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Molecules 2012, 17(6), 7379-7386; doi:10.3390/molecules17067379

Substituted Benzamides Containing Azaspiro Rings as Upregulators of Apolipoprotein A-I Transcription

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Tian Tan Xi Li 1#, Beijing 100050, China
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Received: 30 March 2012 / Revised: 8 June 2012 / Accepted: 11 June 2012 / Published: 14 June 2012
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Abstract

Apolipoprotein A-I (Apo A-I) is the principal protein component of high density lipoprotein (HDL), which is generally considered as a potential therapeutic target against atherosclerosis. The understanding of the Apo A-I regulation mechanism has fuelled the development of novel HDL targeted therapeutic approaches. To identify novel agents that can upregulate Apo A-I expression, we performed a cell-based reporter assay to screen 25,600 small molecules. Based on the dataset obtained from screening, a series of novel analogs of substituted benzamides containing azaspiro rings were assessed for their ability to induce the transcription of the Apo A-I gene, and the structure-activity relationship (SAR) around these analogs was also proposed. The results indicated that the trifluoromethyl substituted benzamide containing an azaspiro ring is a promising backbone for designing Apo A-I transcriptional upregulator and could be viable leads for development of new drugs to prevent and treat atherosclerosis in the future.
Keywords: apolipoprotein A-I; transcriptional upregulator; structure-activity relationship; atherosclerosis apolipoprotein A-I; transcriptional upregulator; structure-activity relationship; atherosclerosis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Du, Y.; Yang, Y.; Jiang, W.; Wang, L.; Jia, X.-J.; Si, S.-Y.; Chen, X.-F.; Hong, B. Substituted Benzamides Containing Azaspiro Rings as Upregulators of Apolipoprotein A-I Transcription. Molecules 2012, 17, 7379-7386.

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