Faculty Publications
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Item Synthesis and biological evaluation of aminoketones(2010) Sankappa Rai, U.; Isloor, A.M.; Shetty, P.; Isloor, N.; Malladi, S.; Fun, H.-K.A three-component Mannich reaction of different ketones with aromatic aldehydes and different amines in microwave irradiation under solvent free condition afforded corresponding ?-amino carbonyl compounds in excellent yields. This method proved as a novel and improved modification of the reported three-component Mannich reaction in terms of milder reaction conditions, reaction times, clean reaction profiles, very small quantity of catalyst and simple workup procedure. Newly synthesized ?-aminoketones were characterized by spectral studies. Structure of compound 4a was also confirmed by single-crystal X-ray analysis. All the compounds were screened for their antimicrobial activity by MIC method. Few of the molecules were found to be biologically potent. © 2010 Elsevier Masson SAS. All rights reserved.Item Synthesis, characterization and in vitro cytotoxic properties of some new Schiff and Mannich bases in Hep G2 cells(Birkhauser Boston, 2011) Dhanya, D.; Isloor, A.M.; Shetty, P.; Chandrakantha, B.; Satyamoorthy, K.A series of 5-substituted-4-amino-3-mercapto- 1,2,4-triazoles were synthesized and were treated with various 3-substituted pyrazole aldehydes to obtain a series of new Schiff bases (3a-l). Few of the selected Schiff bases were converted into Mannich bases by reaction with diphenylamine/morpholine in presence of formaldehyde in ethanol media (4a-e, 5a-e). These newly synthesized compounds were characterized by elemental analysis, IR, NMR and mass spectrometry studies. A comparative study on the cytotoxic activities of few selected Schiff and Mannich bases was done in HepG2 cells using MTT assay. Few of the screened Schiff bases, 3a, 3d, 3e, 3g and 3h showed dose dependent cytotoxic activity, 3a being the most potent with an IC50 value of 0.018 g/l comparable to the standard drug doxorubicin. Among the Mannich bases, 5b was the most active with an IC50 value of 0.034 g/l. The Schiff bases were found to be more active, when compared to Mannich bases derived from them. The morpholine derived Mannich bases were more potent than those obtained from diphenyl amine. © Springer Science+Business Media, LLC 2010.Item A novel series of homoallylic amines as potential antimicrobials(2012) Rai, U.S.; Isloor, A.M.; Shetty, P.; Isloor, N.; Padaki, M.; Fun, H.-K.An efficient catalytic three-component reaction of aldehydes, amines, and allyltributylstannate has been successfully developed to produce homoallylic amines at 25°C, in excellent yields, in the presence of 1 mol% of trifluoroacetic acid an inexpensive and environmentally friendly catalyst. Newly synthesized compounds were confirmed by spectral studies. Compound 3o was characterized by single crystal X-ray analysis. All the compounds were also screened for their antimicrobial activity. Halogen-substituted compounds namely 3d, 3g, 3n, and 3o have showed excellent antibacterial activity. © Springer Science+Business Media, LLC 2011.Item Palladium complex in a room temperature ionic liquid: A convenient recyclable reagent for catalytic oxidation(Taylor and Francis Ltd., 2014) Dileep, R.; Badekai Ramachandra, B.; Suresha Kumara, T.H.S.Palladium (Pd)-catalyzed carbonylation of alcohols proceeds in ionic liquid (IL) media (1-ethyl-3-methylimidazolium hexafluorophosphate). Carbonylation of primary/secondary alcohols to aldehydes/ketones was greatly accelerated by the use of a Pd-based catalyst in the presence of NaOCl as an oxidant. The catalyst was more easier to recycle in the IL [Emim]PF6 with an equal-proportioned CH2Cl2 than in the single CH2Cl2 or IL. © 2014 The Author(s). Published by Taylor & Francis.Item Base-promoted multicomponent synthesis of 1,2,4-triazole-based hybrids from 1,3-diones, β-nitrostyrenes, and hydrazones(Royal Society of Chemistry, 2024) Sreelekha, M.K.; Jijin, R.K.; Nayak, K.H.; Babu, B.P.Herein, we report a metal-free, base-promoted route for the synthesis of hybrid molecular scaffolds in which various 1,3-diones and 1,2,4-triazoles are linked by a benzyl bridge. This three-component, one-pot reaction was accomplished by first treating 4-hydroxycoumarin, trans-β-nitrostyrene, and aldehyde hydrazone in the presence of sodium carbonate. Further, this protocol was successfully expanded to other 1,3-diones, such as dimedone and 4-hydroxy-2-quinolone. A broad substrate scope, mild reaction conditions, and the metal and ligand/additive-free approach are the prominent features of this strategy. © 2024 The Royal Society of Chemistry.Item Amidated pectin and gum Arabic aldehyde-based pH-sensitive hydrogel for targeted colonic treatment(Elsevier B.V., 2025) Singh, H.; JagadeeshBabu, J.; Mohan Balakrishnan, R.In this study, a novel pH-responsive hydrogel was developed by crosslinking amidated pectin(AmPec) with oxidised gum Arabic(GAA) by hydrogen and hemiacetal bonding without the need for toxic crosslinkers for oral delivery of doxorubicin to treat colon cancer. FTIR and NMR confirmed the amidation of pectin and oxidation of Gum Arabic. FTIR confirmed the formation of hydrogen and hemiacetal bonds in the hydrogel. X-ray diffraction(XRD) spectra showed the amorphous characteristic of AmPec-GAA hydrogels compared to their polymer precursors, confirming the formation of a crosslinked hydrogel. AmPec-GAA15 hydrogel swelled around 655 %±39.90 at pH 7.4 compared to 181 %±7.94 swelling at pH 1.2 after 72 h. The release of doxorubicin also followed the same trend, with only 4.48 % ±0.89 doxorubicin release at pH 1.2, while the drug release increased to 68.10 %±3.73 at pH 7.4 after 48 h. SEM micrographs revealed the macroporous and interconnected hydrogel structure with fewer pores in the hydrogel swelled in pH 1.2 compared with pH 7.4, where more visible pores were observed, indicating the pH-sensitive behaviour of the hydrogel. Hydrogel possessed excellent thermal and mechanical stability as revealed by TGA and rheology study, which can also be explored for tissue engineering applications. MTT assay on L929 cells showed cell viability above 95.1 %±,0.0074, demonstrating hydrogels' non-toxic and biocompatible behaviour. Meanwhile, Dox-loaded hydrogel induced higher cytotoxicity against HT-29 cells than free Dox in a dose-dependent manner. Therefore, the developed hydrogel can be used as an effective oral carrier to deliver doxorubicin to colon cancer while hindering its release in the stomach and thus preventing associated toxicity. © 2025 Elsevier B.V.