title: Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, University of Messina, Viale Annunziata, I-98168 Messina, Italy. sferro@unime.it
authors.forename: Stefania
authors.initials: S
authors.lastname: Ferro
authors.forename: Sara De
authors.initials: SD
authors.lastname: Grazia
authors.forename: Laura
authors.initials: L
authors.lastname: De Luca
authors.forename: Rosaria
authors.initials: R
authors.lastname: Gitto
authors.forename: Caterina Elisa
authors.initials: CE
authors.lastname: Faliti
authors.forename: Zeger
authors.initials: Z
authors.lastname: Debyzer
authors.forename: Alba
authors.initials: A
authors.lastname: Chimirri
mesh_terms: D055772:Green Chemistry Technology; D015658:HIV Infections / Q000188:drug therapy* / Q000201:enzymology / Q000821:virology; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008872:Microwaves; D008958:Models, Molecular; D015394:Molecular Structure; D011760:Pyrrolidinones / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology; D000068898:Raltegravir Potassium; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
chemical_list: D019428:HIV Integrase Inhibitors; D007211:Indoles; D011760:Pyrrolidinones; D015363:Quinolones; D054852:Small Molecule Libraries; D000068898:Raltegravir Potassium; C509700:elvitegravir; D019427:HIV Integrase