Faculty Publications
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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 Hantzsch reaction: Synthesis and characterization of some new 1,4-dihydropyridine derivatives as potent antimicrobial and antioxidant agents(2011) Vijesh, A.M.; Isloor, A.M.; Peethambar, S.K.; Shivananda, K.N.; Arulmoli, T.; Isloor, N.In the present study two new series of Hantzsch 1,4-dihydropyridine derivatives (1,4-DHPs) containing substituted pyrazole moiety (4a-f and 5a-f) were synthesized by the reaction of 3-aryl-1H-pyrazole-4-carbaldehydes with 1,3-dicarbonylcompounds (ethylacetoacetate and methylacetoacetate) and ammonium acetate. The newly synthesized compounds were characterized by IR, NMR, mass spectral study and also by C, H, N analyses. New compounds were screened for their antimicrobial activity by well plate method (zone of inhibition). Antioxidant studies of the synthesized compounds were also performed by measuring the DPPH radical scavenging assay. Compounds 4c, 4e and 4f were found to be potent antibacterial and antioxidant agents. The acute oral toxicity study for the compounds 4c, 4e and 4f were carried out and the experimental studies revealed that compounds 4c and 4e is safe up to 3000 mg/kg and no death of animals were recorded. However in compound 4f, we found mortality above 2000 mg and also significant behavioral changes in experimental animals. © 2011 Elsevier Masson SAS. All rights reserved.Item Synthesis, characterization and antimicrobial studies of some new quinoline incorporated benzimidazole derivatives(2012) Garudachari, B.; Satyanarayana, M.N.; Thippeswamy, B.; Shivakumar, C.K.; Shivananda, K.N.; Hegde, G.; Isloor, A.M.Two new series of quinoline incorporated benzimidazole derivatives (4a-i and 8a-f) were synthesized from substituted aniline and isatin through multi-step reaction. 6-substituted-4-carboxyquinolines (3a,b and 7) were synthesized by multi component one pot reactions (via Doebner reaction and Pfitzinger reaction respectively) and the targeted benzimidazole derivatives were obtained by the reaction of 6-substituted-4-carboxyquinolines (3a,b and 7) with substituted aromatic diamines in acidic media. All the newly synthesized compounds were characterized by IR, NMR mass spectral study and also by C, H, N analyses. The final compounds were screened for their in-vitro antibacterial and antifungal activity by well plate method (zone of inhibition). The results revealed that, compounds 4c, 4d, 8c and 8d showed significant antibacterial activity. The compound 8b was found to be potent antifungal agent. 4a, 8a and 8f showed moderate to good antimicrobial activity as compared to the standard drugs against all tested microbial strains. © 2012 Elsevier Masson SAS. All rights reserved.