Synthesis and biological evaluation of novel pleuromutilin derivatives with nitrogen-containing heterocycles as antibacterial agents / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1297-1304, 2015.
Artigo
em Chinês
| WPRIM
| ID: wpr-320086
ABSTRACT
A series of new pleuromutilins derivatives were designed and synthesized through coupling 2-aminothiazole ring of WL001 with different nitrogen-containing substituted heterocycles in the side chain. Their biological activities were evaluated against both Gram-positive and Gram-negative clinical bacteria in vitro Most new compounds displayed specificity to certain strain of bacteria. Particularly, compounds with saturated nitrogen-containing heterocycles exhibited significant antibacterial activities (0.062 5-8 µg · mL(-1)) superior or similar to those of amoxicillin, tiamulin and levofloxcin. Furthermore, treatment with 15a and 15b having piperidine or morpholine residues also could effectively inhibit Gram-negative bacteria. Therefore, our novel findings may provide a new insight into the design of novel pleuromutilin derivatives and lay the basis for further studies on the treatment of drug-resistance of pathogenic bacteria.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Relação Estrutura-Atividade
/
Testes de Sensibilidade Microbiana
/
Química
/
Diterpenos
/
Levofloxacino
/
Bactérias Gram-Negativas
/
Amoxicilina
/
Antibacterianos
/
Nitrogênio
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2015
Tipo de documento:
Artigo
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