153223-14-4Relevant academic research and scientific papers
Functionalized aliphatic P2/P2' analogs of HIV-1 protease inhibitor DMP323
Smallheer, Joanne M.,McHugh, Robert J.,Chang, Chong-Hwan,Kaltenbach III, Robert F.,Worley, Tabitha V.,Klabe, Ronald M.,Bacheler, Lee T.,Rayner, Marlene M.,Erickson-Viitanen, Susan,Seitz, Steven P.
, p. 1365 - 1370 (2007/10/03)
A series of analogs of HIV protease inhibitor DMP323 containing functionalized aliphatic P2/P2' groups was prepared and evaluated for HIV protease inhibition and antiviral activity in a cell-based assay. Asymmetric compounds with a 5-hydroxypentyl substituent at P2 and a benzylic substituent at P2' showed increased potency over the corresponding symmetrically substituted analogs.
Cyclic HIV protease inhibitors: Synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas
Lam, Patrick Y. S.,Ru, Yu,Jadhav, Prabhakar K.,Aldrich, Paul E.,DeLucca, George V.,Eyermann, Charles J.,Chang, Chong-Hwan,Emmett, George,Holler, Edward R.,Daneker, Wayne F.,Li, Liangzhu,Confalone, Pat N.,McHugh, Robert J.,Han, Qi,Li, Renhua,Markwalder, Jay A.,Seitz, Steven P.,Sharpe, Thomas R.,Bacheler, Lee T.,Rayner, Marlene M.,Klabe, Ronald M.,Shum, Linyee,Winslow, Dean L.,Kornhauser, David M.,Jackson, David A.,Erickson-Viitanen, Susan,Hodge, C. Nicholas
, p. 3514 - 3525 (2007/10/03)
High-resolution X-ray structures of the complexes of HIV-1 protease (HIV-1PR) with peptidomimetic inhibitors reveal the presence of a structural water molecule which is hydrogen bonded to both the mobile flaps of the enzyme and the two carbonyls flanking
