Thomas, K.D.Vasudeva Adhikari, A.V.Shetty, N.S.2026-02-052010European Journal of Medicinal Chemistry, 2010, 45, 9, pp. 3803-38102235234https://doi.org/10.1016/j.ejmech.2010.05.030https://idr.nitk.ac.in/handle/123456789/27422A 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.1 [1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl] n,n dimethyl methanamine1 [4 [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl]piperazin 1 yl]ethanone4 [4 [(4 cyclohexylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methylquinoline4 [4 [(4 ethylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methyl quinoline4 [4 [(4 ethylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methylquinoline4 [4 [(4 isopropylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methylquinoline4 [4 [[4 (2 fluorophenyl)piperazin 1 yl]methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methylquinoline4 [4 [[4 (4 fluorophenyl)piperazin 1 yl]methyl] (1h) 1,2,3 triazol 1 yl] 6 methoxy 2 methylquinoline6 methoxy 2 methyl 4 [4 [(4 methylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 2 methyl 4 [4 [(4 morpholinopiperidin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 2 methyl 4 [4 [(4 p tolylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 2 methyl 4 [4 [(4 phenylpiperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 2 methyl 4 [4 [(piperidin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 2 methyl 4 [4 [(pyrrolidin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl]quinoline6 methoxy 4 [4 [(4 (4 methoxyphenyl) piperazin 1 yl)methyl] (1h) 1,2,3 triazol 1 yl] 2 methylquinoline6 methoxy 4 [4 [[4 (4 methoxy 2 methylphenyl)piperazin 1 yl]methyl] (1h) 1,2,3 triazol 1 yl] 2 methylquinolineciclopiroxolamineciprofloxacinn [1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl cyclopropanaminen [1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methylaminen [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl]butan 2 aminen [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) imidazol 4 yl]methyl]cyclohexanaminen [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) imidazol 4 yl]methyl]cyclopentanaminen ethyl n [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl]ethanaminen1 [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl] n1,n2,n2 trimethylethane 1,2 diaminen1 [[1 (6 methoxy 2 methylquinolin 4 yl) (1h) 1,2,3 triazol 4 yl]methyl] n3,n3 diimethylpropane 1,3 diaminequinoline derivativeunclassified drugantifungal activityantimicrobial activityarticleAspergillus flavusAspergillus fumigatusbacterial strainbacterium cultureCandida albicanscontrolled studydrug designdrug structuredrug synthesisEscherichia colifungal straininfrared spectroscopyKlebsiella pneumoniaeminimum inhibitory concentrationnonhumannuclear magnetic resonance spectroscopyPenicillium marneffeiPseudomonas aeruginosaStaphylococcus aureusStreptococcus pyogenesTrichophyton mentagrophytesAminesAniline CompoundsAnti-Infective AgentsBacteriaDrug DesignFungiMicrobial Sensitivity TestsQuinolinesTriazoles