Cover Picture: Discovery of MK‐8970: An Acetal Carbonate Prodrug of Raltegravir with Enhanced Colonic Absorption (ChemMedChem 2/2015). Issue 2 (February 2015)

• Record Type: Journal Article
• Authors: Walji, Abbas M.; Sanchez, Rosa I.; Clas, Sophie‐Dorothee; Nofsinger, Rebecca; de Lera Ruiz, Manuel; Li, Jing; Bennet, Amrithraj; John, Christopher; Bennett, David Jonathan; Sanders, John M.; Di Marco, Christina N.; Kim, Somang Hope; Balsells, Jaume; Ceglia, Scott S.; Dang, Qun; Manser, Kimberly; Nissley, Becky; Wai, John S.; Hafey, Michael; Wang, Junying; Chessen, Gene; Templeton, Allen; Higgins, John; Smith, Ronald; Wu, Yunhui; Grobler, Jay; Coleman, Paul J.
• Is Part Of: ChemMedChem. Volume 10:Issue 2(2015:Feb.)
• Page Start: 213
• Page End: 213
• Publication Date: 2015-02
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201590000
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The front cover picture shows</bold> raltegravir, a safe and efficacious HIV integrase strand‐transfer inhibitor marketed for the treatment of HIV/AIDS under the name Isentress®, in complex with the prototype foamy virus (PFV) intasome. MK‐8970 is an acetal carbonate prodrug of raltegravir, specifically designed to enhance colonic absorption after oral dosing and maintain inhibition of HIV integrase to enable once‐daily dosing. For further details, see the Full Paper by Abbas M. Walji et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 245 ff.</ext-link> Coordinates for the raltegravir–PFV intasome complex were taken from PDB ID 3OYA (S. Hare, S. S. Gupta, E. Valkov, A. Engelman, P. Cherepanov, <italic>Nature</italic>­ <bold>2010</bold>, <italic>464</italic>, 232–236). The cover art was produced in conjunction with Sharon O'Brien (Merck Creative Services).<boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgh3jkhn4s3" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>