Literature summary for 1.3.8.2 extracted from

Wang, Y.; Chen, F.; Di, H.; Xu, Y.; Xiao, Q.; Wang, X.; Wei, H.; Lu, Y.; Zhang, L.; Zhu, J.; Sheng, C.; Lan, L.; Li, J.
Discovery of potent benzofuran-derived diapophytoene desaturase (CrtN) inhibitors with enhanced oral bioavailability for the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections (2016), J. Med. Chem., 59, 3215-3230 .

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli	Staphylococcus aureus

Inhibitors

Inhibitors	Comment	Organism	Structure
(E)-N-(benzofuran-7-ylmethyl)-N-methyl-3-(4-(trifluoromethyl)-phenyl)prop-2-en-1-amine	inhibits the pigment production of S. aureus Newman and three MRSA strains, without any impact on the survival of four strains. Compound shows good oral bioavailability and safety profiles. IC50 value for growth of Staphylococcus aureus 3.9 nM	Staphylococcus aureus

Organism

Organism	UniProt	Comment	Textmining
Staphylococcus aureus	O07855	-	-
Staphylococcus aureus Newman	O07855	-	-

Synonyms

Synonyms	Comment	Organism
CrtN	-	Staphylococcus aureus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000339	-	pH 7.5, 37°C	Staphylococcus aureus	(E)-N-(benzofuran-7-ylmethyl)-N-methyl-3-(4-(trifluoromethyl)-phenyl)prop-2-en-1-amine

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Release 2023.1 (January 2023)