Design and development of integrase inhibitors as anti-HIV agents.
A review is presented on different categories of compounds that have been studied for the inhibition of the HIV-1 integrase to develop anti-HIV agents. These compounds are: oligonucleotides (double-stranded, triplex, and G-quartet), curcumin analogues, polyhydroxylated aromatic compounds, diketo acids, caffeoyl- and galloyl - based compounds, hydrazides and amides, tetracyclines, and depsides and depsidones. For all these compounds, the important structural features essential for the inhibition of the integrase are pointed out.
Gupta
S P
SP
Department of Chemistry, Birla Institute of Technology and Science, Pilani, India. spg@bits-pilani.ac.in
Nagappa
A N
AN
D000577:Amides / Q000494:pharmacology / Q000627:therapeutic use; D019380:Anti-HIV Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002109:Caffeic Acids / Q000494:pharmacology / Q000627:therapeutic use; D003474:Curcumin / Q000031:analogs & derivatives / Q000494:pharmacology; D053630:Depsides; D015195:Drug Design; D019427:HIV Integrase / Q000187:drug effects / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D006834:Hydrazines / Q000494:pharmacology / Q000627:therapeutic use; D062385:Hydroxybenzoates / Q000494:pharmacology / Q000627:therapeutic use; D007651:Keto Acids / Q000494:pharmacology / Q000627:therapeutic use; D007783:Lactones / Q000494:pharmacology / Q000627:therapeutic use; D015394:Molecular Structure; D009841:Oligonucleotides / Q000494:pharmacology; D011084:Polycyclic Aromatic Hydrocarbons / Q000494:pharmacology; D013754:Tetracyclines / Q000494:pharmacology / Q000627:therapeutic use
D000577:Amides; D019380:Anti-HIV Agents; D002109:Caffeic Acids; D053630:Depsides; D019428:HIV Integrase Inhibitors; D006834:Hydrazines; D062385:Hydroxybenzoates; D007651:Keto Acids; D007783:Lactones; D009841:Oligonucleotides; D011084:Polycyclic Aromatic Hydrocarbons; D013754:Tetracyclines; C000875:depsidone; D019427:HIV Integrase; D003474:Curcumin