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Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors
Department of Medicinal Chemistry, University of Messina, Viale Annunziata, I-98168 Messina, Italy
Molecular Medicine, Katholieke Universiteit Leuven and IRC KULAK, Kapucijnenvoer 33, B-3000 Leuven, Flanders, Belgium
* Author to whom correspondence should be addressed.
Received: 18 July 2011; in revised form: 4 August 2011 / Accepted: 8 August 2011 / Published: 11 August 2011
Abstract: 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.
Keywords: AIDS; integrase inhibitors; small molecules; MAOS
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Ferro, S.; Grazia, S.D.; Luca, L.D.; Gitto, R.; Faliti, C.E.; Debyzer, Z.; Chimirri, A. Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors. Molecules 2011, 16, 6858-6870.
Ferro S, Grazia SD, Luca LD, Gitto R, Faliti CE, Debyzer Z, Chimirri A. Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors. Molecules. 2011; 16(8):6858-6870.
Ferro, Stefania; Grazia, Sara De; Luca, Laura De; Gitto, Rosaria; Faliti, Caterina Elisa; Debyzer, Zeger; Chimirri, Alba. 2011. "Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors." Molecules 16, no. 8: 6858-6870.