Synthesis and antibacterial activity of pentacyclines: a novel class of tetracycline analogs.
J Med Chem
; 54(11): 3704-31, 2011 Jun 09.
Article
em En
| MEDLINE
| ID: mdl-21500832
ABSTRACT
Employing a highly efficient total synthesis approach, we synthesized and evaluated for antibacterial activity diverse and novel pentacycline analogs with systematic variations at C7, C8, C9, and C10. Certain substitution groups, as well as substitution patterns at various positions, were found to be preferred for increased antibacterial activity. A number of pentacycline analogs displayed potent activity in vitro and in vivo, especially against Gram-positive organisms. Several analogs have also shown promising oral bioavailability in rats and cynomolgus monkey.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tetraciclinas
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Testes de Sensibilidade Microbiana
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Bactérias Gram-Negativas
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Bactérias Gram-Positivas
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Antibacterianos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article