Design, synthesis, and antifungal activity of inhibitors of brassilexin detoxification in the plant pathogenic fungus Leptosphaeria maculans.
Bioorg Med Chem
; 14(3): 714-23, 2006 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-16202609
ABSTRACT
Potential inhibitors of Leptosphaeria maculans mediated detoxification of the phytoalexin brassilexin were designed and synthesized based on the planar heteroaromatic structure of isothiazolo[5,4-b]indole. Screening of these compounds for inhibition of brassilexin detoxification in cultures of L. maculans indicated that 4-(2-chlorophenyl)isothiazole had the largest effect on the rate of brassilexin detoxification. However, the most antifungal compound among the potential inhibitors, isothiazolo[5,4-b]quinoline, did not appear to affect the metabolism of brassilexin noticeably, suggesting that growth inhibition is not sufficient to slow down the rate of brassilexin detoxification. Furthermore, it was determined that 4-arylisothiazoles as well as isothiazolo[5,4-b]thianaphthene displayed antifungal activity against L. maculans.
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Base de dados:
MEDLINE
Assunto principal:
Plantas
/
Ascomicetos
/
Tiazóis
/
Indóis
/
Antifúngicos
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Canadá