Faculty Publications
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Item Synthesis, characterization and antimicrobial studies of some new pyrazole incorporated imidazole derivatives(2011) Vijesh, A.M.; Isloor, A.M.; Telkar, S.; Peethambar, S.K.; Rai, S.; Isloor, N.In the present study two series of novel imidazole derivatives containing substituted pyrazole moiety (3a-d and 5a-j) were synthesized. The first series were synthesized by the reaction of 3-aryl-1H-pyrazole-4-carbaldehyde thiosemicarbazones (2a-d) with DMAD and the second series by the reaction of 3-aryl-1H-pyrazole-4-carbaldehydes (1a-e) with 1,2-diketones (4a,b) in the presence of ammonium acetate. Structures of newly synthesized compounds were characterized by spectral studies. New compounds were screened for antifungal and antibacterial activities. Among the synthesized compounds, compound 3c was found to be potent antimicrobial agent. The acute oral toxicity study for the compound 3c was carried out and the experimental studies revealed that compound 3c is safe up to 3000 mg/kg and no death of animals were recorded. © 2011 Elsevier Masson SAS. All rights reserved.Item Synthesis, characterization, anticancer, and antioxidant activity of some new thiazolidin-4-ones in MCF-7 cells(2013) Isloor, A.M.; Dhanya, D.; Shetty, P.; Malladi, S.; Pai, K.S.R.; Maliyakkal, N.There are limited studies centring on the potential of thiazolidin-4-ones as anticancer agents. In this study, a new series of 2-(3-substituted-1H- pyrazol-4-yl)-3-(3-substituted-5-sulfanyl-1,2,4-triazol-4-yl)-1, 3-thiazolidin-4-one (4a-o) have been synthesized by cyclo-condensation reaction of 5-substituted-4-[(3-substituted-1H-pyrazol-4-ylmethylidene)amino]-2H-1,2,4- triazole-3-thione (3a-o) and thioglycolic acid. The structures of all the synthesized compounds were confirmed by elemental analysis, spectral techniques like IR, 1H NMR, and mass spectroscopy. Few compounds exhibited dose-dependent cytotoxic effect in MTT assay in human breast cancer (MCF-7) cells. Apoptotic degradation of DNA due to action of potent thiazolidin-4-ones was analysed by agarose gel electrophoresis and visualized by ethidium bromide staining (comet assay). A concentration-dependent increase in tail length and olive tail moment was observed when treated with thiazolidin-4-ones. In vitro antioxidant studies like DPPH and ABTS-free radical scavenging assays-indicated moderate activity of thiazolidin-4-ones. © 2012 Springer Science+Business Media, LLC.