Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.
Antimicrob Agents Chemother
; 54(3): 1315-8, 2010 Mar.
Article
em En
| MEDLINE
| ID: mdl-20047919
ABSTRACT
Thirty-nine new thiazolide/thiadiazolide compounds were compared with the nitrothiazole nitazoxanide for activity against Cryptosporidium parvum development in HCT-8 cells. Twenty-seven agents exerted > or =90% inhibition. Agents with a lower 50% inhibitory concentration (IC(50)) than nitazoxanide were either NO(2) or halogen 5 substituted on the thiazole moiety. Other 5 substitutions such as methyl, C(3)H(7), C(6)H(11), H, SO(2)CH(3), and SCH(3) negatively impacted activity. Five-substituted deacetylated analogues exhibited higher IC(50)s than their acetylated counterparts. Halogeno-thiazolide/thiadiazolides may provide valuable nitro-free alternatives to nitazoxanide.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiadiazinas
/
Tiazóis
/
Cryptosporidium parvum
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article