{"title":"吡嗪酮类化合物ABT-963作为选择性环氧化酶抑制剂的研究进展","authors":"M. Asif","doi":"10.4172/2157-7013.1000243","DOIUrl":null,"url":null,"abstract":"Vicinally disubstituted pyridazinones act as potent and selective COX-2 inhibitors. Compound, ABT-963, (2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one) has an excellent selectivity (ratio of 276, COX-2/COX-1), improved aqueous solubility compared with celecoxib and rofecoxib, high oral anti-inflammatory potency and gastric safety in the animals. After oral administration, ABT-963 reduced prostaglandin (PG) E2 production and reduced the edema. ABT-963 dose dependently reduced nociception. ABT-963 significantly reduced bone loss and soft tissue destruction. ABT-963 is a highly selective COX-2 inhibitor that may be used in the treatment of the pain and inflammation associated with arthritis.","PeriodicalId":150547,"journal":{"name":"Journal of Cell Science and Therapy","volume":"34 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2016-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"A Review on Pyridazinone Compounds ABT-963 as Selective CyclooxygenaseInhibitor\",\"authors\":\"M. Asif\",\"doi\":\"10.4172/2157-7013.1000243\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Vicinally disubstituted pyridazinones act as potent and selective COX-2 inhibitors. Compound, ABT-963, (2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one) has an excellent selectivity (ratio of 276, COX-2/COX-1), improved aqueous solubility compared with celecoxib and rofecoxib, high oral anti-inflammatory potency and gastric safety in the animals. After oral administration, ABT-963 reduced prostaglandin (PG) E2 production and reduced the edema. ABT-963 dose dependently reduced nociception. ABT-963 significantly reduced bone loss and soft tissue destruction. ABT-963 is a highly selective COX-2 inhibitor that may be used in the treatment of the pain and inflammation associated with arthritis.\",\"PeriodicalId\":150547,\"journal\":{\"name\":\"Journal of Cell Science and Therapy\",\"volume\":\"34 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2016-05-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Cell Science and Therapy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4172/2157-7013.1000243\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Cell Science and Therapy","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4172/2157-7013.1000243","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
A Review on Pyridazinone Compounds ABT-963 as Selective CyclooxygenaseInhibitor
Vicinally disubstituted pyridazinones act as potent and selective COX-2 inhibitors. Compound, ABT-963, (2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one) has an excellent selectivity (ratio of 276, COX-2/COX-1), improved aqueous solubility compared with celecoxib and rofecoxib, high oral anti-inflammatory potency and gastric safety in the animals. After oral administration, ABT-963 reduced prostaglandin (PG) E2 production and reduced the edema. ABT-963 dose dependently reduced nociception. ABT-963 significantly reduced bone loss and soft tissue destruction. ABT-963 is a highly selective COX-2 inhibitor that may be used in the treatment of the pain and inflammation associated with arthritis.