249728-38-9Relevant articles and documents
HIV protease inhibitors
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, (2008/06/13)
The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: A lead HIV protease inhibitor
Vara Prasad,Boyer, Frederick E.,Domagala, John M.,Ellsworth, Edmund L.,Gajda, Christopher,Hamilton, Harriet W.,Hagen, Susan E.,Markoski, Larry J.,Steinbaugh, Bruce A.,Tait, Bradley D.,Humblet, Christine,Lunney, Elizabeth A.,Pavlovsky, Alexander,Rubin, John R.,Ferguson, Donna,Graham, Neil,Holler, Tod,Hupe, Donald,Nouhan, Carolyn,Tummino, Peter J.,Urumov,Zeikus, Eric,Zeikus, Greg,Gracheck, Stephen J.,Saunders, James M.,Vanderroest, Steven,Brodfuehrer, Joanne,Iyer,Sinz,Gulnik, Sergei V.,Erickson, John W.
, p. 2775 - 2800 (2007/10/03)
With the insight generated by the availability of X-ray crystal structures of various 5,6-dihydropyran-2-ones bound to HIV PR, inhibitors possessing various alkyl groups at the 6-position of 5,6-dihydropyran-2-one ring were synthesized. The inhibitors pos