Delussu, Maria Paola and Sechi, Mario and Azzena, Ugo Gavino and Derudas, Marco and Neamati, Nouri (2006) Synthesis of bis-amides and hydrazide-containing derivatives of malonic acid as HIV-1 integrase inhibitors. In: SardiniaChem 2006: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive, 5 Giugno 2006, Cagliari, Italia. Conference or Workshop Item.
With the aim to identify novel and/or unified putative pharmacophore required for activity we selected and formally combinated the main structural motifs of I and II together to the hydrazide fragment of compounds III and IV, previously reported as new class of selective IN inhibitors having antiviral activity. Also, the possibility to generate a potential metal chelating pharmacophore has been considered. With this in mind, we designed two sets of symmetrical and unsymmetrical bis-amides and hydrazide derivatives of malonic acid.
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