Tuesday 9 July 2019

Lupine Publishers-Open access Journal of Drug Designing

Synthesis and Anxiolytic Activity of 2-(Substituted)- 5-[(N-Benzotriazolomethyl)-1,3, 4-Thiadiazolyl]-4- Thiazolidinone by V K Singh in Lupine publishers.

1,2,3- Benzotriazole (BTA) is a heterocyclic compound with three nitrogen atoms. It is a polar and colourless compound which can be used for its great versatility. The enormous investigations on derivatives of benzotriazole reveal wide applicability of this molecule for tagging and delivering huge number of heterocyclic nuclei. In the present work synthesis of several derivatives of 2-(substituted)-5-[(n-benzotriazolomethyl)-1,3,4-thiadiazolyl]-4-thiazolidinone has been synthesized and are evaluated for their anxiolytic activity. The antianxiety activities of the synthesized derivatives were evaluated using EPM test and Bright and dark box test experimental models of anxiety. All results were expressed as mean± standard error mean (SEM) and analysed by one-way ANOVA. Post-hoc comparisons were performed by applying Dunnefs test. P <0.05 was considered statistically significant

1,2,3- benzotriazoles were reported to have potential fungicidal [1] and antibacterial activity [2]. Similarly 1,3,4-thiadiazole derivatives were also reported to possess fungicidal, herbicidal, bactericidal [3], pesticidal, insecticidal, antihistaminic, antiamoebic [4], CNS depressant, antihypertensive, anticonvulsant, hypnotic, analgesic [5], anti-inflammatory [6] and agonist for 5-Ht receptor [7]. 4-thiazolidinone nucleus has also occupied a unique place in the field of medicinal chemistry due to its wide range of biological activities like antibacterial, anticancer [8], Respiratory, syncytial, virus Inhibitor [9], anticonvulsant [10], sciatic nerve blocking, local anaesthetic, inhibitors of human (CK2) protein kinase [11], hypnotic, fungicidal, cysticidal, anti leukemic and antioxidant activity. In view of potential biological activities of benzotriazole, thiadiazole and 4-thiazolidinone an attempt has made to unite these nuclei together and synthesize some new derivatives of benzotriazole (X^XJ to probe how far these combinations could develop anxiolytic activity. The procedure of synthesis has been outlined in Figure 1. 

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