Bioorganic & Medicinal Chemistry Letters 2009-01-15

Salicylanilide esters of N-protected amino acids as novel antimicrobial agents.

Ales Imramovský, Jarmila Vinsová, Juana Monreal Férriz, Vladimír Buchta, Josef Jampílek

Index: Bioorg. Med. Chem. Lett. 19 , 348-51, (2009)

Full Text: HTML

Abstract

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.


Related Compounds

Related Articles:

Differential expression of efflux pump genes of Mycobacterium tuberculosis in response to varied subinhibitory concentrations of antituberculosis agents.

2015-03-01

[Tuberculosis (Edinb.) 95(2) , 155-61, (2015)]

Enhancement of in vitro activity of tuberculosis drugs by addition of thioridazine is not reflected by improved in vivo therapeutic efficacy.

2014-12-01

[Tuberculosis (Edinb.) 94(6) , 701-7, (2015)]

Disruption of an M. tuberculosis membrane protein causes a magnesium-dependent cell division defect and failure to persist in mice.

2015-02-01

[PLoS Pathog. 11(2) , e1004645, (2015)]

In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis.

2015-01-01

[Antimicrob. Agents Chemother. 59(1) , 136-44, (2014)]

Antagonistic effects of indoloquinazoline alkaloids on antimycobacterial activity of evocarpine.

2015-04-01

[J. Appl. Microbiol. 118(4) , 864-72, (2015)]

More Articles...