Results 51 to 60 of about 4,342 (172)

Exploring Disulfide Bridge as a Tool to Improve Pioglitazone’s Neuroprotective Potential: Toward the Development of Prolonged‐Acting MAO‐B/PPARγ Modulators

open access: yesChemMedChem, Volume 21, Issue 15, 14 August 2026.
Pioglitazone is an antidiabetic drug acting as a peroxisome proliferator‐activated receptor γ (PPARγ) agonist and later repositioned as a monoamine oxidase B (MAO‐B) inhibitor. Despite promising preclinical premises, it showed a lack of efficacy in clinical trials as a treatment for neurodegenerative diseases.
Filippo Basagni   +12 more
wiley   +1 more source

Design, Synthesis, and Biological Evaluation of Chiral Urea and Thiourea Derivatives as Multitarget‐Directed Anti‐Alzheimer Agents

open access: yesDrug Development Research, Volume 87, Issue 5, August 2026.
ABSTRACT A series of novel chiral urea and thiourea compounds were designed as multitarget‐directed ligands for Alzheimer's disease and evaluated against hAChE, hBChE, and hMAO‐B, with exploratory assessment of HSD10. These chiral compounds were synthesized and fully characterized, and their enantiopurity was confirmed via HPLC.
Sule Erol Gunal   +10 more
wiley   +1 more source

Suppression of Non-Small Cell Lung Cancer Growth and Metastasis by a Novel Small Molecular Activator of RECK

open access: yesCellular Physiology and Biochemistry, 2018
Background/Aims: Reversion-inducing cysteine-rich protein with kazal motifs (RECK) is a novel tumor suppressor gene that is critical for regulating tumor cell invasion and metastasis. The expression of RECK is dramatically down-regulated in human cancers.
Jia Shen   +7 more
doaj   +1 more source

Solid-Contact Potentiometric Sensors Based on Main-Tailored Bio-Mimics for Trace Detection of Harmine Hallucinogen in Urine Specimens

open access: yesMolecules, 2021
All-solid-state potentiometric sensors have attracted great attention over other types of potentiometric sensors due to their outstanding properties such as enhanced portability, simplicity of handling, affordability and flexibility.
Abde El-Galil E. Amr   +4 more
doaj   +1 more source

Multi‐Targeting Ligands as Prospective Therapeutics for Alzheimer's Disease, a Prevalent Neurodegenerative Disorder: Mechanistic Insights, Emerging Targets and Drug Discovery Campaigns

open access: yesMedicinal Research Reviews, Volume 46, Issue 4, Page 1173-1229, July 2026.
ABSTRACT Alzheimer's disease (AD) is a debilitating neurodegenerative condition characterized by progressive cognitive impairment, memory deterioration, and neuronal dysfunction. Its complex pathophysiology involves multiple interlinked processes, including amyloid‐β (Aβ) aggregation, tau hyperphosphorylation, oxidative stress, neuroinflammation ...
Amandeep Thakur   +6 more
wiley   +1 more source

Targeted delivery of harmine to xenografted human pancreatic islets promotes robust cell proliferation

open access: yesScientific Reports, 2022
Type 1 diabetes (T1D) occurs as a consequence of the autoimmune destruction of insulin-producing pancreatic beta (β) cells and commonly presents with insulin deficiency and unregulated glycemic control.
Swati Mishra, Philip R. Streeter
doaj   +1 more source

Preclinical models for evaluating psychedelics in the treatment of major depressive disorder

open access: yesBritish Journal of Pharmacology, Volume 183, Issue 14, Page 3970-3991, July 2026.
Psychedelic drugs have seen a resurgence in interest as a next generation of psychiatric medicines with potential as rapid‐acting antidepressants (RAADs). Despite promising early clinical trials, the mechanisms which underlie the effects of psychedelics are poorly understood.
Laith Alexander   +5 more
wiley   +1 more source

How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition—The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine

open access: yesMolecules, 2020
The β-carboline alkaloid harmine is a potent DYRK1A inhibitor, but suffers from undesired potent inhibition of MAO-A, which strongly limits its application.
Anne Wurzlbauer   +7 more
doaj   +1 more source

Integrative Insights Into DYRK1A From Molecular Function to Therapeutic Advancement

open access: yesChemical Biology &Drug Design, Volume 108, Issue 1, July 2026.
At the center the 3D structure of DYRK1A has been displayed. The dual‐function of DYRK1A involved in cancer and neurodegeneration, i.e., its overexpression drives Down syndrome, neurodegenerative disease etc., and underexpression causes intellectual disability, seizures, etc.
Sampriti Paul   +2 more
wiley   +1 more source

Monoamine Oxidase and Cholinesterase Inhibition Profiles of Semicarbazone and Thiosemicarbazone Derivatives

open access: yesChemistry &Biodiversity, Volume 23, Issue 6, June 2026.
Thiosemicarbazones generally show higher MAO‐B inhibitory potential than their corresponding semicarbazones, and particularly T6 is the most potent, which contains R = H and X = S in its Tail Unit, with an IC50 value of 6.45 µM with SI of 3.6. ABSTRACT Twenty semicarbazone and thiosemicarbazone derivatives (T1–T20) were synthesized and evaluated for ...
Sandeep Bindra   +11 more
wiley   +1 more source

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