Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors

• Published in: Molecules (Basel, Switzerland) Vol. 16; no. 8; pp. 6858 - 6870
• Main Authors: Ferro, Stefania, Grazia, Sara De, De Luca, Laura, Gitto, Rosaria, Faliti, Caterina Elisa, Debyzer, Zeger, Chimirri, Alba
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 11.08.2011; MDPI
• Subjects: Acquired immune deficiency syndrome; AIDS; Drug resistance; Enzymes; FDA approval; Green Chemistry Technology; HIV; HIV Infections - drug therapy; HIV Infections - enzymology; HIV Infections - virology; HIV Integrase - metabolism; HIV Integrase Inhibitors - chemical synthesis; HIV Integrase Inhibitors - pharmacology; HIV Integrase Inhibitors - therapeutic use; HIV-1 - drug effects; HIV-1 - enzymology; Human immunodeficiency virus; Humans; Immune system; Indoles - chemical synthesis; Indoles - pharmacology; Indoles - therapeutic use; integrase inhibitors; Kinetics; Ligands; Magnetic Resonance Spectroscopy; MAOS; Microwaves; Models, Molecular; Molecular Structure; Pharmaceutical sciences; Pyrrolidinones - chemistry; Pyrrolidinones - pharmacology; Quinolones - chemistry; Quinolones - pharmacology; Raltegravir Potassium; Small Molecule Libraries - chemical synthesis; Small Molecule Libraries - pharmacology; Small Molecule Libraries - therapeutic use; small molecules; Structure-Activity Relationship
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules16086858

Integrase (IN) represents a clinically validated target for the development of antivirals against human immunodeficiency virus (HIV). In recent years our research group has been engaged in the stucture-function study of this enzyme and in the development of some three-dimensional pharmacophore models which have led to the identification of a large series of potent HIV-1 integrase strand-transfer inhibitors (INSTIs) bearing an indole core. To gain a better understanding of the structure-activity relationships (SARs), herein we report the design and microwave-assisted synthesis of a novel series of 1-H-benzylindole derivatives.