Paper
Design, synthesis and anti-Parkinsonian evaluation of 3-alkyl/aryl-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidine-2(3H)-thiones against neuroleptic-induced catalepsy and oxidative stress in mice
Published Nov 8, 2010 · F. Azam, Bashir A. El-gnidi, Ismail A. Alkskas
Journal of Enzyme Inhibition and Medicinal Chemistry
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Abstract
A series of 3-alkyl/aryl-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidine-2(3H)-thiones (3a–3f) were synthesised in good yield and evaluated for their anti-Parkinsonian and neuroprotective potential. The structures of the synthesised compounds were confirmed on the basis of their spectral data and elemental analysis. All of the compounds were found to be active in haloperidol-induced catalepsy and oxidative stress in mice. The most active compound carried a propyl group at the 3-position of the thiazolotriazolopyrimidine nucleus while substitution with a phenyl ring produced the least active compound among the series. A computational study was carried out for the prediction of pharmacokinetic properties and none of the compounds violated Lipinski’s rule of five, making them potentially promising agents for the treatment of Parkinson’s disease.
Non-RCT
Animal Study3-alkyl/aryl-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidine-2(3H)-thiones show potential as anti-Parkinson's and neuroprotective agents,
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