Title: Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors
Authors: Pasquini, Serena
Mugnaini, Claudia
Tintori, Cristina
Botta, Maurizio
Trejos, Alejandro
Arvela, Riina K
Larhed, Mats
Witvrouw, Myriam
Michiels, Martine
Christ, Frauke
Debyser, Zeger
Corelli, Federico # ×
Issue Date: Aug-2008
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:51 issue:16 pages:5125-5129
Abstract: A set of 4-quinolone-3-carboxylic acids bearing different substituents on the condensed benzene ring was designed and synthesized as potential HIV-1 integrase inhibitors structurally related to elvitegravir. Some of the new compounds proved to be able to inhibit the strand transfer step of the virus integration process in the micromolar range. Docking studies and quantum mechanics calculations were used to rationalize these data.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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