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

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

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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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