Vega Pérez, José ManuelArgandoña Bertrán, MontserratVega Holm, MargaritaPeriñán, IgnacioPalo Nieto, CarlosBurgos Morón, EstefaníaLópez Lázaro, MiguelVargas Macías, CarmenNieto Gutiérrez, Joaquín JoséIglesias Guerra, Fernando2025-02-032025-02-032012Vega Pérez, J.M., Argandoña Bertrán, M., Vega Holm, M., Periñán, I., Palo Nieto, C., Burgos Morón, E.,...,Iglesias Guerra, F. (2012). Isoprenyl-thiourea and urea derivatives as new farnesyl diphosphate analogues: Synthesis and in vitro antimicrobial and cytotoxic activities. European Journal of Medicinal Chemistry, 58, 591-612. https://doi.org/10.1016/j.ejmech.2012.10.042.0223-52341768-3254https://hdl.handle.net/11441/168078A series of new isoprenyl-thiourea and urea derivatives were synthesized by the reaction of alkyl or aryl isothiocyanate or isocyanate and primary amines. The structures of the compounds were established by 1H NMR, 13C NMR, MS, HRMS and elemental analysis. The new compounds were screened for in vitro antimicrobial activity against seven strains representing different types of gram-positive and gram-negative bacteria. More than a third of the synthesized compounds showed variable inhibition activities against the tested strains. Best antimicrobial activities were found for those thiourea analogues with 3-methyl-2-butenyl, isobutyl or isopentyl groups and aromatic rings possessing electron withdrawing substituents. The new compounds were also subjected to a preliminary screening for antitumoral activity. The presence of a highly lipophilic group and an electron withdrawing group in the aromatic rings enhanced anticancer activity of the synthesized compounds, showing in most cases more activity than that of the controls.application/pdfengAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/AntibacterialAnticancerAntifungalFarnesyl diphosphate analogueIsoprenyl-thiourea/urea derivativeStructural requirementsIsoprenyl-thiourea and urea derivatives as new farnesyl diphosphate analogues: Synthesis and in vitro antimicrobial and cytotoxic activitiesinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccesshttps://doi.org/10.1016/j.ejmech.2012.10.042