Faculty Publications
Permanent URI for this communityhttps://idr.nitk.ac.in/handle/123456789/18736
Publications by NITK Faculty
Browse
12 results
Search Results
Item 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.Item 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.Item 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.Item Novel chromeno [2,3-b]-pyrimidine derivatives as potential anti-microbial agents(2010) Sankappa Rai, U.; Isloor, A.M.; Shetty, P.; Vijesh, A.M.; Prabhu, N.; Isloor, S.; Thiageeswaran, M.; Fun, H.-K.An efficient, microwave irradiated synthesis of novel chromeno[2,3-b]-pyrimidine derivatives was carried out. 2-Amino-3,4-dihydro-2H-chromene-3-carbonitrile was converted into imine using N,N-Dimethylacetaldehyde dimethylacetal to give the core intermediate, which was used for the preparation of chromenopyrimidine library, using acetic acid and different amine in microwave irradiation for 5 min. Structures of newly synthesized compounds were confirmed by spectral studies. Compound 6g was characterized by single crystal X-ray analysis. All the compounds were also screened for their anti-microbial activity. Few of the compounds are found to be potential antimicrobials. © 2010 Elsevier Masson SAS. All rights reserved.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.Item 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.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, characterization and antibacterial activity of some new pyrazole based Schiff bases(2013) Malladi, S.; Isloor, A.M.; Isloor, S.; Akhila, D.S.; Fun, H.-K.In the present study a series of new Schiff bases were synthesized. All the synthesized compounds were characterized by IR, 1H NMR, mass spectral and elemental analyses. Newly synthesized compounds were screened for their antibacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) activity. The results revealed that, compounds 3f and 3c have exhibited significant biological activity against the tested microorganisms. © 2011.Item Synthesis, characterization and antimicrobial studies of some new trifluoromethyl quinoline-3-carbohydrazide and 1,3,4-oxadiazoles(Royal Society of Chemistry, 2014) Garudachari, B.; Isloor, A.M.; Satyanaraya, M.N.; Kulal, K.; Fun, H.-K.The present paper describes the synthesis of two new series of 7-(trifluoromethyl)-4-hydroxy substituted quinoline carbohydrazide derivatives (6a-e and 7a-g) and N-alkyl-3-(5-phenyl-1,3,4-oxadiazol-2-yl)-7- (trifluoromethyl) quinolin-4-amine derivatives (9a-f). Newly synthesized compounds were characterized by spectral studies. The structure of 9a was evidenced by X-ray crystallographic study. Synthesized compounds were screened for their antibacterial performance against Mycobacterium smegmatis and Pseudomonas aeruginosa. Antifungal activity was also carried out on the fungal stains Candida albicans and Penicillium chrysogenum. Compounds 7a and 9c showed significant antimicrobial activity against all the tested microorganisms. Among all the compounds, 6d and 6e showed the lowest MIC value of 6.25 ?g mL -1 against Mycobacterium smegmatis indicating these compounds can be possible future antituberculosis agents. ©2014 the Partner Organisations.