Results 31 to 40 of about 8,411 (245)

Synthesis, Structure and Evaluation of the N-(2-Acetyl-4-(styryl)phenyl)-4-benzenesulfonamide Derivatives for Anticholinesterase and Antioxidant Activities

Crystals, 2021
N-(2-Acetyl-4-bromophenyl)-4-methylbenzenesulfonamide (2) was transformed into 5-(4-methoxymethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3a) and 5-(4- trifluoromethylstyryl)-2-(p-tolylsulfonamido)acetophenone (3b).
Malose J. Mphahlele, Samantha Gildenhuys, Sizwe J. Zamisa   +2 more
doaj   +1 more source

Fine-Tuning the Biological Profile of Multitarget Mitochondriotropic Antioxidants for Neurodegenerative Diseases

Antioxidants, 2021
Neurotransmitter depletion and mitochondrial dysfunction are among the multiple pathological events that lead to neurodegeneration. Following our previous studies related with the development of multitarget mitochondriotropic antioxidants, this study ...
Daniel Chavarria, Ophelie Da Silva, Sofia Benfeito, Sandra Barreiro, Jorge Garrido, Fernando Cagide, Pedro Soares, Fernando Remião, Xavier Brazzolotto, Florian Nachon, Paulo J. Oliveira, José Dias, Fernanda Borges   +12 more
doaj   +1 more source

A twenty-year journey exploring coumarin-based derivatives as bioactive molecules

Frontiers in Chemistry, 2022
The coumarin core (i.e., 1-benzopyran-2 (2H)-one) is a structural motif highly recurrent in both natural products and bioactive molecules. Indeed, depending on the substituents and branching positions around the byciclic core, coumarin-containing ...
Leonardo Pisani, Marco Catto, Giovanni Muncipinto, Orazio Nicolotti, Antonio Carrieri, Mariagrazia Rullo, Angela Stefanachi, Francesco Leonetti, Cosimo Altomare   +8 more
doaj   +1 more source

Sulfonamide-Based 2-Amino-1,3,4-Oxadiazole Derivatives as Dual Cholinesterase and Carbonic Anhydrase Inhibitors: Design, Synthesis, Kinetic Characterization, Molecular Modeling, and ADMET Evaluation. [PDF]

Drug Dev Res
ABSTRACT In this study, 12 novel sulfonamide derivatives incorporating 2‐amino‐1,3,4‐oxadiazole and 1,3‐benzazol‐2(3H)‐one scaffolds were synthesized and structurally characterized using 1H NMR, 13C NMR, and LC–MS analyses. Their inhibitory activities were evaluated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase I
Arslan Karahan G, Gökçe B, Muhammed MT, Ayan EK, Özçelik AB.   +4 more
europepmc   +2 more sources

series as cholinesterases inhibitors: Enzymatic and modeling studies

, 2022
Histamine is involved in several central nervous system processes including cognition. In the last years, H3 receptor (H3R) antagonists have been widely explored for their potential on dementias and other cognitive dysfunctions, and the cooperative role ...
Flávia B. Lopes, Fernandes, Gustavo A. B., Fernandes, João Paulo S., Cecília M. S. Q. Aranha, Michelle F. Corrêa, Okamoto, Debora N., Gustavo A. B. Fernandes, Corrêa, Michelle F., Nailton M. N. Junior, Leonardo P. M. Simões, João Paulo S. Fernandes, Junior, Nailton M. N. [UNESP], Debora N. Okamoto, Lopes, Flávia B., Aranha, Cecília M. S. Q., Simões, Leonardo P. M. [UNESP]   +15 more
core   +1 more source

Molecular Basis for Activation to Inhibition Switching in Kv7.2 Channel Modulators

Angewandte Chemie, EarlyView.
The paper describes the serendipitous discovery of chemical manipulation allowing the activator‐to‐inhibitor switching in Kv7.2 channel modulators. The molecular determinants driving this switch have been rationalized by multidisciplinary investigation encompassing synthetic and analytical chemistry, in silico methods, cryo‐EM analysis ...
Tania Ciaglia, Giusy Carleo, Zhenni Yang, Francesca Di Matteo, Federica De Rosa, Gerardina Smaldone, Zhao‐Bing Gao, Marco D'Alì, Rita Turcio, Demin Ma, Veronica Di Sarno, Nannan Su, Salvatore Vincenzo Giofrè, Giacomo Pepe, Pietro Campiglia, Alessia Bertamino, Francesco Miceli, Jiangtao Guo, Nunzio Iraci, Carmine Ostacolo, Maurizio Taglialatela   +20 more
wiley   +2 more sources

Exploring Structure-Activity Relationship in Tacrine-Squaramide Derivatives as Potent Cholinesterase Inhibitors

Biomolecules, 2019
Tacrine was the first drug to be approved for Alzheimer’s disease (AD) treatment, acting as a cholinesterase inhibitor. The neuropathological hallmarks of AD are amyloid-rich senile plaques, neurofibrillary tangles, and neuronal degeneration.
Barbora Svobodova, Eva Mezeiova, Vendula Hepnarova, Martina Hrabinova, Lubica Muckova, Tereza Kobrlova, Daniel Jun, Ondrej Soukup, María Luisa Jimeno, José Marco-Contelles, Jan Korabecny   +10 more
doaj   +1 more source

N-Hydroxy-N-Propargylamide Derivatives of Ferulic Acid: Inhibitors of Cholinesterases and Monoamine Oxidases

Molecules, 2022
Alzheimer’s disease (AD) is a complex disorder characterized by impaired neurotransmission in cholinergic and monoaminergic neurons, which, in combination with the accumulation of misfolded proteins and increased oxidative stress, leads to the typical ...
Óscar M. Bautista-Aguilera, José M. Alonso, Marco Catto, Isabel Iriepa, Damijan Knez, Stanislav Gobec, José Marco-Contelles   +6 more
doaj   +1 more source

Autoregulation of Acetylcholine Release and Micro-Pharmacodynamic Mechanisms at Neuromuscular Junction: Selective Acetylcholinesterase Inhibitors for Therapy of Myasthenic Syndromes

Frontiers in Pharmacology, 2018
Neuromuscular junctions (NMJs) are directly involved into such indispensable to life processes as respiration and locomotion. However, motor nerve forms only one synaptic contact at each muscle fiber.
Konstantin A. Petrov, Konstantin A. Petrov, Evgeny E. Nikolsky, Patrick Masson   +3 more
doaj   +1 more source

Therapeutic Potentials of Microalgae in the Treatment of Alzheimer’s Disease

Molecules, 2017
Current research is geared towards the discovery of new compounds with strong neuroprotective potential and few or no side effects compared to synthetic drugs.
Tosin A. Olasehinde, Ademola O. Olaniran, Anthony I. Okoh   +2 more
doaj   +1 more source