期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 -, 页码 591-612出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.10.042
关键词
Antibacterial; Antifungal; Anticancer; Farnesyl diphosphate analogue; Isoprenyl-thiourea/urea derivative; Structural requirements
资金
- Junta de Andalucia, the Spanish Ministerio de Educacion y Ciencia (MEC) [P06-FQM-01885, CTQ2007-61185]
- Junta de Andalucia [P09-AGR4597]
- Ministerio de Asuntos Exteriores y Cooperacion [AECID A/023577/09]
A 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 H-1 NMR, C-13 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. (C) 2012 Elsevier Masson SAS. All rights reserved.
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