N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation.
Future Med Chem
; 15(19): 1791-1806, 2023 10.
Article
in En
| MEDLINE
| ID: mdl-37877255
ABSTRACT
Background:
The development of novel antimicrobial drugs is an essential part of combatting the uprising of antimicrobial resistance. Proper hit-to-lead development is crucially needed. Methods &results:
We present a hit-expansion study of N-pyrazinyl- and N-pyridyl-hydroxybenzamides with a comprehensive determination of structure-activity relationships. The antimicrobial screening revealed high selectivity to staphylococci along with antimycobacterial activity with the best value of 6.25 µg/ml against Mycobacterium tuberculosis H37Rv. We proved an inhibition of proteosynthesis and a membrane depolarization of methicillin-resistant Staphylococcus aureus.Conclusion:
Our results are a good starting point for further development of new antimicrobial compounds, where the next step would be tuning the potential between relatively nonspecific membrane depolarization effect and specific inhibition of proteosynthesis.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Methicillin-Resistant Staphylococcus aureus
/
Anti-Infective Agents
Language:
En
Journal:
Future Med Chem
Year:
2023
Document type:
Article
Affiliation country:
Czech Republic