Jutamas JiaranaikulwanitchChantana BoonyaratValery V. FokinOpa VajraguptaMahidol UniversityKhon Kaen UniversityScripps Research Institute2018-09-242018-09-242010-11-15Bioorganic and Medicinal Chemistry Letters. Vol.20, No.22 (2010), 6572-65760960894X2-s2.0-77958063689https://repository.li.mahidol.ac.th/handle/123456789/28597Tryptoline, a core structure of ochrolifuanine E, which is a hit compound from virtual screening of the Thai herbal database against BACE1 was used as a scaffold for the design of BACE1 inhibitors. The tryptoline was linked with different side chains by 1,2,3-triazole ring readily synthesized by catalytic azide-alkyne cycloaddition reactions. Twenty two triazolyl tryptoline derivatives were synthesized and screened for the inhibitory action against BACE1. JJCA-140 was the most potent inhibitor (IC50= 1.49 μM) and was 100 times more selective for BACE1 than for Cat-D. © 2010 Elsevier Ltd. All rights reserved.Mahidol UniversityBiochemistry, Genetics and Molecular BiologyChemistryPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.bmcl.2010.09.043