Browse Items · NEOMED Bibliography Database

Serotonin 5-HT6 receptor antagonists for the treatment of Alzheimer's disease.

Recently, the serotonin 5-HT(6) receptor has been identified as a drug target for attenuating cognitive deficits associated with Alzheimer's disease (AD). Additionally, this receptor may also play a role in schizophrenia, anxiety and obesity. Reports…

Tags: 2008, Alzheimer Disease/*drug therapy, Current topics in medicinal chemistry, Geldenhuys Werner J, Humans, Molecular Structure, Nootropic Agents/chemistry/*therapeutic use, Receptors, Serotonin Antagonists/chemistry/*therapeutic use, Serotonin/*metabolism, Van der Schyf Cornelis J

Novel multifunctional anti-Alzheimer drugs with various CNS neurotransmitter targets and neuroprotective moieties.

Traditionally, drug design programs are focused on optimizing the specificity of lead compounds against a carefully selected drug target. Disappointingly, this approach to discover a "magic bullet" drug has not met with the expected success for CNS…

Role of serotonin in Alzheimer's disease: a new therapeutic target?

Mounting evidence accumulated over the past few years indicates that the neurotransmitter serotonin plays a significant role in cognition. As a drug target, serotonin receptors have received notable attention due in particular to the role of several…

Tags: 2011, Alzheimer Disease/*drug therapy/*metabolism, Alzheimer's Disease – Drug Therapy, Alzheimer's Disease – Metabolism, Animals, Cell Surface – Metabolism, Clinical Trials, Clinical Trials as Topic, CNS drugs, Drug Evaluation, Geldenhuys Werner J, Humans, Preclinical, Receptors, Serotonin – Pharmacodynamics, Serotonin – Therapeutic Use, Serotonin/*metabolism, Serotonin/*pharmacology/*therapeutic use, Van der Schyf Cornelis J

Oxidative stress and Alzheimer's disease: dietary polyphenols as potential therapeutic agents.

Oxidative stress has been strongly implicated in the pathophysiology of neurodegenerative disorders such as Alzheimer's disease (AD). In recent years, antioxidants - especially those of dietary origin - have been suggested as possible agents useful…

Tags: 2010, Alzheimer Disease/*physiopathology/*therapy, Animals, Antioxidants/*administration & dosage/chemistry/pharmacology, Bishayee Anupam, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Expert review of neurotherapeutics, Flavonoids/*administration & dosage/chemistry/pharmacology, Geldenhuys Werner J, Humans, Mitochondria/drug effects/physiology, NEOMED College of Pharmacy, Neurodegenerative Diseases/physiopathology, Oxidative Stress/drug effects/*physiology, Phenols/*administration & dosage/chemistry/pharmacology, Polyphenols, Van der Schyf Cornelis J

The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.

The serotonin 6 receptor is attracting attention as an etiological contributor in cognition deficits in diseases such as Alzheimer's disease, anxiety/depression and schizophrenia. In this review, we discuss the role of this recently discovered G…

Tags: 2009, Alzheimer Disease/*complications, Animals, Biological, Cognition Disorders/*drug therapy/*etiology, Drug Design, Expert review of neurotherapeutics, Geldenhuys Werner J, Humans, Models, Receptors, Serotonin Antagonists/chemistry/*therapeutic use, Serotonin/*metabolism, Structure-Activity Relationship, Van der Schyf Cornelis J

Designing drugs with multi-target activity: the next step in the treatment of neurodegenerative disorders.

INTRODUCTION: Neurodegenerative diseases have had devastating effects on patients' quality of life. These complex diseases have several pathways that are affected to initiate cell death. Current therapies, designed to address only a single target,…

Tags: *Drug Design, 2013, Central Nervous System Diseases/*drug therapy, Clinical Trials as Topic, Expert opinion on drug discovery, Geldenhuys Werner J, Humans, Neurodegenerative Diseases/*drug therapy, Neuroprotective Agents/*chemistry/therapeutic use, Van der Schyf Cornelis J

In vivo brain microdialysis: advances in neuropsychopharmacology and drug discovery.

INTRODUCTION: Microdialysis is an important in vivo sampling technique, useful in the assay of extracellular tissue fluid. The technique has both pre-clinical and clinical applications but is most widely used in neuroscience. The in vivo…

Tags: 2011, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Expert opinion on drug discovery, Geldenhuys Werner J, Gudelsky Gary A, Klein Jochen, Meshul Charles K, NEOMED College of Pharmacy, Van der Schyf Cornelis J

Curcumin and neurodegenerative diseases: a perspective.

INTRODUCTION: Curcumin, a dietary polyphenol found in the curry spice turmeric, possesses potent antioxidant and anti-inflammatory properties and an ability to modulate multiple targets implicated in the pathogenesis of chronic illness. Curcumin has…

Tags: 2012, Animals, Bishayee Anupam, Carroll Richard T, Curcumin/adverse effects/pharmacokinetics/*pharmacology/*therapeutic use, Darvesh Altaf S, Department of Pharmaceutical Sciences, Drug Evaluation, Expert opinion on investigational drugs, Geldenhuys Werner J, Humans, NEOMED College of Pharmacy, Neurodegenerative Diseases/*drug therapy/metabolism, Neuroprotective Agents/adverse effects/pharmacokinetics/*pharmacology/*therapeutic use, Novotny Nicholas A, Oxidative Stress/drug effects, Preclinical, Van der Schyf Cornelis J

The emergence of designed multiple ligands for neurodegenerative disorders.

The incidence of neurodegenerative diseases has seen a constant increase in the global population, and is likely to be the result of extended life expectancy brought about by better health care. Despite this increase in the incidence of…

Tags: *Drug Design, *Ligands, 2011, Amyloid beta-Peptides/metabolism, Antiparkinson Agents/therapeutic use, Carroll Richard T, Clinical Trials as Topic, Geldenhuys Werner J, Humans, Molecular Structure, Neurodegenerative Diseases/*drug therapy, Neuroprotective Agents/*therapeutic use, Progress in neurobiology, Van der Schyf Cornelis J, Youdim Moussa B H

Polycyclic compounds: ideal drug scaffolds for the design of multiple mechanism drugs?

Recently there has been a resurging interest in developing multi-functional drugs to treat diseases with complex pathological mechanisms. Such drug molecules simultaneously target multiple etiologies that have been found to be important modulators in…

Tags: *Drug Design, 2009, Adamantane/chemistry/pharmacology, Animals, Central Nervous System Diseases/*drug therapy, Geldenhuys Werner J, Humans, Molecular Structure, Neuroprotective Agents/chemistry/*pharmacology/therapeutic use, Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, Polycyclic Compounds/*chemistry/pharmacology/therapeutic use, Psychotropic Drugs/chemistry/*pharmacology/therapeutic use, Quantitative Structure-Activity Relationship, Van der Schyf Cornelis J

Development and validation of an LC-MS/MS method for determination of the L-type voltage-gated calcium channel/NMDA receptor antagonist NGP1-01 in mouse serum.

NGP1-01 (8-benzylamino-8,11-oxapentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecane) is a heterocyclic cage compound with multifunctional calcium channel blocking activity that has been demonstrated to be neuroprotective in several neurodegenerative…

3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (sigma1) receptor.

Pentacycloundecylamine (PCU) derived compounds have been shown to be promising lead structures for the development of novel drug candidates aimed at a variety of neurodegenerative and psychiatric diseases. Here we show for the first time a 3D…

Tags: *Quantitative Structure-Activity Relationship, 2013, Amines/*chemistry/metabolism, Aza Compounds/chemistry, Binding Sites, Bioorganic & medicinal chemistry letters, Geldenhuys Werner J, Kinetics, Malan Sarel F, Molecular Docking Simulation, Novotny Nicholas, Protein Binding, Protein Structure, Receptors, sigma/*chemistry/metabolism, Tertiary, Van der Schyf Cornelis J

Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.

A series of compounds related to piperine and antiepilepsirine was screened in a monoamine oxidase A and B assay. Piperine is an alkaloid from the source plant of both black and white pepper grains, Piper nigrum. Piperine has been shown to have a…

A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.

Monoamine oxidase B (MAO-B) inhibitors are used to treat Parkinson's disease. In this study, we searched for novel MAO-B inhibitors using a scaffold hopping approach based on our experience with the thiazolidinedione (TZD) class of compounds as MAO-B…

Tags: *Monoamine Oxidase/chemistry/metabolism, 2012, Benzofurans/chemistry/pharmacology, Bioorganic & medicinal chemistry letters, Carroll Richard T, Enzyme Activation/drug effects, Flavonoids/chemistry/pharmacology, Funk Max O, Geldenhuys Werner J, Humans, Inhibitory Concentration 50, Models, Molecular, Molecular Structure, Monoamine Oxidase Inhibitors/*chemistry/*pharmacology, Protein Binding/drug effects, Small Molecule Libraries, Structure-Activity Relationship, Van der Schyf Cornelis J

Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.

Parkinson's disease is a severe debilitating neurodegenerative disorder. Recently, it was shown that the peroxisome proliferating-activator receptor-gamma agonist pioglitazone protected mice from

Tags: 2010, Bioorganic & medicinal chemistry letters, Carroll Richard T, Darvesh Altaf S, Department of Pharmaceutical Sciences, Funk Max O, Geldenhuys Werner J, Models, Molecular, Monoamine Oxidase Inhibitors/chemistry/*pharmacology, Monoamine Oxidase/*drug effects, NEOMED College of Pharmacy, Structure-Activity Relationship, Van der Schyf Cornelis J

Structure-activity relationships of pentacycloundecylamines at the

Prompted by our interest in neuroprotective agents with multiple mechanisms of action, we assessed the structure-activity relationship of a series of pentacycloundecylamine derivatives previously shown to have both L-type calcium channel blocking…

Multimodal drugs and their future for Alzheimer's and Parkinson's disease.

This chapter discusses the rationale for developing multimodal or multifunctional drugs (also called designed multiple ligands or DMLs) aimed at disease-modifying treatment strategies for the most common neurodegenerative diseases Alzheimer's and…

Tags: 2011, Alzheimer Disease/*drug therapy/*enzymology/prevention & control, Animals, Combined Modality Therapy/*methods, Forecasting, Geldenhuys Werner J, Humans, International review of neurobiology, Monoamine Oxidase Inhibitors/*pharmacology/therapeutic use, Parkinson Disease/*drug therapy/*enzymology/prevention & control, Van der Schyf Cornelis J

Methyl Yellow: A Potential Drug Scaffold for Parkinson's Disease.

Parkinson's disease (PD) is an age-related neurodegenerative disease affecting movement. To date, there are no currently available therapeutic agents which can prevent or slow disease progression. Here, we evaluated an azobenzene derivative, methyl…

Tags: *MAO-B inhibitor, *methyl yellow, *MPTP mouse model, *Parkinson's disease, *TMRM, 2014, Chembiochem : a European journal of chemical biology, Dluzen Dean E, Geldenhuys Werner J, Kochi Akiko, Lim Mi Hee, Lin Li, Sutariya Vijaykumar, Van der Schyf Cornelis J

Synthesis and Biological Evaluation of Pentacycloundecylamines and Triquinylamines as Voltage-Gated Calcium Channel Blockers.

Preclinical studies for neurodegenerative diseases have shown a multi-targeted approach to be successful in the treatment of these complex disorders with several pathoetiological pathways. Polycyclic compounds, such as NGP1-01 (7a), have demonstrated…

Browse Items (19 total)