Synthesis of novel aryl-substituted 2-aminopyridine derivatives by the cascade reaction of 1,1-enediamines with vinamidinium salts to develop novel anti-Alzheimer agents.

Authors: Loori, Sama¹ (AUTHOR), Pourtaher, Hormoz¹ (AUTHOR), Mehranpour, Abdolmohammad¹ (AUTHOR) ammehranpour@hotmail.com, Hasaninejad, Alireza¹ (AUTHOR), Eftekharian, Mohammadreza² (AUTHOR), Iraji, Aida^3,4 (AUTHOR) iraji@sums.ac.ir

Source: Scientific Reports. 6/14/2024, Vol. 14 Issue 1, p1-21. 21p.

Subject Terms: *TACRINE, *AMINOPYRIDINES, *ALZHEIMER'S disease, *MOLECULAR dynamics, *DIMETHYL sulfoxide, *SALTS

Tailored Melatonin- and Donepezil-Based Hybrids Targeting Pathognomonic Changes in Alzheimer's Disease: An In Vitro and In Vivo Investigation.

Authors: Mihaylova, Rositsa¹ (AUTHOR) rmihaylova@pharmfac.mu-sofia.bg, Angelova, Violina T.¹ (AUTHOR) V.stoyanova@pharmfac.mu-sofia.bg, Tchekalarova, Jana² (AUTHOR) didiatanasova7@gmail.com, Atanasova, Dimitrinka^2,3 (AUTHOR) Ivanova.petya91@gmail.com, Ivanova, Petja² (AUTHOR), Simeonova, Rumyana¹ (AUTHOR) rsimeonova@pharmfac.mu-sofia.bg

Source: International Journal of Molecular Sciences. Jun2024, Vol. 25 Issue 11, p5969. 19p.

Subject Terms: *ALZHEIMER'S disease, *TACRINE, *SCOPOLAMINE, *ACUTE toxicity testing, *DONEPEZIL, *ENZYME-linked immunosorbent assay, *CARDIOTONIC agents, *NEUROPROTECTIVE agents, *SINGLE molecules

Design, Synthesis and Molecular Modeling Study of Radiotracers Based on Tacrine and Its Derivatives for Study on Alzheimer's Disease and Its Early Diagnosis.

Authors: Koźmiński, Przemysław¹, p.kozminski@ichtj.waw.pl, Gniazdowska, Ewa¹, p.kozminski@ichtj.waw.pl

Source: Applied Sciences (2076-3417); Apr2024, Vol. 14 Issue 7, p2827, 18p

A Sustainable Synthetic Approach to Tacrine and Cholinesterase Inhibitors in Deep Eutectic Solvents under Aerobic Conditions.

Authors: Cicco, Luciana¹ (AUTHOR) filippo.perna@uniba.it, Perna, Filippo Maria¹ (AUTHOR), Capriati, Vito¹ (AUTHOR) luciana.cicco@uniba.it, Vitale, Paola¹ (AUTHOR)

Source: Molecules. Mar2024, Vol. 29 Issue 6, p1399. 10p.

Subject Terms: *CHOLINESTERASE inhibitors, *TACRINE, *VOLATILE organic compounds, *DRUG development, *SUSTAINABLE chemistry, *COPPER catalysts

Multi-targeted benzylpiperidine–isatin hybrids: Design, synthesis, biological and in silico evaluation as monoamine oxidases and acetylcholinesterase inhibitors for neurodegenerative disease therapies.

Authors: Negi, Nikita¹, Ayyannan, Senthil R.², Tripathi, Rati K. P.³, rati.tripathi.phe09@iitbhu.ac.in

Source: Journal of Computer-Aided Molecular Design; 2/28/2025, Vol. 39 Issue 1, p1-31, 31p

Synthesis, biological evaluation, and computational studies of N-benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity.

Authors: Al-Rifai, Nafisah M.¹ (AUTHOR) nafisah.rifai@gju.edu.jo, Al-Khalileh, Nemeh M.² (AUTHOR), Zahra, Jalal A.² (AUTHOR), El-Barghouthi, Musa I.³ (AUTHOR), Darras, Fouad H.⁴ (AUTHOR)

Source: Journal of Enzyme Inhibition & Medicinal Chemistry. Dec2023, Vol. 38 Issue 1, p1-12. 12p.

Subject Terms: *CURCUMINOIDS, *TACRINE, *CHEMICAL synthesis, *ANTIOXIDANTS, *CHEMICAL libraries

Pd/Co2(CO)8‐mediated bi‐metallic catalysis: Facile synthesis of pharmacologically relevant novel tacrine analogues.

Authors: Babu, Aravinda¹ (AUTHOR), Sunil, K.¹ (AUTHOR) sunilk999@gmail.com, Sajith, Ayyiliath Meleveetil¹ (AUTHOR), Muthipeedika, Nibin Joy² (AUTHOR) mnibinjoy@gmail.com, Santra, Sougata² (AUTHOR), Zyryanov, Grigory V.^2,3 (AUTHOR)

Source: Journal of Heterocyclic Chemistry. Nov2023, Vol. 60 Issue 11, p1911-1917. 7p.

Subject Terms: *TACRINE, *CATALYSIS, *COBALT, *AMIDES, *ESTERS

Selenylated Analogs of Tacrine: Synthesis, In Silico and In Vitro Studies of Toxicology and Antioxidant Properties.

Authors: do Sacramento, Manoela¹, Morais, Roberto B.¹, Silveira Lima, Ariana¹, Zugno, Giuliana P.², de Oliveira, Renata L.², da Costa, Gabriel P.¹, Savegnago, Lucielli², luciellisavegnago@uyahoo.com.br, Alves, Diego¹, diego.alves@ufpel.edu.br

Source: Chemistry - An Asian Journal; Oct2024, Vol. 19 Issue 19, p1-8, 8p

Inhibition of Acetylcholinesterase by Novel Lupinine Derivatives.

Authors: Schepetkin, Igor A.¹ (AUTHOR) igor@montana.edu, Nurmaganbetov, Zhangeldy S.^2,3 (AUTHOR) nzhangeldy@yandex.ru, Fazylov, Serik D.² (AUTHOR) iosu8990@mail.ru, Nurkenov, Oralgazy A.² (AUTHOR) nurkenov_oral@mail.ru, Khlebnikov, Andrei I.⁴ (AUTHOR) aikhl@chem.org.ru, Seilkhanov, Tulegen M.⁵ (AUTHOR) tseilkhanov@mail.ru, Kishkentaeva, Anarkul S.² (AUTHOR) anar_kish@mail.ru, Shults, Elvira E.⁶ (AUTHOR), Quinn, Mark T.¹ (AUTHOR) mquinn@montana.edu

Source: Molecules. Apr2023, Vol. 28 Issue 8, p3357. 15p.

Subject Terms: *TACRINE, *ACETYLCHOLINESTERASE, *FISHER discriminant analysis, *ALZHEIMER'S disease, *TRIAZOLE derivatives, *MOLECULAR docking

Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer's disease.

Authors: Przybyłowska, Maja¹, Dzierzbicka, Krystyna¹ krydzier@pg.edu.pl, Kowalski, Szymon², Demkowicz, Sebastian¹, Daśko, Mateusz³, Inkielewicz-Stepniak, Iwona² iinkiel@gumed.edu.pl

Source: Journal of Enzyme Inhibition & Medicinal Chemistry. 2022, Vol. 37 Issue 1, p1012-1022. 11p.

Subject Terms: *TACRINE, *ALZHEIMER'S disease, *BIOSYNTHESIS, *DRUG derivatives, *MOLECULAR docking

Design, synthesis, and evaluation of chalcone-Vitamin E-donepezil hybrids as multi-target-directed ligands for the treatment of Alzheimer's disease.

Authors: Zhipei Sang^1,2 sangzhipei@126.com, Qing Song², Zhongcheng Cao², Yong Deng², Li Zhang³ zl.glx.gjq@163.com

Source: Journal of Enzyme Inhibition & Medicinal Chemistry. 2022, Vol. 37 Issue 1, p69-85. 17p.

Subject Terms: *TACRINE, *ALZHEIMER'S disease, *CHALCONE, *LIGANDS (Biochemistry), *BLOOD-brain barrier

Design and synthesis of new indole drug candidates to treat Alzheimer's disease and targeting neuro-inflammation using a multi-target-directed ligand (MTDL) strategy.

Authors: Lamie, Phoebe F.¹ dr.feby@pharm.bsu.edu.eg, Abdel-Fattah, Maha M.², Philoppes, John N.¹

Source: Journal of Enzyme Inhibition & Medicinal Chemistry. 2022, Vol. 37 Issue 1, p2660-2678. 19p.

Subject Terms: *ALZHEIMER'S disease, *TACRINE, *INDOLE, *MOLECULAR docking, *CELL lines

SYNTHESIS AND CHARACTERIZATION OF SCHIFF BASES CONTAINING 1,2,3-TRIAZOLE UNIT: PHOTOPHYSICAL AND ACETYL CHOLINE (AChE) INHIBITORY PROPERTIES.

Authors: Şahin, İ.¹ (AUTHOR) irfansahin@ksu.edu.tr

Source: Journal of Structural Chemistry. Nov2022, Vol. 63 Issue 11, p1787-1796. 10p.

Subject Terms: *TACRINE, *ALZHEIMER'S disease, *CHEMICAL synthesis, *SCHIFF bases, *CHOLINE, *GALANTHAMINE

Conjugates of Tacrine with Aminomethylidene-Substituted Malonates: Synthesis and Biological Evaluation.

Authors: Grishchenko, M. V.¹, Elkina, N. A.¹, Makhaeva, G. F.², Burgart, Ya. V.¹, Boltneva, N. P.², Rudakova, E. V.², Shchegolkov, E. V.¹, Kovaleva, N. V.², Serebryakova, O. G.², Saloutin, V. I.¹ saloutin@ios.uran.ru

Source: Russian Journal of General Chemistry. Nov2022, Vol. 92 Issue 11, p2259-2266. 8p.

Subject Terms: *TACRINE, *BIOSYNTHESIS, *MALONATES, *ALZHEIMER'S disease, *PROPIDIUM iodide, *ACETYLCHOLINESTERASE inhibitors, *MUSCARINIC receptors

Tacrine Derivatives Containing an Antioxidant Moiety.

Authors: Serkov, I. V.¹ (AUTHOR) serkoviv@mail.ru, Proshin, A. N.¹ (AUTHOR), Kovaleva, N. V.¹ (AUTHOR), Boltneva, N. P.¹ (AUTHOR), Rudakova, E. V.¹ (AUTHOR), Makhaeva, G. F.¹ (AUTHOR), Bachurin, S. O.¹ (AUTHOR)

Source: Doklady Chemistry. Sep2022, Vol. 506 Issue 1, p190-195. 6p.

Subject Terms: *TACRINE, *MOIETIES (Chemistry), *ANTIOXIDANTS, *CHOLINESTERASES, *ACETYLCHOLINESTERASE, *VANILLIN

New compounds from heterocyclic amines scaffold with multitarget inhibitory activity on Aβ aggregation, AChE, and BACE1 in the Alzheimer disease.

Authors: García Marín, Iohanan Daniel¹ (AUTHOR), Camarillo López, Raúl Horacio^1,2 (AUTHOR), Martínez, Oscar Aurelio¹ (AUTHOR), Padilla-Martínez, Itzia Irene³ (AUTHOR), Correa-Basurto, José⁴ (AUTHOR), Rosales-Hernández, Martha Cecilia¹ (AUTHOR) marcrh2002@yahoo.com.mx

Source: PLoS ONE. 6/3/2022, Vol. 17 Issue 6, p1-20. 20p.

Subject Terms: *ALZHEIMER'S disease, *TACRINE, *HETEROCYCLIC compounds, *AMINES, *GIBBS' free energy, *NEUROFIBRILLARY tangles, *SECRETASE inhibitors

Design, Synthesis, and Evaluation of Novel 2 H -Benzo[b][1,4]thiazin-3(4 H)-one Derivatives as New Acetylcholinesterase Inhibitors.

Authors: Haji Ali, Sazan^1,2 (AUTHOR) dosmaniye@anadolu.edu.tr, Osmaniye, Derya^2,3 (AUTHOR) bnsaglik@anadolu.edu.tr, Sağlık, Begüm Nurpelin^2,3 (AUTHOR) serkanlevent@anadolu.edu.tr, Levent, Serkan^2,3 (AUTHOR) yozkay@anadolu.edu.tr, Özkay, Yusuf^2,3 (AUTHOR), Kaplancıklı, Zafer Asım² (AUTHOR) zakaplan@anadolu.edu.tr

Source: Molecules. Apr2022, Vol. 27 Issue 7, p2121-2121. 18p.

Subject Terms: *TACRINE, *ACETYLCHOLINESTERASE inhibitors, *BINDING sites, *ALZHEIMER'S disease, *BLOOD-brain barrier, *ANTIOXIDANTS, *NEURODEGENERATION, *KINASE inhibitors

Company/Entity: NATIONAL Institutes of Health (U.S.)

Synthesis of conjugates of ipidacrine with oxa/azaheterocycles and their potential as agents for the treatment of Alzheimer's disease.

Authors: Khudina, O. G.¹ (AUTHOR), Grishchenko, M. V.¹ (AUTHOR), Makhaeva, G. F.² (AUTHOR), Burgart, Ya. V.¹ (AUTHOR), Boltneva, N. P.² (AUTHOR), Goryaeva, M. V.¹ (AUTHOR), Kovaleva, N. V.² (AUTHOR), Rudakova, E. V.² (AUTHOR), Bachurin, S. O.² (AUTHOR), Saloutin, V. I.¹ (AUTHOR) saloutin@ios.uran.ru

Source: Russian Chemical Bulletin. Jun2024, Vol. 73 Issue 6, p1755-1765. 11p.

Subject Terms: *ALZHEIMER'S disease, *TACRINE, *COUMARINS, *ESTER derivatives, *BUTYRYLCHOLINESTERASE, *NUCLEAR magnetic resonance spectroscopy, *COUMARIN derivatives

Competitive Inhibition and Synergistic Effects of Nutraceutical and Metabolite Molecules on Anti-Acetylcholinesterase Activity.

Authors: Girgin, Munteha¹, Tarbiat, Shirin¹, Isik, Sevim^2,3, Kantarci-Carsibasi, Nigar¹, nigar.carsibasi@uskudar.edu.tr

Source: Journal of the Turkish Chemical Society Section A: Chemistry; 2024, Vol. 11 Issue 2, p575-583, 9p

Bis(7)-harmine derivatives as potential multi-target anti-Alzheimer agents.

Authors: Du, Hongtao, Ma, Fang, Cao, Yuanyuan, Bai, Miaoyan, Gao, Xinyi, Yang, Ziyi, Xu, Yang, Yan, Yan

Source: Frontiers in Chemistry; 2025, p1-14, 14p

Subject Terms: ALZHEIMER'S disease, NUCLEAR magnetic resonance, MONOAMINE oxidase, CYTOTOXINS, PEPTIDES, TACRINE