1
40
2
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Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1016/j.bmcl.2012.09.056" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2012.09.056</a>
Pages
7183–7188
Issue
23
Volume
22
Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
A name given to the resource
Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.
Publisher
An entity responsible for making the resource available
Bioorganic & medicinal chemistry letters
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-12
Subject
The topic of the resource
Alkaloids/*chemistry/isolation & purification/pharmacology; Animals; Benzodioxoles/*chemistry/isolation & purification/pharmacology; Binding Sites; Blood-Brain Barrier/drug effects; Bovine/metabolism; Cattle; Humans; Hydrogen Bonding; Molecular Docking Simulation; Monoamine Oxidase Inhibitors/*chemistry/isolation & purification/pharmacology; Monoamine Oxidase/*chemistry/metabolism; Parkinson Disease/metabolism/pathology; Piper nigrum/*chemistry; Piperidines/*chemistry/isolation & purification/pharmacology; Polyunsaturated Alkamides/*chemistry/isolation & purification/pharmacology; Protein Binding; Protein Structure; Serum Albumin; Tertiary
Creator
An entity primarily responsible for making the resource
Al-Baghdadi Osamah B; Prater Natalie I; Van der Schyf Cornelis J; Geldenhuys Werner J
Description
An account of the resource
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 wide range of activity, including MAO inhibitory activity. The z-factor for the screening assay was found to be greater than 0.8 for both assays. Notably, the compounds tested were selective towards MAO-B, with the most potent compound having an IC(50) of 498 nM. To estimate blood-brain barrier (BBB) permeability, we used a PAMPA assay, which suggested that the compounds are likely to penetrate the BBB. A fluorescent bovine serum albumin (BSA) high-throughput screening (HTS) binding assay showed an affinity of 8 muM for piperine, with more modest binding for other test compounds. Taken together, the data described here may be useful in gaining insight towards the design of selective MAO-B inhibitory compounds devoid of MAO-A activity.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.1016/j.bmcl.2012.09.056" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2012.09.056</a>
Rights
Information about rights held in and over the resource
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2012
Al-Baghdadi Osamah B
Alkaloids/*chemistry/isolation & purification/pharmacology
Animals
Benzodioxoles/*chemistry/isolation & purification/pharmacology
Binding Sites
Bioorganic & medicinal chemistry letters
Blood-Brain Barrier/drug effects
Bovine/metabolism
Cattle
Geldenhuys Werner J
Humans
Hydrogen Bonding
Molecular Docking Simulation
Monoamine Oxidase Inhibitors/*chemistry/isolation & purification/pharmacology
Monoamine Oxidase/*chemistry/metabolism
Parkinson Disease/metabolism/pathology
Piper nigrum/*chemistry
Piperidines/*chemistry/isolation & purification/pharmacology
Polyunsaturated Alkamides/*chemistry/isolation & purification/pharmacology
Prater Natalie I
Protein Binding
Protein Structure
Serum Albumin
Tertiary
Van der Schyf Cornelis J
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.3390/molecules22060917" target="_blank" rel="noreferrer noopener">http://doi.org/10.3390/molecules22060917</a>
Issue
6
Volume
22
Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
A name given to the resource
Exploring Adenosine Receptor Ligands: Potential Role in the Treatment of Cardiovascular Diseases.
Publisher
An entity responsible for making the resource available
Molecules (Basel, Switzerland)
Date
A point or period of time associated with an event in the lifecycle of the resource
2017
2017-06
Subject
The topic of the resource
Humans; Animals; Protein Binding; Signal Transduction; atherosclerosis; *Drug Discovery; *Ligands; Adenosine/metabolism; cardiac death; Cardiovascular Diseases/drug therapy/metabolism; Cardiovascular System/metabolism; Hydrogen Bonding; Molecular Structure; myocardial infarction; Structure-Activity Relationship; vascular tone; Receptors; Models; Molecular; Purinergic P1/*chemistry/*metabolism
Creator
An entity primarily responsible for making the resource
Geldenhuys Werner J; Hanif Ahmad; Yun June; Nayeem Mohammed A
Description
An account of the resource
Cardiovascular diseases remain the number one diseases affecting patients' morbidity and mortality. The adenosine receptors are G-protein coupled receptors which have been of interest for drugs target for the treatment of multiple diseases ranging from cardiovascular to neurological. Adenosine receptors have been connected to several biological pathways affecting the physiology and pathology of the cardiovascular system. In this review, we will cover the different adenosine receptor ligands that have been identified to interact with adenosine receptors and affect the vascular system. These ligands will be evaluated from clinical as well as medicinal chemistry perspectives with more emphasis on how structural changes in structure translate into ligand potency and efficacy. Adenosine receptors represent a novel therapeutic target for development of treatment options treating a wide variety of diseases, including vascular disease and obesity.
Identifier
An unambiguous reference to the resource within a given context
<a href="http://doi.org/10.3390/molecules22060917" target="_blank" rel="noreferrer noopener">10.3390/molecules22060917</a>
Rights
Information about rights held in and over the resource
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
*drug discovery
*Ligands
2017
Adenosine/metabolism
Animals
Atherosclerosis
Cardiac death
Cardiovascular Diseases/drug therapy/metabolism
Cardiovascular System/metabolism
Department of Integrative Medical Sciences
Geldenhuys Werner J
Hanif Ahmad
Humans
Hydrogen Bonding
Models
Molecular
Molecular Structure
Molecules (Basel, Switzerland)
myocardial infarction
Nayeem Mohammed A
NEOMED College of Medicine
Protein Binding
Purinergic P1/*chemistry/*metabolism
Receptors
Signal Transduction
Structure-Activity Relationship
Vascular tone
Yun June