Garudachari, B.Isloor, A.M.Satyanarayana, M.N.Fun, H.-K.Pavithra, N.Kulal, A.2026-02-052013European Journal of Medicinal Chemistry, 2013, 68, , pp. 422-4322235234https://doi.org/10.1016/j.ejmech.2013.07.021https://idr.nitk.ac.in/handle/123456789/26861Three 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.1 (2,4 dichlorobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide1 (2,4 dichlorobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acid1 (2,4 dichlorobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide1 (2,4 dichlorobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acid1 (4 cyanobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide1 (4 cyanobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acid1 (4 cyanobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide1 (4 cyanobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acid4 oxo 1 (prop 2 yn 1 yl) 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide4 oxo 1 (prop 2 yn 1 yl) 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acid4 oxo 1 (prop 2 yn 1 yl) 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carbohydrazide4 oxo 1 (prop 2 yn 1 yl) 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylic acidantifungal agentciprofloxacinethyl 1 (2,4 dichlorobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylateethyl 1 (2,4 dichlorobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylateethyl 1 (4 cyanobenzyl) 4 oxo 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylateethyl 1 (4 cyanobenzyl) 4 oxo 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylateethyl 4 oxo 1 (prop 2 yn 1 yl) 7 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylateethyl 4 oxo 1 (prop 2 yn 1 yl) 8 (trifluoromethyl) 1,4 dihydroquinoline 3 carboxylatequinolone derivativetrifluoromethylquinolone derivativeunclassified drugalkylationantibacterial activityantifungal activityarticlebacterial straincontrolled studycrystal structuredrug designdrug screeningdrug selectivitydrug synthesisin vitro studyminimum inhibitory concentrationnonhumanX ray crystallographyAntibacterial studyAntifungal studyRegioselective synthesisTrifluoromethylquinolone derivativeAnti-Infective AgentsBacteriaCandida albicansCiprofloxacinCrystallography, X-RayDrug DesignFluorineMolecular StructurePenicillium chrysogenumQuinolinesDesign and regioselective synthesis of trifluoromethylquinolone derivatives as potent antimicrobial agents