1080025-90-6Relevant academic research and scientific papers
Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid
Halambage, Upul D.,Wong, Jason P.,Melancon, Bruce J.,Lindsley, Craig W.,Aiken, Christopher
supporting information, p. 5190 - 5195 (2015/09/15)
Despite the availability of>30 effective drugs for managing HIV-1 infection, no current therapy is curative, and long-term management is challenging owing to the emergence and spread of drug-resistant mutants. Identification of drugs against novel HIV-1 targets would expand the current treatment options and help to control resistance. The highly conserved HIV-1 capsid protein represents an attractive target because of its multiple roles in replication of the virus. However, the low antiviral potencies of the reported HIV-1 capsid-targeting inhibitors render them unattractive for therapeutic development. To facilitate the identification of more-potent HIV-1 capsid inhibitors, we developed a scintillation proximity assay to screen for small molecules that target a biologically active and specific intersubunit interface in the HIV-1 capsid. The assay, which is based on competitive displacement of a known capsid-binding small-molecule inhibitor, exhibited a signal-to-noise ratio of>9 and a Z factor of>0.8. In a pilot screen of a chemical library containing 2,400 druglike compounds, we obtained a hit rate of 1.8%. This assay has properties that are suitable for screening large compound libraries to identify novel HIV-1 capsid ligands with antiviral activity.
Syntheses of IAA- and IPA-amino acid conjugates
Katritzky, Alan R.,Khelashvili, Levan,Munawar, Ali
supporting information; experimental part, p. 9171 - 9173 (2009/04/11)
(Chemical Equation Presented) Amino acid derivatives of IAA and IPA are prepared conveniently and efficiently by coupling of readily available 2a-b with diverse free amino acids 3a-g and (3c+3c′) to give compounds 4a-j, (4c+4c′) and (4h+4h′) in 38-70% yie
