Use of quinolinone compound as hCBS enzyme inhibitor

• Main Authors: Fang Wu, Jing Yu, Yueyang Zhou
• Format: Patent
• Language: English
• Published: 15.06.2016
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; ENZYMOLOGY; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MUTATION OR GENETIC ENGINEERING; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES OF PREPARING SUCH COMPOSITIONS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; TESTING; VINEGAR; WINE

The use of quinolinone compound as human cystathionine β-synthase (hCBS) enzyme inhibitors, particularly the use of the compound 7-amino-2-hydroxy-5-imino-6,7-dihydroquinolin-8(5H)-one as an hCBS enzyme inhibitor. The small molecule compound is 5,7-diamino quinolinone compound, the IC50 of which for in vitro hCBS enzyme assay is 20 µM. Such small molecule compound can be used as a drug tool for studying H2S signaling pathways, and as a lead compound for developing the drugs for treating the H2S related diseases, such as circulatory shock, stroke, Down's syndrome, etc. In another aspect, a method for inhibiting in vitro hCBS using7-amino-2-hydroxy-5-imino-6,7-dihydroquinolin-8(5H)-one, said method involving the detection of H2S. In another aspect, a method for inhibiting the activity of the intracellular hCBS enzyme using7-amino-2-hydroxy-5-imino-6,7-dihydroquinolin-8(5H)-one, the method involving the detection of H2S.