Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity

Hongcai Li; Chao Wang; Tino Sanchez; Yanmei Tan; Chunying Jiang; Nouri Neamati; Guisen Zhao

doi:10.1016/j.bmc.2009.01.077

Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity

Bioorg Med Chem. 2009 Apr 1;17(7):2913-9. doi: 10.1016/j.bmc.2009.01.077. Epub 2009 Feb 7.

Authors

Hongcai Li¹, Chao Wang, Tino Sanchez, Yanmei Tan, Chunying Jiang, Nouri Neamati, Guisen Zhao

Affiliation

¹ School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province 250012, PR China.

PMID: 19269185
DOI: 10.1016/j.bmc.2009.01.077

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amides / chemical synthesis*
Amides / chemistry
HIV Integrase / chemistry
HIV Integrase / metabolism*
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / chemistry
HIV Integrase Inhibitors / pharmacology
Keto Acids / chemical synthesis*
Keto Acids / chemistry
Keto Acids / pharmacology
Structure-Activity Relationship

Substances

Amides
HIV Integrase Inhibitors
Keto Acids
HIV Integrase
p31 integrase protein, Human immunodeficiency virus 1