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Virtual screening of plant compounds and nonsteroidal anti-inflammatory drugs for inhibition of quorum sensing and biofilm formation in Salmonella.
Microb Pathog
August 2018
Department of Microbiology, Universidade Federal de Viçosa, Viçosa, MG, Brazil. Electronic address:
Article Synopsis
- Salmonella, part of the Enterobacteriaceae family, can adapt to stressful environments and communicate with other bacteria through a mechanism called quorum sensing, even though it lacks a key gene for producing its own signaling molecule.
- Researchers focused on virtual screening of plant compounds and NSAIDs to find inhibitors of this quorum sensing in Salmonella, discovering that many tested compounds had higher binding affinities than known quorum sensing inducers and inhibitors.
- Two molecules, Z-phytol and lonazolac, emerged as promising candidates for further testing, highlighting the potential of combining these inhibitors with antibiotics for improved treatment options against Salmonella infections.
Non-acidic 1,3,4-trisubstituted-pyrazole derivatives as lonazolac analogs with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.
Bioorg Chem
April 2018
Pharmacology Department, Faculty of Veterinary, Cairo University, Cairo, Egypt.
Twelve new compounds of 1,3,4-trisubstituted-pyrazole derivatives possessing two cyclooxygenase-2 (COX-2) pharmacophoric moieties (SOMe or/and SONH) 11a-c, 12a-c, 13a-c and 14a-c were designed and synthesized to be evaluated for their COX inhibition, anti-inflammatory activity, ulcerogenic liability. All compounds were more selective for COX-2 isozyme and showed good in vivo anti-inflammatory activity. The bisaminosulphonyl derivatives (14a-c) were the most COX-2 selective compounds (S.
View Article and Find Full Text PDFModified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.
J Med Chem
October 2012
Department of Pharmaceutical/Medicinal Chemistry, Eberhard Karls University, Tübingen, Auf der Morgenstelle 8, D-72076 Tübingen, Germany.
mPGES-1 is a promising target for development of new anti-inflammatory drugs. We aimed to create mPGES-1 inhibitors by modifying the structure of NSAIDs by replacing the carboxylic acid functionality by sulfonamide moieties. Compounds were also tested for 5-LOX inhibition.
View Article and Find Full Text PDFDetermination of lonazolac and its hydroxy and O-sulfated metabolites by on-line sample preparation liquid chromatography with fluorescence detection.
J Chromatogr B Analyt Technol Biomed Life Sci
January 2002
Institute of Contract Research, Pharmbiodyn, Denzlingen, Germany.
A reliable method, which can be used for the determination of lonazolac and its hydroxylated and O-sulfated metabolites in cell culture media with methyllonazolac as the internal standard is described. The procedure employs on-line sample enrichment using a BioTrap 500 MS (20 x 4 mm I.D.
View Article and Find Full Text PDFScreening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation.
J Anal Toxicol
November 2001
Department of Experimental and Clinical Toxicology, University of Saarland, Homburg, Germany.
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used as analgesic and anti-rheumatic drugs, and they are often misused. A gas chromatographic-mass spectrometric (GC-MS) screening procedure was developed for their detection in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons after extractive methylation. The compounds were separated by capillary GC and identified by computerized MS in the full-scan mode.
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