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

Identifieur interne : 002080 ( Main/Curation ); précédent : 002079; suivant : 002081

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

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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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Le document en format XML

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<name sortKey="Gitto, Rosaria" sort="Gitto, Rosaria" uniqKey="Gitto R" first="Rosaria" last="Gitto">Rosaria Gitto</name>
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<term>HIV Infections (virology)</term>
<term>HIV Integrase (metabolism)</term>
<term>HIV Integrase Inhibitors (chemical synthesis)</term>
<term>HIV Integrase Inhibitors (pharmacology)</term>
<term>HIV Integrase Inhibitors (therapeutic use)</term>
<term>HIV-1 (drug effects)</term>
<term>HIV-1 (enzymology)</term>
<term>Humans</term>
<term>Indoles (chemical synthesis)</term>
<term>Indoles (pharmacology)</term>
<term>Indoles (therapeutic use)</term>
<term>Kinetics</term>
<term>Magnetic Resonance Spectroscopy</term>
<term>Microwaves</term>
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<term>Pyrrolidinones (chemistry)</term>
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<term>Quinolones (chemistry)</term>
<term>Quinolones (pharmacology)</term>
<term>Raltegravir Potassium</term>
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<term>Indoles (pharmacologie)</term>
<term>Indoles (synthèse chimique)</term>
<term>Indoles (usage thérapeutique)</term>
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<term>Infections à VIH (traitement médicamenteux)</term>
<term>Infections à VIH (virologie)</term>
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<front>
<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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