Matches in SemOpenAlex for { <https://semopenalex.org/work/W2951497766> ?p ?o ?g. }
Showing items 1 to 83 of
83
with 100 items per page.
- W2951497766 endingPage "no" @default.
- W2951497766 startingPage "no" @default.
- W2951497766 abstract "Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to relieve physical and mental pain, and to improve patients' quality of life. However, stomach irritation is a major side effect. Most NSAIDs inhibit cyclooxygenases (COXs), and inhibition of COX-1 on the stomach mucous membrane is thought to be responsible for the gastric disturb- ance. Consequently, development efforts have focused on COX-2-selective inhibitors, while COX-1-selective inhibitors have been rather neglected. Subsequently, however, it was shown that inhibition of either COX-1 or COX-2 alone does not induce gastric damage. Therefore, we have developed the COX-1-selective inhibitor N-(4-aminophenyl)-4-trifluoromethylbenzamide (TFAP), which shows analgesic activity without causing gastric damage. However, metabolism of TFAP generates a colored metabolite, resulting in red-purple coloration of urine after administration. In addition, the analgesic activity of TFAP is weaker than that of indomethacin. Thus, we designed a series of new COX-1-selective inhibitors, the 5-amino-2-ethoxy-N-(substituted)benzamide (ABEX) series, in order to avoid formation of the colored metabolite by modifying the diaminopyridine skeleton. As a result of structural modification and in vitro and in vivo testing of compounds in the ABEX series, we found a novel COX-1-selective inhibitor, 5-amino-2-ethoxy-N-(3-trifluoromethylphenyl)benzamide (ABEX-3TF), which shows better analgesic activity than indomethacin, and does not cause coloration of urine." @default.
- W2951497766 created "2019-06-27" @default.
- W2951497766 creator A5042086715 @default.
- W2951497766 creator A5055587462 @default.
- W2951497766 creator A5069761560 @default.
- W2951497766 creator A5081660375 @default.
- W2951497766 date "2011-08-18" @default.
- W2951497766 modified "2023-09-23" @default.
- W2951497766 title "ChemInform Abstract: Significance and Creation of Novel Cyclooxygenase-1 (COX-1) Selective Inhibitors" @default.
- W2951497766 cites W2326018575 @default.
- W2951497766 doi "https://doi.org/10.1002/chin.201137253" @default.
- W2951497766 hasPublicationYear "2011" @default.
- W2951497766 type Work @default.
- W2951497766 sameAs 2951497766 @default.
- W2951497766 citedByCount "0" @default.
- W2951497766 crossrefType "journal-article" @default.
- W2951497766 hasAuthorship W2951497766A5042086715 @default.
- W2951497766 hasAuthorship W2951497766A5055587462 @default.
- W2951497766 hasAuthorship W2951497766A5069761560 @default.
- W2951497766 hasAuthorship W2951497766A5081660375 @default.
- W2951497766 hasConcept C150903083 @default.
- W2951497766 hasConcept C181199279 @default.
- W2951497766 hasConcept C185592680 @default.
- W2951497766 hasConcept C203014093 @default.
- W2951497766 hasConcept C207001950 @default.
- W2951497766 hasConcept C2777063393 @default.
- W2951497766 hasConcept C2777477808 @default.
- W2951497766 hasConcept C2779422922 @default.
- W2951497766 hasConcept C2779689624 @default.
- W2951497766 hasConcept C2780231548 @default.
- W2951497766 hasConcept C2780820201 @default.
- W2951497766 hasConcept C55493867 @default.
- W2951497766 hasConcept C71240020 @default.
- W2951497766 hasConcept C71924100 @default.
- W2951497766 hasConcept C86803240 @default.
- W2951497766 hasConcept C98274493 @default.
- W2951497766 hasConceptScore W2951497766C150903083 @default.
- W2951497766 hasConceptScore W2951497766C181199279 @default.
- W2951497766 hasConceptScore W2951497766C185592680 @default.
- W2951497766 hasConceptScore W2951497766C203014093 @default.
- W2951497766 hasConceptScore W2951497766C207001950 @default.
- W2951497766 hasConceptScore W2951497766C2777063393 @default.
- W2951497766 hasConceptScore W2951497766C2777477808 @default.
- W2951497766 hasConceptScore W2951497766C2779422922 @default.
- W2951497766 hasConceptScore W2951497766C2779689624 @default.
- W2951497766 hasConceptScore W2951497766C2780231548 @default.
- W2951497766 hasConceptScore W2951497766C2780820201 @default.
- W2951497766 hasConceptScore W2951497766C55493867 @default.
- W2951497766 hasConceptScore W2951497766C71240020 @default.
- W2951497766 hasConceptScore W2951497766C71924100 @default.
- W2951497766 hasConceptScore W2951497766C86803240 @default.
- W2951497766 hasConceptScore W2951497766C98274493 @default.
- W2951497766 hasIssue "37" @default.
- W2951497766 hasLocation W29514977661 @default.
- W2951497766 hasOpenAccess W2951497766 @default.
- W2951497766 hasPrimaryLocation W29514977661 @default.
- W2951497766 hasRelatedWork W130440447 @default.
- W2951497766 hasRelatedWork W1567838639 @default.
- W2951497766 hasRelatedWork W2017917394 @default.
- W2951497766 hasRelatedWork W2069024951 @default.
- W2951497766 hasRelatedWork W2084224669 @default.
- W2951497766 hasRelatedWork W2095710337 @default.
- W2951497766 hasRelatedWork W2166699495 @default.
- W2951497766 hasRelatedWork W2189651229 @default.
- W2951497766 hasRelatedWork W2205478614 @default.
- W2951497766 hasRelatedWork W2214786699 @default.
- W2951497766 hasRelatedWork W2278280617 @default.
- W2951497766 hasRelatedWork W2326018575 @default.
- W2951497766 hasRelatedWork W2372712126 @default.
- W2951497766 hasRelatedWork W2411901332 @default.
- W2951497766 hasRelatedWork W2552087272 @default.
- W2951497766 hasRelatedWork W2889707681 @default.
- W2951497766 hasRelatedWork W347227128 @default.
- W2951497766 hasRelatedWork W655910326 @default.
- W2951497766 hasRelatedWork W2129644223 @default.
- W2951497766 hasRelatedWork W2487998021 @default.
- W2951497766 hasVolume "42" @default.
- W2951497766 isParatext "false" @default.
- W2951497766 isRetracted "false" @default.
- W2951497766 magId "2951497766" @default.
- W2951497766 workType "article" @default.