Faculty Publications
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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 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.Item 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.Item Synthesis, and antitubercular and antimicrobial activity of 1?-(4-chlorophenyl)pyrazole containing 3,5-disubstituted pyrazoline derivatives(Royal Society of Chemistry, 2016) Harikrishna, N.; Isloor, A.M.; Kulal, K.; AlObaid, A.; Fun, H.-K.A new series of 1?-(4-chlorophenyl)-5-(substituted aryl)-3?-(substituted aryl)-3,4-dihydro-2H,1?H-[3,4?]bipyrazolyl derivatives (6a-e, 8a-e, 10a-e) have been synthesized, characterized and screened for antimicrobial and antitubercular activity. Among the synthesized compounds, the minimum inhibition concentration of 10e was found to be as low as 1.56 ?g ml-1 and that of 10c was 6.25 ?g ml-1 as compared to the standard anti-tb drugs pyrazinamide and streptomycin. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2016.Item Antitubercular and antimicrobial activity of nh4vo3 promoted 1,4-dihydropyridine incorporated 1,3,4-Trisubstituted pyrazole(Bentham Science Publishers B.V. P.O. Box 294 Bussum 1400 AG, 2017) Harikrishna, N.; Isloor, A.M.; Kulal, K.; Parish, T.; Jamalis, J.; Ghabbour, H.A.; Fun, H.-K.Background: A new series of pyrazole containing 1,4-dihydropyridine derivatives 5a-i and 6a-i were synthesized from substituted acetylated aryls and substituted phenylhydrazine by the multistep reaction. Method: The target compounds 1,4-dihydropyridine derivatives were obtained from green synthesis of 1,3-disubstituted phenyl-1H-pyrazole-4-carbaldehydes 4a-i with ethyl acetoacetate and methyl acetoacetate at higher temperatures in the presence of ammonium acetate and the catalytic amount of ammonium metavanadate (NH4VO3). The role of ammonium metavanadate was increases rate of the reaction and obtained high yields. Result: Structures of newly synthesized 1,4-dihydropyridine moiety containing pyrazole derivatives were confirmed by FT-IR, NMR and Mass spectral studies. The structure of compound 5b was confirmed by S-XRD study. Further, these compounds were tested for in-vitro antitubercular and antimicrobial studies. Compounds 5a, 5b, 5i, 6a, 6b, 6g, 6h, and 6i were found to be active against all the bacterial microorganisms. Conclusion: The above mentioned compounds have shown lowest MIC ranging between 3.12-12.5 ?g/ml against Mycobacterium tuberculosis and MIC values ranging between 7.8- 15.6 ?g/ml for Mycobacterium smegmatis, Staphylococcus aureus and Pseudomonas aeruginosa. For the control of life threatening diseases such as tuberculosis, these eight compounds may be strongly promising synthetic compounds. © 2017 Bentham Science Publishers.