Vijesh, A.M.Isloor, A.M.Telkar, S.Peethambar, S.K.Rai, S.Isloor, N.2026-02-052011European Journal of Medicinal Chemistry, 2011, 46, 8, pp. 3531-35362235234https://doi.org/10.1016/j.ejmech.2011.05.005https://idr.nitk.ac.in/handle/123456789/27216In 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.3 (2,4 dichlorophenyl) 4 (4,5 diphenyl 1h imidazol 2 yl) 1h pyrazole3 (2,5 dichlorothiophen 3 yl) 4 (4,5 diphenyl 1h imidazol 2 yl) 1h pyrazole3 (biphenyl 4 yl) 4 (4,5 diphenyl 1h imidazol 2 yl) 1h pyrazole3 (biphenyl 4 yl) 4 [4,5 bis(4 bromophenyl) 1h imidazol 2 yl] 1h pyrazole4 (4,5 diphenyl 1h imidazol 2 yl) 3 (4 methylphenyl) 1h pyrazole4 (4,5 diphenyl 1h imidazol 2 yl) 3 [4 (methylsulfanyl)phenyl] 1h pyrazole4 [4,5 bis(4 bromophenyl) 1h imidazol 2 yl] 3 (2,4 dichlorophenyl) 1h pyrazole4 [4,5 bis(4 bromophenyl) 1h imidazol 2 yl] 3 (2,5 dichlorothiophen 3 yl) 1h pyrazole4 [4,5 bis(4 bromophenyl) 1h imidazol 2 yl] 3 (4 methylphenyl) 1h pyrazole4 [4,5 bis(4 bromophenyl) 1h imidazol 2 yl] 3 [4 (methylsulfanyl)phenyl] 1h pyrazoleantiinfective agentfluconazoleimidazole derivativem ethyl 2 [5 oxo 2 thioxo 3 [[3 (4 tolyl)] 1h pyrazol 4 yl]methyleneamino]imidazolidin 4 ylidene)acetatemethyl 2 [3 [[3 (2,4 dichlorophenyl) 1h pyrazol 4 yl]methyleneamino] 5 oxo 2 thioxoimidazolidin 4 ylidene]acetatemethyl 2 [3 [[3 (2,5 dichlorothiophen 3 yl) 1h pyrazol 4 yl]methyleneamino] 5 oxo 2 thioxoimidazolidin 4 ylidene]acetatemethyl 2 [3 [[3 [4 (methylthio)phenyl] 1h pyrazol 4 yl]methyleneamino] 5 oxo 2 thioxoimidazolidin 4 ylidene]acetatepyrazole derivativeunclassified druganimal behavioranimal experimentantibacterial activityantifungal activityArthroderma gypseumarticleAspergillus flavusAspergillus nigerBacillus subtilisCandida albicansClostridium perfringensconcentration responsedrug potencydrug safetydrug structuredrug synthesisEscherichia colifemalein vitro studymousenonhumanPseudomonas aeruginosaSalmonella typhimuriumStaphylococcus aureusstructure activity relationTrichophyton rubrumAdministration, OralAnimalsAnti-Infective AgentsBacterial InfectionsFemaleFungiGram-Negative BacteriaGram-Positive BacteriaImidazolesMaximum Tolerated DoseMiceMicrobial Sensitivity TestsMolecular StructureMycosesPyrazoles