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Molecules 2011, 16(8), 6858-6870; doi:10.3390/molecules16086858

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 / 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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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
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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.

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