Pyrazolone-nicotinic acid derivative (4Z)-4-(2-hydroxybenzylidine)-5-methyl-2-(pyridine-3-ylcarbonyl)-2, 4-dihydro-3H-pyrazole-3-one (IIc) as multitarget inhibitor of neurodegeneration and behavioural impairment in Dementia DOI
Madiha Kanwal, Sadia Sarwar, Humaira Nadeem

et al.

Journal of Pharmacy and Pharmacology, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 14, 2024

Abstract Objective The study was aimed at the synthesis and pharmacological investigation of (4Z)-4-(2-hydroxybenzylidine)-5-methyl-2-(pyridine-3-ylcarbonyl)-2, 4-dihydro-3H-pyrazole-3-one (IIc) in mice model scopolamine-induced neurodegeneration cognition impairment. Methods behavioural studies included Y-Maze Test, Water Morris Novel Object Recognition Test Albino (20–25 g). Scopalamine used as an inducing agent. acetylcholinesterase (AChE) inhibitory assay to assess role test compounds vitro. Crystal Violet Staining (Nissl staining) neuroprotective antiapoptotic effect through quantifying number neurons viability. expression anti-inflammatory enzyme cyclooxygenase-2 (COX-2), cytokine tumour necrotic factor (TNF-α), key transcription producing pro-inflammatory signals nuclear kappa B (P-NFkB), apoptosis marker p-JNK validated enzyme-linked immunosorbent (ELISA) immunohistochemical (IHC) analysis. tested compound reverted cognitive impairment inhibiting inflammation oxidative stress. Key findings We found that IIc improved short-term memory learning behaviour experimental animals. Further into molecular mechanisms showed this manifestation immunomodulatory, antioxidant, consequently, downsizing inflammatory cytokines. These results were further docking Conclusion Finally, we conclude pyrazolone-nicotinic acid derivative reversed deficits, attributed inhibition, neuronal recovery, antioxidant potential, downregulating neuroinflammatory mediators p-NF-kB, TNF-α, COX-2.

Language: Английский

Antioxidants in Anti-Alzheimer's Disease Drug Discovery DOI

Jianan Guo,

Yalan Zhu,

Jia Zhi

et al.

Ageing Research Reviews, Journal Year: 2025, Volume and Issue: 107, P. 102707 - 102707

Published: Feb. 27, 2025

Language: Английский

Citations

1

Design, synthesis, characterization, molecular docking studies, molecular properties, toxicity, and bioactivity score prediction evaluation of novel chalcone-sulfonate hybrid derivatives DOI
Adem Korkmaz

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1286, P. 135597 - 135597

Published: April 18, 2023

Language: Английский

Citations

14

Novel Mannich bases derived from 1,2,4-triazoles: Design, synthesis, characterization, and glutathione S-transferase inhibition properties investigations DOI
Onur Akyıldırım, Hilal Medetalibeyoğlu, Ercan Oğuz

et al.

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1293, P. 136321 - 136321

Published: July 30, 2023

Language: Английский

Citations

14

Recent progresses in natural based therapeutic materials for Alzheimer's disease DOI Creative Commons
Tayebeh Zivari‐Ghader, Ferzane Valioğlu, Aziz Eftekhari

et al.

Heliyon, Journal Year: 2024, Volume and Issue: 10(4), P. e26351 - e26351

Published: Feb. 1, 2024

Alzheimer's disease is a neurological disorder that causes increased memory loss, mood swings, behavioral disorders, and disruptions in daily activities. Polymer scaffolds for the brain have been grown under laboratory, physiological, pathological circumstances because of limitations conventional treatments patients with central nervous system diseases. The blood-brain barrier prevents medications from entering brain, challenging AD treatment. Numerous biomaterials such as biomolecules, polymers, inorganic metals, metal oxide nanoparticles used to transport therapeutic medicines into system. Incorporating biocompatible materials support neurogenesis through combination topographical, pharmacological, mechanical stimuli has also shown promise transfer cells replenish dopaminergic neurons. Components made naturally occurring biodegradable polymers are appropriate regeneration nerve tissue. ability natural-based (biomaterials) promote endogenous cell development after implantation. Also, strategic functionalization polymeric nanocarriers could be employed treating AD. In particular, resolve Aβ aggregation thus help cure disease. Drug moieties can effectively directed by utilizing nano-based systems diverse colloidal carriers, including hydrogels scaffolds. Notably, early investigations employing neural stem yielded promising results, further emphasizing potential advancements this field. Few studies fully leveraged cutting-edge biomaterials. This study provides comprehensive overview prior research, highlighting pivotal role sophisticated drug carriers. It delves various intelligent delivery systems, encompassing pH thermo-triggered mechanisms, lipid nanoparticles, other vectors. discussion synthesizes existing knowledge underscores transformative impact these devising innovative strategies, augmenting current methodologies, shaping new paradigms realm

Language: Английский

Citations

5

In Silico and in Vitro Biological Evaluation of Novel Serial Sulfonate Derivatives on Pancreatic Lipase Activity DOI
Fuat Yetişsin, Adem Korkmaz, Esin Kaya

et al.

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(11)

Published: Sept. 25, 2023

The novel benzothiazole sulfonate hybrid derivatives containing azomethine group were synthesized and characterized using 1 H-NMR, 13 C-NMR, HR-MS analysis. potential enzyme inhibition activities against pancreatic lipase of the screened with in vitro silico methods. IC50 values compounds 5 b (23.89 μM), i (28.87 f (30.13±4.32) found to be more effective inhibitors than orlistat (57.75 μM) studies. Also, binding affinities (-8.7 kcal/mol), (-8.6 (-8.9 kcal/mol) for In addition, absorption distribution, metabolism, excretion properties (ADME), molecular properties, toxicity estimation, bioactivity scores scanned. It was have ability cross brain-blood barrier a, b, c, d. All calculated taken orally as drugs, suitable intestinal tract not carcinogenic, well very strongly bound plasma proteins. Finally, compound observed best inhibitor according

Language: Английский

Citations

13

2-hydrazinobenzothiazole based derivatives: Synthesis, characterization, antifungal, DNA binding and molecular modelling approaches DOI

Nouman,

Manish Rana,

Saiema Ahmedi

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1308, P. 138051 - 138051

Published: March 14, 2024

Language: Английский

Citations

4

Design, synthesis, molecular docking, DFT analysis, dynamics simulation and cytotoxicity evaluation of coumarin derivatives as acetylcholinesterase (AChE) inhibitors against alzheimer's disease DOI

Shivangi Rai,

Vishal Singh, Iqrar Ahmad

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141436 - 141436

Published: Jan. 1, 2025

Language: Английский

Citations

0

Synthesis and biological evaluation of novel Trifluoromethylated Arylidene-hydrazinyl-thiazoles as neuroprotective agents DOI

Ranjana Aggarwal,

Prince Kumar,

Suresh Kumar

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108390 - 108390

Published: March 1, 2025

Language: Английский

Citations

0

A novel, rapid and eco-sustainable approach for the synthesis of novel benzothiazole derivatives as potent urease inhibitors: biological assay, molecular docking, dynamic simulation, DFT and ADMET studies DOI
Billel Belhani, Mohamed Aissaoui, Hacène K’tir

et al.

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1293, P. 136221 - 136221

Published: July 16, 2023

Language: Английский

Citations

4

Discovery of 3-(2-aminobenzo[d]thiazol-5-yl) benzamide derivatives as potent anticancer agents via ROR1 inhibition DOI

Fang Luo,

Jie Liu,

Rongtao Wang

et al.

Bioorganic & Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 117, P. 118011 - 118011

Published: Nov. 20, 2024

Language: Английский

Citations

1