Faculty Publications
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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 and anti-inflammatory evaluation of some new 3,6-disubstituted-1, 2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles bearing pyrazole moiety(2012) Malladi, S.; Isloor, A.M.; Shetty, P.; Fun, H.-K.; Telkar, S.; Mahmood, R.; Isloor, N.In the present study, a new series of 3,6-disubstituted- 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles (4aj) have been synthesized by condensing 3-substituted-4-amino-5- mercapto-1,2,4-triazoles (1a-b) with various 3-substitutedpyrazole- 4-carboxylic acids (3a-e) in the presence ofPOCl3. The structures of newly synthesized compounds were characterized by elemental analysis, IR, 1H NMR, 13CNMR, and mass spectroscopic studies. Structure of the compound 4b was also confirmed by recording the single crystal X-ray structure. All the synthesized compounds were screened for their anti-inflammatory activities by carrageenan induced paw edema method. Anti-inflammatory screening indicated that, compounds 4d, 4e, and 4h were found to be biologically active whereas remaining compounds showed poor antiinflammatory activity. Also molecular docking studies were also performed for compounds which showed good antiinflammatory activity. © Springer Science+Business Media, LLC 2011.Item Synthesis and evaluation of antioxidant, antimicrobial activities of new 2,4-disubstituted thiazoles(2012) Malladi, S.; Isloor, A.M.; Peethambar, S.K.; Shivananda, K.N.A new series of 2,4-disubstituted thiazole derivatives were synthesized by the reaction of various 3-aryl-1H-pyrazole-4- carbaldehyde thiosemicarbazones (2a-e) and phenacyl bromides. The compounds (3a-n) were characterized by IR, NMR, mass spectra and C, H, N analyses. All the synthesized compounds were screened for their antioxidant and antimicrobial activities. Antioxidant studies revealed that, compounds 3b, 3j and 3n showed significant scavenging activity whereas compounds 3e and 3n exhibited significant antimicrobial activity. The acute oral toxicity study for the compound 3e and 3n have revealed good safety profile till the uppermost dose (2000 mg/kg).Item Synthesis, characterization and their anticonvulsant, anti-inflammatory studies of some novel chromeno oxadiazoles(2013) Ubaradka, S.R.; Isloor, A.M.; Shetty, P.; Shetty, P.; Isloor, N.A.In this study, a series of new 1,2,4-oxadiazole derivatives containing 3,4-dihydro-2H-chromen-2-amine moiety were synthesized by efficient microwave reaction of 2-amino-N?-hydroxychroman-3-carboxamidine and suitable aldehyde. Structures of all the synthesized compounds were confirmed by spectral studies and C, H, N analyses. Newly synthesized compounds were screened for their anticonvulsant and anti-inflammatory properties. Few of the compounds exhibited excellent anticonvulsant activity as compared to the standard drug Diazepam. Also compounds have exhibited moderate anti-inflammatory activity as compared to the standard drug Diclofenac sodium. © 2012 Springer Science+Business Media, LLC.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.