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

Identifieur interne : 001481 ( PubMed/Curation ); précédent : 001480; suivant : 001482

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

Auteurs : Stefania Ferro [Italie] ; Sara De Grazia ; Laura De Luca ; Rosaria Gitto ; Caterina Elisa Faliti ; Zeger Debyzer ; Alba Chimirri

Source :

RBID : pubmed:21836543

Descripteurs français

English descriptors

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.

DOI: 10.3390/molecules16086858
PubMed: 21836543

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pubmed:21836543

Le document en format XML

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<div type="abstract" xml:lang="en">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.</div>
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