Faculty Publications

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Publications by NITK Faculty

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    Regioselective reaction: Synthesis, characterization and pharmacological studies of some new Mannich bases derived from 1,2,4-triazoles
    (2009) Isloor, A.M.; Kalluraya, B.; Shetty, P.
    In the present investigation, a series of new 4[(3-substituted-1H-pyrazol-4-yl)methyleneamino]-5-substituted-2-[(4-methylpiperzine-1-yl)methyl]-2H-1,2,4-triazole-3(4H)-thiones (4) were synthesized by the aminomethylation of 4-(3-substituted-1H-pyrazol-3-yl)methyleneamino-5-substituted-4H-1,2,4-triazole-3-thiols (3) with formaldehyde and N-methylpiperzine. These newly synthesized Schiff and Mannich bases were characterized by IR, 1H NMR, mass spectral data and elemental analyses. These compounds were screened for their antibacterial and antifungal activity. Some of the compounds were found to exhibit significant antimicrobial activity. © 2009 Elsevier Masson SAS. All rights reserved.
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    Synthesis and antimicrobial activities of novel quinoline derivatives carrying 1,2,4-triazole moiety
    (2009) Eswaran, S.; Vasudeva Adhikari, A.V.; Shetty, N.S.
    A new class of quinoline derivatives containing 1,2,4-triazole moiety were synthesized from derivatives of 4-hydroxy-8-(trifluoromethyl)quinoline-3-carbohydrazide 4 through multi-step reactions. The compound 4, on treatment with substituted Isothiocyanates yielded quinoline-thiosemicarbazides 5a-c, which were conveniently cyclized to (5-mercapto-4H-triazol-3-yl)-quinolin-4-ols 6a-c in basic medium. These intermediates were then transformed to their respective chloro derivatives 7a-c by treatment with phosphorus oxychloride, which on further reaction with different biologically active rare amines yielded the target compounds 8a-g, 9a-h and 10a-h in good yield. The ultimate step, involving nucleophilic substitution reaction was achieved by microwave-induced technique, which has reduced the reaction time drastically as well as improved the yield when compared to conventional heating. The newly synthesized final compounds were evaluated for their in vitro antibacterial and antifungal activities against four strains each. Preliminary results indicated that most of the compounds demonstrated very good antimicrobial activity, comparable to the first line standard drugs. The most effective compounds have exhibited activity at MIC of 6.25 ?g/mL. © 2009 Elsevier Masson SAS. All rights reserved.
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    Synthesis, characterization and biological activities of some new benzo[b]thiophene derivatives
    (2010) Isloor, A.M.; Kalluraya, B.; Pai, K.
    Benzo[b]thiophene molecules are found to be important tools in synthetic medicinal chemistry. They are of current interest due to their wide spectrum of pharmacological properties. In view of the biological activities of benzo[b]thiophene containing molecules, in this present research work, we propose the synthesis of some new benzo[b]thiophene derivatives such as thiadiazoles, oxadiazoles, pyrazolin & diaryl pyrazoles starting from 3-chlorobenzo[b]thiophene-2-carboxyl chloride. These newly synthesized compounds were characterized by elemental analyses, I.R, NMR and Mass spectral studies. Some of the selected compounds were screened for their antibacterial, antifungal and anti-inflammatory studies. Many of the molecules were found to be potent. © 2009 Elsevier Masson SAS. All rights reserved.
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    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.
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    Design, synthesis and antimicrobial activities of some new quinoline derivatives carrying 1,2,3-triazole moiety
    (2010) Thomas, K.D.; Vasudeva Adhikari, A.V.; Shetty, N.S.
    A new series of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3-triazol-4-yl] methanamine derivatives were synthesized starting from 4-methoxyaniline through multi-step reactions. The title compounds 5a-y were prepared by treating the azide intermediate 4 with propargyl bromide and different alkyl/heterocyclic amines in a sequential three component synthesis. All the new compounds were characterized by spectral and elemental analyses. The newly synthesized final compounds were evaluated for their in vitro antibacterial and antifungal activities against pathogenic strains. The preliminary screening results indicated that most of the compounds demonstrated moderate to very good antibacterial and antifungal activities, comparable to the first-line drugs. Twenty five new derivatives of [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2,3- triazol-4-yl] methanamine have been synthesized and the most effective compounds have MIC of 6.25 ?g/mL, which are in comparable with present antibiotics. © 2010 Elsevier Masson SAS. All rights reserved.
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    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.
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    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.
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    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.
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    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.
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    Design and regioselective synthesis of trifluoromethylquinolone derivatives as potent antimicrobial agents
    (Elsevier Masson SAS infos@masson.fr 62 rue Camille Desmoulins Issy les Moulineaux Cedex 92442, 2013) Garudachari, B.; Isloor, A.M.; Satyanarayana, M.N.; Fun, H.-K.; Pavithra, N.; Kulal, A.
    Three series of new trifluoromethyl substituted quinolone derivatives were synthesized (4a-f, 6a-f and 8a-f) from corresponding substituted anilines by multi-step reactions. The regioselective alkylation with different alkyl halides were carried out by approaching two different routes to get the final products in good yield. Newly synthesized compounds were characterized by spectral study and also by C, H, N analyses. Three dimensional structure of 2b and 4b were also confirmed by single crystal X-ray studies. The final compounds (4a-f, 6a-f and 8a-f) were screened for their in-vitro antibacterial and antifungal activity by well plate method (zone of inhibition). The results revealed that, compounds 4a, 6b, 6c and 8e showed significant antibacterial activity as compared to the standard drug Ciprofloxacin. The compound 8a was found to be a potent antifungal agent. © 2013 Elsevier Masson SAS. All rights reserved.