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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

1,* , 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.
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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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