The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of Isentress™, represents a validated target for anti-retroviral therapy. Incorporation of the dihydroxycarbonyl pharmacophore into a pyrrolinone scaffold led to the discovery of 5-pyrrolinone-3-carboxamides as a structurally diverse class of HIV-1 integrase inhibitors. © 2008 Elsevier Ltd. All rights reserved.
4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors / Pace, ; Paola, ; Spieser, ; Stephane, A. H.; Summa, V. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 18:14(2008), pp. 3865-3869. [10.1016/j.bmcl.2008.06.056]
4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors
Summa V
2008
Abstract
The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of Isentress™, represents a validated target for anti-retroviral therapy. Incorporation of the dihydroxycarbonyl pharmacophore into a pyrrolinone scaffold led to the discovery of 5-pyrrolinone-3-carboxamides as a structurally diverse class of HIV-1 integrase inhibitors. © 2008 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
