Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity.
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed.
Li
Hongcai
H
School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province 250012, PR China.
Wang
Chao
C
Sanchez
Tino
T
Tan
Yanmei
Y
Jiang
Chunying
C
Neamati
Nouri
N
Zhao
Guisen
G
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D019427:HIV Integrase / Q000737:chemistry / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007651:Keto Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000577:Amides; D019428:HIV Integrase Inhibitors; D007651:Keto Acids; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1