The effects of novel heme oxygenase inhibitors on the growth of Pseudomonas aeruginosa
摘要:
Objectives: This study was aimed to develop small molecule inhibitors of the P. aeruginosa heme oxygenase (paHemO) as potential treatment of infections caused by P. aeruginosa.Methods: New compounds were designed based on the crystal structure of pa-HemO. The binding affinities (K-D) were determined using intrinsic fluorescence quenching assays. The anti-microbial effects of the new compounds was evaluated by minimal inhibitory concentration 50% (MIC50).Results: Eleven compounds were synthesized as potential pa-HemO inhibitors. New compounds demonstrated Ku values ranging from 1.5 to 180 mu M, and MIC50 values ranging from 26 to 260 mu M/mL. The compounds had good affinity with HemO and promising anti-microbial effects on P. aeruginosa.Conclusions: The new inhibitors described herein can inhibit the growth of P. aeruginosa via the inhibition of paHemO. There may be broad prospects for HemO inhibitors to treat P. aeruginosa related infections.
A compound is represented by Chemical Formula 1.
In Chemical Formula 1, R
1
to R
4
, R
11a
to R
14c
, and n are the same as defined in the detailed description.
Verfahren zur Herstellung von N-substituierten Benz[c,d]indol-2-onen
申请人:BAYER AG
公开号:EP0185240A2
公开(公告)日:1986-06-25
Dei Herstellung von N-substituierten Benz[c,d]indol-2- onen erfolgt durch Umsetzung von am Stickstoff nichtsubstituierten Benz [c,d]-indol-2-onen mit einem Alkylierungsmittel in einem zweiphasigen System in Gegenwart einer Base und eines Phasentransferkatalysators.
N 取代的苯并[c,d]吲哚-2-酮是在碱和相转移催化剂存在下,通过在两相体系中使氮上未取代的苯并[c,d]吲哚-2-酮与烷基化剂反应制备的。
The application relates to compounds of the Chemical Formula 1 having improved infrared absorption properties. The compounds are useful for infrared absorbers, infrared (IR) absorbing/blocking films, photoelectric devices, image sensors, and electronic devices comprising the photoelectric devices or sensors.