INHIBIDORES DE COA-IT Y PAF

• Main Authors: CHILTON, FLOYD, HAROLD, III, WINKLER, JAMES, DAVID, HICKEY, DEIRDRE MARY BERNADETTE
• Format: Patent
• Language: Spanish
• Published: 01.11.2000
• Edition: 7
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; ENZYMOLOGY; HETEROCYCLIC COMPOUNDS; 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; ORGANIC CHEMISTRY; 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

LA TRANSACILASA INDEPENDIENTE DE LA COENZIMA A SE REQUIERE PARA LA LIBERACION DE ACIDO ARAQUIDONICO LIBRE Y PARA LA PRODUCCION DE METABOLITOS DE ACIDO ARAQUIDONICO Y DEL FACTOR DE ACTIVACION DE LAS PLAQUETAS. EL BLOQUEO DE ESTA ENZIMA INHIBE LA PRODUCCION DE ESTOS MEDIADORES INFLAMATORIOS Y SERA DE UTILIZADA TERAPEUTICA PARA UNA AMPLIA GAMA DE ENFERMEDADES Y TRASTORNOS ALERGICOS E INFLAMATORIOS. AQUI DENTRO SE DESCRIBEN COMPUESTOS QUE INHIBEN LA ACCION DE LA COAIT Y QUE POR TANTO SON UTILES PARA EL TRATAMIENTO DE LOS ESTADOS ENFERMIZOS PROVOCADOS POR LA MISMA. EN LA FIGURA SE MUESTRA EL EFECTO DEL COMPUESTO 3 EN LA ACTIVIDAD DE LA COA-IT. Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.