Literature DB >> 20429782

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.

Faizul Azam1, Bashir A El-gnidi, Ismail A Alkskas, Musa A Ahmed.   

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.

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Year:  2010        PMID: 20429782     DOI: 10.3109/14756361003671052

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  3 in total

1.  Molecular docking studies of 1-(substituted phenyl)-3-(naphtha [1, 2-d] thiazol-2-yl) urea/thiourea derivatives with human adenosine A(2A) receptor.

Authors:  Faizul Azam; Medapati Vijaya Vara Prasad; Neelaveni Thangavel; Hamed Ismail Ali
Journal:  Bioinformation       Date:  2011-07-19

2.  in Silico investigation of the structural requirements for the AMPA receptor antagonism by quinoxaline derivatives.

Authors:  Faizul Azam; Ismaiel Mohamed Abugrain; Mohamed Hussin Sanalla; Radwan Fatahalla Elnaas; Ibrahim Abdassalam Ibn Rajab
Journal:  Bioinformation       Date:  2013-10-16

3.  Molecular Docking and Prediction of Pharmacokinetic Properties of Dual Mechanism Drugs that Block MAO-B and Adenosine A(2A) Receptors for the Treatment of Parkinson's Disease.

Authors:  Faizul Azam; Arwa M Madi; Hamed I Ali
Journal:  J Young Pharm       Date:  2012-07
  3 in total

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