M. Bhat*, S.L. Belagali, N.K.H. Kumar and S. Jagannath Pages 66 - 73 ( 8 )
Background: Nitrogen-containing heterocyclics are abundant in natural products and also in synthetic drug molecules because of a variety of applications and superior pharmacological profile action. Pyrazoles are the integral architects of many of the heterocyclic compounds with superior biological activity.
Methods: Two series of the pyrazole conjugated Benzothiazole derivatives were synthesized. The pyrazoles were synthesized by the Vilsmeier-Haack reaction and then conjugated with benzothiazole hydrazine and hydrazide by imine bond formation. The synthesized compounds were screened for anti-mitotic activity using Allium assay.
Results: Here, the anti-mitotic activity, the percentage of cell division and the percentage of inhibition compared to the control were calculated. Compound 4b (-OMe), 4c (-OH), 5b (-OMe), 5c (- OH) and 5d (-CH3) had electron donating groups which showed excellent activity, was followed by 4f and 5f where they contain p-Bromo substitution, showing moderate activity.
Conclusion: In the two series, benzothiazole linked to pyrazole through the hydrazide bridging (5a-5i) had superior to hydrazine bridging (4a-4i). The observed chromosomal aberrations are because of the structural morphology and binding sites of the molecule with the chromosome.
Pyrazole, benzothiazole, antimitotic activity, ID50 value, hydrazine, chromosome.
Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Environmental Chemistry Laboratory, Department of Studies in Environmental Science, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Department of Studies in Botany, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka, Department of Studies in Botany, University of Mysore, Manasagangothri, Mysore -570 006, Karnataka