Faculty Publications
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Item 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.Item Synthesis, characterization and anti-microbial studies of some novel 2,4-disubstituted thiazoles(2010) Vijesh, A.M.; Isloor, A.M.; Prabhu, V.; Ahmad, S.; Malladi, S.In the present study a series of novel 2,4-disubstituted thiazole derivatives containing substituted pyrazole moiety was synthesized by the reaction of 3-Aryl-1H-pyrazole-4-carbaldehyde thiosemicarbazone with 6-Bromo/H-3-(bromoacetyl)-2H-chromen-2-one/phenacyl chloride. Structures of newly synthesized compounds were characterized by spectral studies. New compounds were screened for their antibacterial studies against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The results revealed that compounds 7c, 8e, and 8f having 2,5-dichlorothiophene substituent and 8c, 8d having 2,4-dichlorophenyl substituent showed significant antibacterial activity against all tested microorganisms. © 2010 Elsevier Masson SAS. All rights reserved.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 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 of some new pyrazolone derivatives as potent antimicrobial agents(2011) Vijesh, A.M.; Isloor, A.M.; Isloor, S.; Shivananda, K.N.; Shyma, P.C.; Arulmoli, T.Invasive microbial infections are major problems around the world, especially in immuno compromised patients. The recent expansion of antimicrobial drug research has occurred because there is a critical need for new antimicrobial agents to treat these life threatening invasive infections. In the present study three series of new substituted pyrazolone derivatives (5a-f, 6a-f and 8a,b) were synthesized by the Knoevenagel condensation reaction of pyrazolones (3a,b) with various substituted carbaldehydes (4a-f, 7). These newly synthesized compounds were characterized by IR, NMR, mass spectra and also by C, H, N analyses. New compounds were screened for their antimicrobial studies against S. aureus, B. subtilis, E. coli and P. aeruginosa. The results revealed that compounds 5c and 6c having 2,5-dichlorothiophene substituent showed significant antibacterial activity against all tested microorganisms as compared to the standard drug Ceftriaxone.Item Synthesis and antimicrobial activity of some new pyrazole containing cyanopyridone derivatives(2012) Malladi, S.; Isloor, A.M.; Peethambar, S.K.; Ganesh, B.M.; Goud, P.S.K.A series of new 4,6-disubstituted-3-cyano-2-pyridone derivatives (4a-o) were synthesized. The structures of all target molecules (4a-o) have been confirmed by various spectral techniques and elemental analyses. The newly synthesized compounds were screened for antibacterial and antifungal activity and most of the compounds showed significant activity comparable with that of the standard drug. The results revealed that 4b, 4c, 4d, 4g, 4m, 4n and 4o showed good antibacterial activity towards all bacterial strains (Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa) when compared to standard drug streptomycin. Amongst all the compounds, 4c showed moderate antifungal activity against Aspergillus flavus. The acute toxicity study has also been carried out for biologically active compounds and the experimental studies revealed that compounds were safe up to 2000 mg/kg and no deaths of animals were recorded.Item 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.Item 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.Item Molecular docking studies of some new imidazole derivatives for antimicrobial properties(2013) Vijesh, A.M.; Isloor, A.M.; Telkar, S.; Arulmoli, T.; Fun, H.-K.In modern drug designing, molecular docking is routinely used for understanding drug-receptor interaction. In the present study six imidazole derivatives containing substituted pyrazole moiety (2a,. b and 4a-d) were synthesized. Structures of the newly synthesized compounds were characterized by spectral studies. Compounds were screened for their antibacterial activity. Compound 4c was found to be potent antimicrobial against Pseudomonas aeruginosa at concentrations of 1 and 0.5. mg/mL compared to standard drug Streptomycin. All the compounds were subjected to molecular docking studies for the inhibition of the enzyme l-glutamine: d-fructose-6-phosphate amidotransferase [GlcN-6-P] (EC 2.6.1.16). The in silico molecular docking study results showed that, all the synthesized compounds having minimum binding energy and have good affinity toward the active pocket, thus, they may be considered as good inhibitor of GlcN-6-P synthase. © 2011.Item New pyrazole derivatives containing 1,2,4-triazoles and benzoxazoles as potent antimicrobial and analgesic agents(2013) Vijesh, A.M.; Isloor, A.M.; Shetty, P.; Sundershan, S.; Fun, H.-K.Azole class of compounds are well known for their excellent therapeutic properties. Present paper describes about the synthesis of three series of new 1,2,4-triazole and benzoxazole derivatives containing substituted pyrazole moiety (11a-d, 12a-d and 13a-d). The newly synthesized compounds were characterized by spectral studies and also by C, H, N analyses. All the synthesized compounds were screened for their analgesic activity by the tail flick method. The antimicrobial activity of the new derivatives was also performed by Minimum Inhibitory Concentration (MIC) by the serial dilution method. The results revealed that the compound 11c having 2,5-dichlorothiophene substituent on pyrazole moiety and a triazole ring showed significant analgesic and antimicrobial activity. © 2012 Elsevier Masson SAS. All rights reserved.