Your browser doesn't support javascript.
loading
Anti-MRSA activities of cycloberberine derivatives with a novel chemical scaffold / 药学学报
Yao Xue Xue Bao ; (12): 1627-1635, 2019.
Article en Zh | WPRIM | ID: wpr-780268
Biblioteca responsable: WPRO
ABSTRACT
Using CBBR as the parent core constructed in our lab, we designed and synthesized 15 novel compounds with diverse structures for evaluation of anti-bacterial activities. Structure activity relationship studies revealed that ① ring C was essential for the activity; ② 7,8- or 8,13-disubstituted CBBR derivatives showed ideal activities, weaker or similar to those corresponding to 7-, 8-, or 13-monosubstituted CBBR derivatives. Among those, compound 9a showed the most potential activity against MRSA/VISA isolates with MIC values of 1-2 μg·mL-1, much better than Lev. 9a also displayed higher stability in the plasma and liver microsomes. Molecular docking indicated that 9a might target bacterial DNA Topo IV ParE subunit, indicating a mode of action distinct from current antibacterial drugs on market. The results provided key scientific evidence for developing such compounds into a new family of anti-MRSA drugs.
Palabras clave
Texto completo: 1 Índice: WPRIM Idioma: Zh Revista: Yao Xue Xue Bao Año: 2019 Tipo del documento: Article
Texto completo: 1 Índice: WPRIM Idioma: Zh Revista: Yao Xue Xue Bao Año: 2019 Tipo del documento: Article