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Salicylanilide esters of N-protected amino acids as novel antimicrobial agents.
Imramovský, Ales; Vinsová, Jarmila; Férriz, Juana Monreal; Buchta, Vladimír; Jampílek, Josef.
Afiliación
  • Imramovský A; Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic. ales.imramovsky@faf.cuni.cz
Bioorg Med Chem Lett ; 19(2): 348-51, 2009 Jan 15.
Article en En | MEDLINE | ID: mdl-19081718
A series of novel, highly antimicrobial salicylanilide esters of N-protected amino acids were synthesized and characterized. Their in vitro antimicrobial activity against eight fungal strains and Mycobacterium tuberculosis was determined. The compounds had the highest level of activity against Aspergillus fumigatus, Absidia corymbifera and Trichophyton mentagrophytes, and these levels were higher than that of the standard drug fluconazole. In addition, three compounds showed interesting antituberculosis activity, with inhibition ranging from 89% to 99%. (S)-4-Chloro-2-(4-trifluoromethylphenylcarbamoyl)-phenyl 2-benzyloxy-carbonylamino-propionate had the highest level of both antifungal and antimycobacterial activity. The structure-activity relationships of the new compounds are discussed.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Salicilanilidas / Aminoácidos / Antiinfecciosos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: República Checa Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Salicilanilidas / Aminoácidos / Antiinfecciosos Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: República Checa Pais de publicación: Reino Unido