Faculty Publications

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Publications by NITK Faculty

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Author: search.filters.author.Chandrakantha, B.Subject: search.filters.subject.unclassified drug

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    Synthesis, characterization and biological activity of some new 1,3,4-oxadiazole bearing 2-flouro-4-methoxy phenyl moiety
    (2010) Chandrakantha, B.; Shetty, P.; Nambiyar, V.; Isloor, N.; Isloor, A.M.
    In the present study a series of new 1,3,4-oxadiazole derivatives containing 2-fluoro-4-methoxy moiety were synthesized. These newly synthesized compounds were characterized by NMR, mass spectral, IR spectral study and also by C, H, N analyses. All the newly synthesized compounds were screened for their antibacterial and antifungal studies. Antimicrobial studies revealed that compounds 4a and 4b showed significant antibacterial activity against Escherichia coli and Pseudomonas aeruginosa Compound 4i showed significant antifungal activity against C. albicans. © 2009 Elsevier Masson SAS. All rights reserved.
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    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.
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    Synthesis, characterization and antimicrobial activity of novel ethyl 1-(N-substituted)-5-phenyl-1H-pyrazole-4-carboxylate derivatives
    (2012) Chandrakantha, B.; Isloor, A.M.; Shetty, P.; Isloor, S.; Malladi, S.; Fun, H.-K.
    In the present study, a novel series of Pyrazole derivatives (3a-m) were synthesized by condensing ethyl-3-(dimethylamino)-2-(phenylcarbonyl)prop-2- enoate with different aromatic and aliphatic hydrazines. These newly synthesized compounds were characterized by NMR, mass spectral, IR spectral studies as well as by C, H, and N analyses. All the newly synthesized compounds were screened for their antibacterial properties against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. Among the screened samples, 3c, 3f, 3k, and 3l have showed excellent antibacterial activity against all the tested bacterial strains as compared to the standard drug Ceftriaxone. Few of the compounds were found to be biologically potent. Molecular structure of compound 3i was confirmed by single crystal X-ray analysis. © Springer Science+Business Media, LLC 2011.
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    T3P mediated synthesis of some new quinoline substituted pyrazole derivatives and its antibacterial studies
    (2012) Chandrakantha, B.; Isloor, A.M.; Peethambar, S.K.; Shetty, P.
    A series of new N-(substituted)-5-phenyl-1-(quinolin-2-yl)-1H-pyrazole-4-carboxamide derivatives (5a-h) have been synthesized by condensing ethyl-3-(dimethylamino)-2-[(phenyl)carbonyl]prop-2-enoate 2 with quinoline-2-yl-hydrazine. Compound 3 is hydrolyzed into 4 which is upon further coupled with different aromatic/aliphatic amines using 50% prpopyl phosphonic anhydride (T3P) in ethyl acetate as coupling reagent to afford different quinoline substituted pyrazole carboxamide derivatives. All the newly synthesized compounds were screened for their invitro antibacterial studies against Escherichia coli, Bacillus subtilis and Pseudomonas aeruginosa. The results revealed that compounds 5d, 5f, and 5h showed good antibacterial activity towards all bacterial strains. These newly synthesized compounds were characterized by NMR, mass spectral, IR spectral study and also by C, H, N analyses.
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    Synthesis and biological evaluation of novel substituted 1,3,4-thiadiazole and 2,6-di aryl substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives
    (Elsevier Masson s.r.l., 2014) Chandrakantha, B.; Isloor, A.M.; Shetty, P.; Fun, H.-K.; Hegde, G.
    A new series of N-[5-(4-(alkyl/aryl)-3-nitro-phenyl)-[1,3,4-thiadiazol-2- yl]-2,2-dimethyl-propionamide 4 (a-l) and 6-(4-Methoxy-phenyl)-2-(4-alkyl/aryl)- 3-nitro-phenyl)-Imidazo [2,1-b] [1,3,4] thiadiazole 6 (a-l) were synthesized starting from 5-(4-Fluoro-3-nitro-phenyl)-[1,3,4] thiadiazole-2-ylamine. The synthesized compounds were characterized by IR, NMR, mass spectral and elemental analysis. All the compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by well plate method (zone of inhibition). Compounds 4a, 4c and 6e, 6g displayed appreciable activity at the concentration 0.5-1.0 mg/mL.© 2013 Elsevier Masson SAS. All rights reserved.