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Article

Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors

by
Stefania Ferro
1,*,
Sara De Grazia
1,
Laura De Luca
1,
Rosaria Gitto
1,
Caterina Elisa Faliti
1,
Zeger Debyzer
2 and
Alba Chimirri
1
1
Department of Medicinal Chemistry, University of Messina, Viale Annunziata, I-98168 Messina, Italy
2
Molecular Medicine, Katholieke Universiteit Leuven and IRC KULAK, Kapucijnenvoer 33, B-3000 Leuven, Flanders, Belgium
*
Author to whom correspondence should be addressed.
Molecules 2011, 16(8), 6858-6870; https://doi.org/10.3390/molecules16086858
Submission received: 18 July 2011 / Revised: 4 August 2011 / Accepted: 8 August 2011 / Published: 11 August 2011
(This article belongs to the Special Issue Microwave Assisted Synthesis)
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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 AIDS; integrase inhibitors; small molecules; MAOS

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MDPI and ACS Style

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. https://doi.org/10.3390/molecules16086858

AMA Style

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. https://doi.org/10.3390/molecules16086858

Chicago/Turabian Style

Ferro, Stefania, Sara De Grazia, Laura De Luca, Rosaria Gitto, Caterina Elisa Faliti, Zeger Debyzer, and Alba Chimirri. 2011. "Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors" Molecules 16, no. 8: 6858-6870. https://doi.org/10.3390/molecules16086858

APA Style

Ferro, S., Grazia, S. D., Luca, L. D., Gitto, R., Faliti, C. E., Debyzer, Z., & Chimirri, A. (2011). Microwave Assisted Organic Synthesis (MAOS) of Small Molecules as Potential HIV-1 Integrase Inhibitors. Molecules, 16(8), 6858-6870. https://doi.org/10.3390/molecules16086858

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