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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