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

被引:36
作者
Azam, Faizul [1 ]
El-gnidi, Bashir A. [1 ]
Alkskas, Ismail A. [1 ]
Ahmed, Musa A. [2 ]
机构
[1] Univ Seventh October, Fac Pharm, Med Chem Lab, Misurata, Libya
[2] Al Arab Med Univ, Fac Pharm, Dept Med Chem, Benghazi, Libya
关键词
Parkinson's disease; oxidative stress; neuroprotection; thiazolotriazolopyrimidine; HALOPERIDOL-INDUCED CATALEPSY; POTENTIAL ANTICANCER; THIOUREA DERIVATIVES; ANTIOXIDANT; AGENTS; GLUTATHIONE; ANTAGONIST; MECHANISMS; THERAPY; NEURONS;
D O I
10.3109/14756361003671052
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
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.
引用
收藏
页码:818 / 826
页数:9
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