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.

Pasquini, S., Mugnaini, C., Tintori, C., Botta, M., A., T., R. K., A., et al. (2008). 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. JOURNAL OF MEDICINAL CHEMISTRY, 51, 5125-5129.

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.

PASQUINI, SERENA;MUGNAINI, CLAUDIA;TINTORI, CRISTINA;BOTTA, MAURIZIO;CORELLI, FEDERICO
2008

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/24484
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