Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integraseiInhibitors
Ferro, Stefania × Grazia, Sara De De Luca, Laura Gitto, Rosaria Faliti, Caterina Elisa Debyser, Zeger Chimirri, Alba #
Molecules vol:16 issue:8 pages:6858-6870
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.