Total Synthesis of Aspergillomarasmineâ
A and Related Compounds: A Sulfamidate Approach Enables Exploration of Structure-Activity Relationships.
Angew Chem Int Ed Engl
; 55(42): 13259-13262, 2016 10 10.
Article
en En
| MEDLINE
| ID: mdl-27633338
ABSTRACT
The fungal secondary metabolite aspergillomarasmineâ
A (AMA) has recently been identified as an inhibitor of metallo-ß-lactamases NDM-1 and VIM-2. Described herein is an efficient and practical route to AMA and its related compounds by a sulfamidate approach. In addition, a series of derivatives has been prepared and tested for biological activity in an effort to explore preliminary structure activity relationships. While it was determined that natural LLL isomer of AMA remains the most effective inactivator of NDM-1 enzyme activity both inâ
vitro and in cells, the structure is highly tolerant of the changes in the stereochemistry at positions 3, 6, and 9.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Beta-Lactamasas
/
Ácido Aspártico
/
Inhibidores Enzimáticos
/
Amidas
/
Antibacterianos
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2016
Tipo del documento:
Article
País de afiliación:
Canadá