ORIGINAL ARTICLE
Year : 2015  |  Volume : 14  |  Issue : 2  |  Page : 130-138

Synthesis and evaluation of neuropharmacological profile of isatin-3-[ N2 -(2-benzalaminothiazol-4-yl)] hydrazones


1 Department of Pharmaceutical Chemistry, Talla Padmavathi College of Pharmacy, Urus, Warangal, India
2 Neuropharmacology Divison, Vaagdevi College of Pharmacy, Warangal; Department of Biotechnology, Acharya Nagarjuna University, Guntur, Andhra Pradesh, India
3 Neuropharmacology Divison, Vaagdevi College of Pharmacy, Warangal, India

Correspondence Address:
Venkateshwar Rao Jupally
Talla Padmavathi College of Pharmacy, Urus, Warangal - 506 002
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/1687-4315.161287

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Background and objective Isatin and its derivatives are versatile lead molecule for potential bioactive agents and are reported to possess a wide spectrum of activities such as central nervous system (CNS), antibacterial, antifungal, anticonvulsant, anti-HIV, antidepressant, anti-inflammatory, etc. In this study, we evaluated neuropharmacological profile of isatin-3-[N2 -(2-benzalaminothiazol-4-yl)] hydrazone derivatives using well-defined preclinical models. Materials and methods The isatin-3-[N2 -(2-benzalaminothiazol-4-yl)] hydrazone derivatives ( Va-Vj ) were synthesized and characterized using spectral data. Neuropharmacological profile of Va-Vj (10 and 100 mg/kg, orally) was investigated by gross behavioural profile, hole board, locomotor activity, hypnotic activity, forced swim test, tail suspension test and rota rod test in mice. Imipramine (10 mg/kg) and diazepam (2 mg/kg) were used as standard for antidepressant and sedative as well as a hypnotic drug, respectively. Results and conclusion Isatin derivatives showed dose-dependent neuropharmacological action on the CNS, such as anxiolytic, sedative, hypnotic and depressant action. Among all the derivatives, halogen-substituted compounds ( Vh and Vi ) at 100 mg/kg showed significant (P < 0.001) action when compared with the control group (0.1% sodium carboxy methylcellulose (CMC)), and other substituted isatin derivatives Va, Vb, Vc, Vd, Ve, Vf, Vg and Vj also proved to possess a significant (P < 0.05) action at 100 mg/kg compared with the control group. From these results, we concluded that Va-Vj compounds possessed a wide range of CNS activities.


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