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
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- 作者：Serena Pasquini ; Claudia Mugnaini ; Cristina Tintori ; Maurizio Botta ; Alejandro Trejos ; Riina K. Arvela ; Mats Larhed ; Myriam Witvrouw ; Martine Michiels ; Frauke Christ ; Zeger Debyser ; Federico Corelli
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：August 28, 2008
- 年：2008
- 卷：51
- 期：16
- 页码：5125-5129
- 全文大小：192K
- 年卷期：v.51,no.16(August 28, 2008)
- ISSN：1520-4804
文摘
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.