| 摘要 |
The present invention provides an integrase inhibitor. The inventors have found the following compound of formula (I) possessing an integrase inhibitory activity.;;(wherein, RC and RD taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxyl, mercapto or amino; Z is O, S or NH; RA is a group shown by;;(wherein, C ring is N-containing aromatic heterocycle) or the like). |
| 主权项 |
1. A method of inhibiting HIV integrase activity, the method comprising contacting an HIV integrase protein with an effective amount of a compound of Formula (I): wherein RC and RD taken together with the neighboring carbon atoms form a 5- to 6-membered heterocycle which may contain heteroatom (s) of N and/or O and may be condensed with a benzene ring; Y is hydroxy; Z is O; the ring formed by RC and RD is optionally substituted with hydrogen, C1-C6 alkyl, or C3-C6 cycloalkyl; RA is wherein ring C is selected from the group consisting of pyridin-2-yl, pyrimidin-4-yl, pyrimidin-2-yl, and 1,3,4-oxadiazol-2-yl, or wherein X is O and RB is amino, 2-furyl, or phenyl; and at least one of RB and the ring formed by RC and RD is substituted with —Z1—Z2—Z3—R1, wherein Z is independently a bond or C1-C6 alkylene; Z2 is independently a bond or —NR2CO—; Z3 is a bond; R2 is hydrogen; and R1 is independently aryl or heteroaryl, wherein R1 is optionally substituted with one or more substituents selected from the group consisting of C1-C6 alkyl and halogen; or a salt thereof. |
