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.
Synthesis of bis-amides and hydrazide-containing derivatives of malonic acid as HIV-1 integrase inhibitors / Sechi, Mario; Azzena, Ugo Gavino; Delussu, Maria Paola; Derudas, Marco; Neamati, Nouri. - (2006). (Intervento presentato al convegno SardiniaChem 2006: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive).
Synthesis of bis-amides and hydrazide-containing derivatives of malonic acid as HIV-1 integrase inhibitors
Sechi, Mario;Azzena, Ugo Gavino;
2006-01-01
Abstract
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.File | Dimensione | Formato | |
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