含不同肽基团的三嗪氮芥类化合物作为新型 AChE 和 BACE1 抑制剂候选物。
1,3,5-Triazine Nitrogen Mustards with Different Peptide Group as Innovative Candidates for AChE and BACE1 Inhibitors.
机构信息
Department of Organic Chemistry, Medical University, Mickiewicza Street 2a, 15-222 Białystok, Poland.
Institute of Organic Chemistry, Faculty of Chemistry, Lodz University of Technology, Zeromskiego 116, 90-924 Lodz, Poland.
出版信息
Molecules. 2021 Jun 28;26(13):3942. doi: 10.3390/molecules26133942.
A series of new analogs of nitrogen mustards (-) containing the 1,3,5-triazine ring substituted with dipeptide residue were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and -secretase (BACE1) enzymes. The AChE inhibitory activity studies were carried out using Ellman's colorimetric method, and the BACE1 inhibitory activity studies were carried out using fluorescence resonance energy transfer (FRET). All compounds displayed considerable AChE and BACE1 inhibition. The most active against both AChE and BACE1 enzymes were compounds and , with an inhibitory concentration of AChE IC = 0.051 µM; 0.055 µM and BACE1 IC = 9.00 µM; 11.09 µM, respectively.
一系列含有取代二肽残基的 1,3,5-三嗪环的新型氮芥类似物（-）被合成并评估了对乙酰胆碱酯酶（AChE）和β-分泌酶（BACE1）的抑制作用。AChE 抑制活性研究采用 Ellman 比色法进行，BACE1 抑制活性研究采用荧光共振能量转移（FRET）法进行。所有化合物均表现出相当的 AChE 和 BACE1 抑制活性。对 AChE 和 BACE1 酶均具有最强活性的化合物为 和 ，对 AChE 的抑制浓度 IC = 0.051 µM；0.055 µM，对 BACE1 的抑制浓度 IC = 9.00 µM；11.09 µM。
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