4.2 Article Proceedings Paper

Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1,2,4] oxadiazole analogues and their evaluation as anti-Parkinson's agents

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MEDICINAL CHEMISTRY RESEARCH
卷 17, 期 2-7, 页码 386-398

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SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-007-9074-z

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dopamine receptor antagonist; antiparkinson; oxadiazole

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A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives was prepared and their evaluation for anti-Parkinson's activity was measured in vivo using albino rats. The result of the biological activity studies indicated that some of the synthesized compounds have good agonistic activity on the dopamine receptors and a few of them were also found to be free from neurotoxicity. Thus these compounds might be useful ligands for studying the functional role of dopamine receptors in vivo. The high log P value of the compounds indicates that they should easily cross the blood-brain barrier (log P > 2.6).

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