Selective inhibitors of prostaglandin endoperoxide synthase-2

摘要

The present invention provides a compound of the formula ;wherein when X is S; R is selected from the group consisting of CH₃, CH₂CH₃, CH₂Ph, (CH₂)₂Ph, (CH₂)₂CH₃, (CH₂)₃CH₃, (CH₂)₄CH₃, CH₂)₅CH₃, (CH₂)₆CH₃, (CH₂)₂O(CH₂)₃CH₃, CH₂HCCH(CH₂)₃CH₃, CH₂CC(CH₂)₃CH₃, CH₂CC(CH₂)₂CH₃, CH₂CCCH₂CH₃, CH₂CCCH₃, CH₂CCH, CH₂CC(CH₂)₄CH₃, CH₂CC(CH₂)₅CH₃, CH₂CC(CH₂)₆CH₃, (CH₂)₂CC(CH₂)₂CH₃, CH(Ch₃)CC(CH₂)₃CH₃, (CH₂)₆I, (CH₂)₆Br, (CH₂)₅Br, (CH₂)₅COOH and (CH₂)₅OCOCH₃, and R is selected from the group consisting of CH₃, CF₃, CH₂Cl, CH₂Br, CH₂CH₃, NH₂, and OSO₂CH₃; wherein when R is CH₃, R can not be CH₃ or CH₂Cl; wherein when R is CH₂CH₃, R can not be CH₃; wherein when X is Se, R is (CH₂)₆CH₃, and R is CH₃ or a pharmaceutically acceptable salt or hydrate thereof; and wherein when X is O, R is CH₂CC(CH₂)₃CH₃, and R is CH₃ or a pharmaceutically acceptable salt or hydrate thereof. Also provided is a method of inhibiting the synthesis of prostaglandin endoperoxide synthase-2 (PGHS-2) in a mammal.