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• W1966791119 startingPage "7379" @default.
• W1966791119 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." @default.
• W1966791119 created "2016-06-24" @default.
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• W1966791119 date "2012-06-14" @default.
• W1966791119 modified "2023-09-22" @default.
• W1966791119 title "Substituted Benzamides Containing Azaspiro Rings as Upregulators of Apolipoprotein A-I Transcription" @default.
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• W1966791119 doi "https://doi.org/10.3390/molecules17067379" @default.
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