Design, synthesis and structure-activity relationship of novel Relacin analogs as inhibitors of Rel proteins.
Eur J Med Chem
; 70: 497-504, 2013.
Article
in En
| MEDLINE
| ID: mdl-24189495
ABSTRACT
Rel proteins in bacteria synthesize the signal molecules (p)ppGpp that trigger the Stringent Response, responsible for bacterial survival. Inhibiting the activity of such enzymes prevents the Stringent Response, resulting in the inactivation of long-term bacterial survival strategies, leading to bacterial cell death. Herein, we describe a series of deoxyguanosine-based analogs of the Relacin molecule that inhibit in vitro the synthetic activity of Rel proteins from Gram positive and Gram negative bacteria, providing a deeper insight on the SAR for a better understanding of their potential interactions and inhibitory activity. Among the inhibitors evaluated, compound 2d was found to be more effective and potent than our previously reported Relacin.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Drug Design
/
Proto-Oncogene Proteins c-rel
/
Deoxyguanosine
/
Dipeptides
Language:
En
Journal:
Eur J Med Chem
Year:
2013
Document type:
Article
Affiliation country:
Israel