SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW 6-(SUBSTITUTEDPHENYL) THIAZOLO [3,2-B][1,2,4] TRIAZOLE DERIVATIVES IN MICE

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DENG XIAN QING; SONG MING XIA; GONG GUO HUA; WANG SHI BEN; QUAN ZHE SHAN

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Journal: Iranian Journal of Pharmaceutical Research Year:2014 | Volume:13 | Issue:2 Page(s): 459-469

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Title

SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW 6-(SUBSTITUTEDPHENYL) THIAZOLO [3,2-B][1,2,4] TRIAZOLE DERIVATIVES IN MICE

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Keywords

SYNTHESIS

ANTICONVULSANT

THIAZOLOTRIAZOLE

MAXIMAL ELECTROSHOCK

PENTYLENETETRAZOLE

Abstract

Epilepsy is the most frequent nearological affiction and afflicts 1% about of the worlds population. Currently there is an urgent need for the development of novel ANTICONVULSANTs with higher levels of potency and lower levels of toxicity. In this paper, a series of new 6- (substituted-phenyl) thiazolo [3, 2-b] [1, 2, 4] triazole derivatives were synthesized and tested for their ANTICONVULSANT activities using the MAXIMAL ELECTROSHOCK (MES) and subcutaneous PENTYLENETETRAZOLE (PTZ) screens, which are the most widely employed seizure models for early identification of candidate ANTICONVULSANTs. Their neurotoxicity was determined applying the rotarod test. In these compounds, 6- (4-fluorophenyl) thiazolo [3, 2-b] [1, 2, 4] triazole (3c) showed selective protection against the MES seizures with an ED50 value of 49.1 mg/Kg and a TD50 value of 94.1 mg/Kg, which provided compound 3c a protective index (PI=TD50/ED50) of 1.9 in the MES test.6- (4-Propoxyphenyl) thiazolo [3, 2-b] [1, 2, 4] triazole (5b) was found to be active in both models, i.e. MES test and PTZ test. In the PTZ screen, compound 5b gave an ED50 of 63.4 mg/Kg and a TD50 of 105.6 mg/Kg, resulting in a PI value of 1.7 which is higher than carbamazepine.

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APA: Copy

DENG, XIAN QING, SONG, MING XIA, GONG, GUO HUA, WANG, SHI BEN, & QUAN, ZHE SHAN. (2014). SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW 6-(SUBSTITUTEDPHENYL) THIAZOLO [3,2-B][1,2,4] TRIAZOLE DERIVATIVES IN MICE. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 13(2), 459-469. SID. https://sid.ir/paper/288245/en

Vancouver: Copy

DENG XIAN QING, SONG MING XIA, GONG GUO HUA, WANG SHI BEN, QUAN ZHE SHAN. SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW 6-(SUBSTITUTEDPHENYL) THIAZOLO [3,2-B][1,2,4] TRIAZOLE DERIVATIVES IN MICE. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2014;13(2):459-469. Available from: https://sid.ir/paper/288245/en

IEEE: Copy

XIAN QING DENG, MING XIA SONG, GUO HUA GONG, SHI BEN WANG, and ZHE SHAN QUAN, “SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME NEW 6-(SUBSTITUTEDPHENYL) THIAZOLO [3,2-B][1,2,4] TRIAZOLE DERIVATIVES IN MICE,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 13, no. 2, pp. 459–469, 2014, [Online]. Available: https://sid.ir/paper/288245/en

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