Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors |
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Authors: | Ferro Stefania Grazia Sara De De Luca Laura Gitto Rosaria Faliti Caterina Elisa Debyzer Zeger Chimirri Alba |
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Institution: | Department of Medicinal Chemistry, University of Messina, Viale Annunziata, I-98168 Messina, Italy. sferro@unime.it |
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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. |
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