A comprehensive review of multi-target directed ligands in the treatment of Alzheimer’s disease

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 144, P. 107152 - 107152

Published: Jan. 27, 2024

Language: Английский

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Piperazine-2-carboxylic acid derivatives as MTDLs anti-Alzheimer agents: Anticholinesterase activity, mechanistic aspect, and molecular modeling studies

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 142, P. 106916 - 106916

Published: Oct. 21, 2023

Language: Английский

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Study of the Antileishmanial Activity of Novel Guanidine and Hybrid Acridine – Guanidine Compounds

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 117651 - 117651

Published: April 1, 2025

Language: Английский

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Conjugates of amiridine and thiouracil derivatives as effective inhibitors of butyrylcholinesterase with the potential to block β‐amyloid aggregation

Archiv der Pharmazie, Journal Year: 2023, Volume and Issue: 357(2)

Published: Dec. 10, 2023

Abstract New amiridine‐thiouracil conjugates with different substituents in the pyrimidine fragment (R = CH 3 , CF 2 Н, (CF ) H) and spacer lengths ( n 1–3) were synthesized. The rather weakly inhibit acetylcholinesterase (AChE) exhibit high inhibitory activity (IC 50 up to 0.752 ± 0.021 µM) selectivity butyrylcholinesterase (BChE), which increases elongation; lead compounds are 11c 12c 13c . mixed‐type reversible inhibitors of both cholinesterases practically do not structurally related off‐target enzyme carboxylesterase. results molecular docking AChE BChE consistent experiment on inhibition explain structure–activity relationships, including low anti‐AChE anti‐BChE long‐chain conjugates. displace propidium from peripheral anion site (PAS) at level reference compound donepezil, agrees mechanism main mode binding active due interaction moiety PAS. This indicates ability studied block AChE‐induced aggregation β‐amyloid, thereby exerting a disease‐modifying effect. According computer calculations, all synthesized have an ADME profile acceptable for drugs.

Language: Английский

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Meet the Section Editor

Current Neuropharmacology, Journal Year: 2024, Volume and Issue: 22(10), P. 1577 - 1577

Published: April 26, 2024

Language: Английский

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