207123-94-2Relevant academic research and scientific papers
Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents
Kaltenbach III, Robert F.,Klabe, Ronald M.,Cordova, Beverly C.,Seitz, Steven P.
, p. 2259 - 2262 (2007/10/03)
A series of alkyl substituted P1/P1' analogs was prepared in an attempt to increase translation of the 3-aminoindazole class of HIV protease inhibitors. Increasing the lipophilicity of the P1/P1' residues dramatically improved translation of enzyme activity to antiviral activity in the whole cell assay.
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups
Rodgers, James D.,Johnson, Barry L.,Wang, Haisheng,Erickson-Viitanen, Susan,Klabe, Ronald M.,Bacheler, Lee,Cordova, Beverly C.,Chang, Chong-Hwan
, p. 715 - 720 (2007/10/03)
Cyclic ureas containing 3-aminoindazole P2/P2' groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a K(i) 0.01 nM but poor translation of enzyme activity to antiviral activity was observed. A series of 3-alkylaminoindazoles revealed that translation improved with increasing lipophilicity. An X-ray crystal structure of 6 bound to HIV protease was obtained.
