Keyword search (4,163 papers available)

"Forgione P" Authored Publications:

Title Authors PubMed ID
1 Regioselective Stepwise Synthesis of Unsymmetrical 1,2,5-Triarylpyrroles via Palladium-Catalyzed Decarboxylative Cross-Coupling and C-H Arylation Buonomano C; Patterson S; Ngou JS; Messina C; Taylor S; Bilodeau F; Forgione P; 41900086
CHEMBIOCHEM
2 A Modular and Regioselective Synthesis of Di- and Triarylated Thiophenes: Strategies for Accessing Challenging Isomeric Motifs Messina C; McKibbon K; Wong KS; Prevost P; Petkov V; Forgione P; 41160050
CONCORDIA
3 In vitro evaluation of isatin-pyridine oxime hybrids as potential acetylcholinesterase inhibitors for nerve agent prophylaxis Silva MCJD; Pinto AMV; Balthar MA; Correa ABA; Bhattacharyya D; Simas ABC; Kuca K; Forgione P; França TCC; Cavalcante SFA; Kitagawa DAS; 40516590
CHEMBIOCHEM
4 A Modular and Catalytic Methodology To Access 2,5-Furan-Based Phenylene/Thiophene Oligomers through a One-Pot Decarboxylative Cross-Coupling from 5-Bromofurfural Cigana B; Lapointe V; Majewski MB; Forgione P; 38808994
CHEMBIOCHEM
5 Sterically-Hindered Molecular p-Dopants Promote Integer Charge Transfer in Organic Semiconductors Charoughchi S; Liu JT; Berteau-Rainville M; Hase H; Askari MS; Bhagat S; Forgione P; Salzmann I; 37220083
CHEMBIOCHEM
6 Diverse Applications of Biomass-Derived 5-Hydroxymethylfurfural and Derivatives as Renewable Starting Materials Chacón-Huete F; Messina C; Cigana B; Forgione P; 35652539
CHEMBIOCHEM
7 Solvent-free synthesis of 3,5-isoxazoles via 1,3-dipolar cycloaddition of terminal alkynes and hydroxyimidoyl chlorides over Cu/Al2O3 surface under ball-milling conditions Hernandez R RA; Burchell-Reyes K; Braga APCA; Lopez JK; Forgione P; 35424611
CHEMBIOCHEM
8 Characterization of a recently synthesized microtubule-targeting compound that disrupts mitotic spindle poles in human cells Jaunky DB; Larocque K; Husser MC; Liu JT; Forgione P; Piekny A; 34880347
BIOLOGY
9 Programmed Synthesis of Tetra-Aryl Thiophenes with Stepwise, Ester-Controlled Regioselectivity Messina C; Ottenwaelder X; Forgione P; 34506149
CHEMBIOCHEM
10 Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent Liu JT; Jaunky DB; Larocque K; Chen F; Mckibbon K; Sirouspour M; Taylor S; Shafeii A; Campbell D; Braga H; Piekny A; Forgione P; 34416378
BIOLOGY
11 Synthesis of 2,5-Diaryl Nonsymmetric Furans C6-Platform Chemicals via Catalytic Conversion of Biomass and the Formal Synthesis of Dantrolene. Chacón-Huete F, Lasso JD, Szavay P, Covone J, Forgione P 33253575
CHEMBIOCHEM
12 Approaching the Integer-Charge Transfer Regime in Molecularly Doped Oligothiophenes by Efficient Decarboxylative Cross-Coupling Liu JT; Hase H; Taylor S; Salzmann I; Forgione P; 31961982
CHEMBIOCHEM
13 Facile Aqueous-Phase Synthesis of an Ultrasmall Bismuth Nanocatalyst for the Reduction of 4-Nitrophenol. Liang Y, Manioudakis J, Macairan JR, Askari MS, Forgione P, Naccache R 31552336
CHEMBIOCHEM
14 Virtual screening, docking, and dynamics of potential new inhibitors of dihydrofolate reductase from Yersinia pestis. Bastos Lda C, de Souza FR, Guimarães AP, Sirouspour M, Cuya Guizado TR, Forgione P, Ramalho TC, França TC 26494420
CHEMISTRY
15 Analysis of Coxiela burnetti dihydrofolate reductase via in silico docking with inhibitors and molecular dynamics simulation. de Souza FR, Guimarães AP, Cuya T, de Freitas MP, Gonçalves ADS, Forgione P, Costa França TC 27726597
CHEMBIOCHEM
16 Investigating the selectivity of potential new inhibitors of dihydrofolate reductase from Yersinia pestis designed by molecular modeling. Bastos LDC, de Souza FR, Pereira Souza LM, Forgione P, Cuya T, de Alencastro RB, Pimentel AS, Celmar Costa França T 29542379
CHEMBIOCHEM

 

Title:In vitro evaluation of isatin-pyridine oxime hybrids as potential acetylcholinesterase inhibitors for nerve agent prophylaxis
Authors:Silva MCJD,  Pinto AMV,  Balthar MA,  Correa ABA,  Bhattacharyya D,  Simas ABC,  Kuca K,  Forgione P,  França TCC,  Cavalcante SFA,  Kitagawa DAS
Link:https://pubmed.ncbi.nlm.nih.gov/40516590/
DOI:10.1016/j.cbi.2025.111605
Publication:Chemico-biological interactions
Keywords:Acetylcholinesterase;  Alzheimer;  inhibition;  isatin;  neurodegenerative diseases;  organophosphorus;  reactivators; 
PMID:40516590 Category: Date Added:2025-06-15
Dept Affiliation: CHEMBIOCHEM
1 Institute of Chemical, Biological, Radiological and Nuclear Defense (IDQBRN), Brazilian Army Technological Center (CTEx), Avenida das Américas 28705, 23020-470, Rio de Janeiro, RJ, Brazil; Laboratory of Molecular Modeling Applied to Chemical and Biological Defense (LMACBD), Military Institute of Engineering (IME), Praça General Tibúrcio 80, 22290-270, Rio de Janeiro, RJ, Brazil. Electronic address: cristina.munique@eb.mil.br.
2 Laboratory of Molecular Modeling Applied to Chemical and Biological Defense (LMACBD), Military Institute of Engineering (IME), Praça General Tibúrcio 80, 22290-270, Rio de Janeiro, RJ, Brazil. Electronic address: amanda.moraes@ime.eb.br.
3 Medical Course, Souza Marques College (FSM), Rio de Janeiro, RJ, Brazil. Electronic address: marianabalthar@gmail.com.
4 Institute of Chemical, Biological, Radiological and Nuclear Defense (IDQBRN), Brazilian Army Technological Center (CTEx), Avenida das Américas 28705, 23020-470, Rio de Janeiro, RJ, Brazil. Electronic address: anabeatriz.correa@eb.mil.br.
5 Department of Chemistry and Biochemistry, Concordia University, Montreal, QC, Canada. Electronic address: dipanjan.bhattacharyya@concordia.ca.
6 Laboratory Roderick A. Barnes, Walter Mors Institute of Research on Natural Products (IPPN), Federal University of Rio de Janeiro (UFRJ), CCS, Bloco H, 21941-902, Rio de Janeiro, RJ, Brazil. Electronic address: abcsimas@ippn.ufrj.br.
7 Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 50003, Hradec Kralove, Czech Republic. Electronic address: kamil.kuca@uhk.cz.
8 Department of Chemistry and Biochemistry, Concordia University, Montreal, QC, Canada. Electronic address: pat.forgione@concordia.ca.
9 Laboratory of Molecular Modeling Applied to Chemical and Biological Defense (LMACBD), Military Institute of Engineering (IME), Praça General Tibúrcio 80, 22290-270, Rio de Janeiro, RJ, Brazil; Center for Basic and Applied Research, Faculty of Informatics and Management, University of Hradec Kralove, 50003 Hradec Kralove, Czech Republic. Electronic address: tanos@ime.eb.br.
10 Institute of Chemical, Biological, Radiological and Nuclear Defense (IDQBRN), Brazilian Army Technological Center (CTEx), Avenida das Américas 28705, 23020-470, Rio de Janeiro, RJ, Brazil. Electronic address: samir.cavalcante@eb.mil.br.
11 Agency for Management and Technological Innovation (AGITEC), Brazilian Army Department of Science and Technology, Avenida das Américas 28705, 23020-470, Rio de Janeiro, RJ, Brazil. Electronic address: kitagawa.daniel@eb.mil.br.

Description:

Given the recent deployment of nerve agents as a method of warfare and in targeted assassinations, the development of robust, broad-spectrum medical countermeasures is essential. Our research group has synthesized isatin-pyridine oxime hybrids that have previously demonstrated the ability to rescue Electrophorus eel acetylcholinesterase (EeAChE) inhibited by nerve agent surrogates. In this work, we investigate the in vitro AChE inhibitory properties of these hybrids, estimating their IC50. Compounds 14 and 15 evidenced inhibitiory ability (226.4 and 24.7 µM of IC50, respectively), and this last was similar to compound reference pyridostigmine bromide, the only reported drug used as prophylactic measure for nerve agent exposure. Results suggest promisor dual-functional compounds for nerve agent prophylaxis and the reactivation of enzyme catalytic activity.





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