Faculty Publications
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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 of new 3-aryl-4-(3-aryl-4,5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H- pyrazole derivatives as potential antimicrobial agents(2013) Malladi, S.; Isloor, A.M.; Peethambar, S.K.; Fun, H.-K.New (E)-1-aryl-3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)prop-2-en-1-ones 6 (pyrazolic chalcones) were synthesized from Claisen-Schmidt reaction of 3-aryl-1-phenylpyrazol-4-carboxaldehydes 4 with several acetophenone derivatives 5. Subsequently, the cyclocondensation reaction of chalcones 6 with phenylhydrazine in acetic acid medium afforded the new 3-aryl-4-(3-aryl-4,5- dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazoles 7. The synthesized compounds were characterized by spectral studies and evaluated for their in vitro antibacterial activity against three pathogenic bacterial strains, Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa, and in vitro antifungal activity against three pathogenic fungal strains Aspergillus flavus, Chrysosporium keratinophilum, and Candida albicans. © 2012 Springer Science+Business Media New York.Item Click chemistry approach: Regioselective one-pot synthesis of some new 8-trifluoromethylquinoline based 1,2,3-triazoles as potent antimicrobial agents(2014) Garudachari, B.; Isloor, A.M.; Satyanarayana, M.N.; Fun, H.-K.; Hegde, G.Three series of 8-trifluoromethylquinoline based 1,2,3-triazoles derivatives (5a-c, 6a-d and 7a-c) were synthesized by multi-step reactions by click chemistry approach. Synthesized compounds were characterized by spectral studies and X-ray analysis. The final compounds were screened for their in-vitro antimicrobial activity by well plate method (zone of inhibition). Compounds 5c, 6b, 8b, 11 and 12 were found to be active against tested microbial strains. The results are summarized in Tables 5 and 6. © 2014 Elsevier Ltd. All rights reserved.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.