[HTML][HTML] Quinones as neuroprotective agents

Á Cores, N Carmona-Zafra, J Clerigué, M Villacampa… - Antioxidants, 2023 - mdpi.com
Quinones can in principle be viewed as a double-edged sword in the treatment of
neurodegenerative diseases, since they are often cytoprotective but can also be cytotoxic …

BACE1 Inhibitors for Alzheimer's Disease: Current Challenges and Future Perspectives

JRM Coimbra, R Resende, J Custódio… - Journal of …, 2024 - content.iospress.com
Disease-modifying therapies (DMT) for Alzheimer's disease (AD) are highly longed-for. In
this quest, antiamyloid therapies take center stage supported by genetic facts that highlight …

Rottlerin renders a selective and highly potent CYP2C8 inhibition to impede EET formation for implication in cancer therapy

D Manhas, S Bhatt, G Rai, V Kumar, S Bharti… - Chemico-biological …, 2023 - Elsevier
CYP2C8 is a crucial CYP isoform responsible for the metabolism of xenobiotics and
endogenous molecules. CYP2C8 converts arachidonic acid to epoxyeicosatrienoic acids …

Identification of Azelastine and Carvedilol as Cholinesterase Inhibitors via Structure‐Based Virtual Screening of FDA‐approved Drugs

M Sharma, S Thakur, HR Jadhav… - ChemistrySelect, 2023 - Wiley Online Library
The structure‐based virtual screening (SBVS) has gained immense importance in early drug
discovery. Herein, we report the SBVS‐driven identification of new cholinesterase inhibitors …

Glabridin plays dual action to intensify anti-metastatic potential of paclitaxel via impeding CYP2C8 in liver and CYP2J2/EETs in tumor of an orthotopic mouse model of …

A Jamwal, J Chand, A Dash, S Bhatt, S Dhiman… - Chemico-Biological …, 2023 - Elsevier
In spite of unprecedented advances in modern cancer therapy, there is still a dearth of
targeted therapy to circumvent triple-negative breast cancer (TNBC). Paclitaxel is the front …

EIDD-1931 Treatment Tweaks CYP3A4 and CYP2C8 in Arthritic Rats to Expedite Drug Interaction: Implication in Oral Therapy of Molnupiravir

M Bhardwaj, D Kour, G Rai, S Bhattacharya… - ACS …, 2024 - ACS Publications
EIDD-1931 is the active form of molnupiravir, an orally effective drug approved by the United
States Food and Drug Administration (USFDA) against COVID-19. Pharmacokinetic …

Novel Lawsone–Quinoxaline Hybrids as New Dual Binding Site Acetylcholinesterase Inhibitors

P Suwanhom, T Nualnoi, P Khongkow, V Tipmanee… - ACS …, 2023 - ACS Publications
A new family of lawsone–quinoxaline hybrids was designed, synthesized, and evaluated as
dual binding site cholinesterase inhibitors (ChEIs). In vitro tests revealed that compound 6d …

ADME/PK Insights of Crocetin: A Molecule Having an Unusual Chemical Structure with Druglike Features

D Manhas, S Dhiman, H Kour, D Kour, K Sharma… - ACS …, 2024 - ACS Publications
Crocetin is a promising phyto-based molecule to treat Alzheimer's disease (AD). The
chemical structure of crocetin is incongruent with various standard structural features of CNS …

Design, synthesis, and pharmacological evaluation of indole-piperidine amides as Blood− brain barrier permeable dual cholinesterase and β-secretase inhibitors

R Banoo, VK Nuthakki, BN Wadje, A Sharma… - European Journal of …, 2024 - Elsevier
Heterocyclic compounds play a crucial role in the discovery of therapeutics. Alzheimer's
disease (AD) is an unfathomable sporadic neurodegenerative disorder that involves multiple …

Synthesis of novel rapanone derivatives via organocatalytic reductive C-alkylation: biological evaluation of antioxidant properties, in vivo zebrafish embryo toxicity …

V Mariyappan, G Munuswamy-Ramanujam… - RSC Medicinal …, 2024 - pubs.rsc.org
A biologically crucial natural product rapanone 1 was isolated from Embelia ribes at the
gram scale with excellent purity. Semi-synthetic analogs of 1 semi-synthesized through …