Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors

HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site

Synthesis of bis-amides and hydrazide-containing derivatives of malonic acid as HIV-1 integrase inhibitors

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

Design and synthesis of novel DNA binders

In this context, molecular recognition of DNA by polycyclic heterocycles having a planar structure bearing appropriate side chains have been widely investigated. In the course of our work aimed at developing novel heterocycles of pharmaceutical interest, we designed and synthetized several templates as potential substrate in drug design

Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors

HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site