|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
7
|
|
pubmed:dateCreated |
2010-4-5
|
|
pubmed:abstractText |
Novel thiazolotriazolopyrimidine derivatives (23-33) designed as potential adenosine A(2A) receptor (A(2A)R) antagonists were synthesized. Molecular docking studies revealed that all compounds (23-33) exhibited strong interaction with A(2A)R. The strong interaction of the compounds (23-33) with A(2A)R in silico was confirmed by their high binding affinity with human A(2A)R stably expressed in HEK293 cells using radioligand-binding assay. The compounds 24-26 demonstrated substantial binding affinity and selectivity for A(2A)R as compared to SCH58261, a standard A(2A)R antagonist. Decrease in A(2A)R-coupled release of endogenous cAMP in treated HEK293 cells demonstrated in vitro A(2A)R antagonist potential of the compounds 24-26. Attenuation in haloperidol-induced motor impairments (catalepsy and akinesia) in Swiss albino male mice pre-treated with compounds 24-26 further supports their role in the alleviation of PD symptoms.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
1464-3391
|
|
pubmed:author |
|
|
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
18
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2491-500
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
pubmed-meshheading:20303771-Adenosine A2 Receptor Antagonists,
pubmed-meshheading:20303771-Animals,
pubmed-meshheading:20303771-Antipsychotic Agents,
pubmed-meshheading:20303771-Catalepsy,
pubmed-meshheading:20303771-Cell Line,
pubmed-meshheading:20303771-Cell Membrane,
pubmed-meshheading:20303771-Chromatography, Thin Layer,
pubmed-meshheading:20303771-Computer Simulation,
pubmed-meshheading:20303771-Crystallography, X-Ray,
pubmed-meshheading:20303771-Cyclic AMP,
pubmed-meshheading:20303771-Drug Evaluation, Preclinical,
pubmed-meshheading:20303771-Dyskinesia, Drug-Induced,
pubmed-meshheading:20303771-Haloperidol,
pubmed-meshheading:20303771-Humans,
pubmed-meshheading:20303771-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20303771-Male,
pubmed-meshheading:20303771-Mice,
pubmed-meshheading:20303771-Models, Molecular,
pubmed-meshheading:20303771-Motor Activity,
pubmed-meshheading:20303771-Protein Binding,
pubmed-meshheading:20303771-Pyrimidines,
pubmed-meshheading:20303771-Radioligand Assay,
pubmed-meshheading:20303771-Structure-Activity Relationship,
pubmed-meshheading:20303771-Thiones
|
|
pubmed:year |
2010
|
|
pubmed:articleTitle |
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
|
|
pubmed:affiliation |
Medicinal Chemistry Division, Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, North Campus, Mall Road, Delhi 110 007, India.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
