کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1370232 | 981814 | 2011 | 5 صفحه PDF | دانلود رایگان |

β-Secretase (BACE1) is widely recognized as a prime drug target for the treatment of Alzheimer’s disease (AD). In this Letter, we report the synthesis and the BACE1 inhibitory activity of novel, variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylcarboxamides. The best results have been obtained with the introduction of a 4-OMe substituent (IC50 = 3.8 μM) or a 3,4-dichloro substituent (IC50 = 2.5 μM) in the amidic aromatic ring. The blood–brain barrier penetration predictions resulted to be promising for this type of compounds. To better understand the structure–activity relationships (SAR) of the new derivatives, a docking study procedure has been applied exploiting different conformational and ionic states of BACE1.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 22, 15 November 2011, Pages 6657–6661