylonitriles as in vitro tubulin polymerization inhibitors: Synthesis, biological activity and computational analysis

N Perin, L Hok, A Beč, L Persoons, E Vanstreels… - European journal of …, 2021 - Elsevier
We present the design, synthesis and biological activity of novel N-substituted
benzimidazole based acrylonitriles as potential tubulin polymerization inhibitors. Their …

[HTML][HTML] COVID-19 infection and neurodegeneration: Computational evidence for interactions between the SARS-CoV-2 spike protein and monoamine oxidase …

L Hok, H Rimac, J Mavri, R Vianello - Computational and structural …, 2022 - Elsevier
Although COVID-19 has been primarily associated with pneumonia, recent data show that
its causative agent, the SARS-CoV-2 coronavirus, can infect many vital organs beyond the …

Novel imidazo [4, 5-b] pyridine derived acrylonitriles: A combined experimental and computational study of their antioxidative potential

I Boček, K Starčević, IN Jovanović, R Vianello… - Journal of molecular …, 2021 - Elsevier
We describe the synthesis of novel unsubstituted and N-substituted imidazo [4, 5-b] pyridine
derived acrylonitriles, which were prepared by classical and microwave assisted organic …

Harmicines− harmine and cinnamic acid hybrids as novel antiplasmodial hits

I Perković, S Raić-Malić, D Fontinha… - European journal of …, 2020 - Elsevier
Harmicines constitute novel hybrid compounds that combine two agents with reported
antiplasmodial properties, namely β-carboline harmine and a cinnamic acid derivative …

Synthesis and spectroscopic characterization of multifunctional D-π-A benzimidazole derivatives as potential pH sensors

A Beč, R Vianello, M Hranjec - Journal of molecular liquids, 2023 - Elsevier
We report multifunctional D-π-A molecular systems having the N, N-diethylamino group as a
pH sensitive donor unit connected to the electron accepting substituents such as the cyano …