Publication: Triazolyl tryptoline derivatives as β-secretase inhibitors
Issued Date
2010-11-15
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ISSN
0960894X
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2-s2.0-77958063689
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Mahidol University
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SCOPUS
Bibliographic Citation
Bioorganic and Medicinal Chemistry Letters. Vol.20, No.22 (2010), 6572-6576
Suggested Citation
Jutamas Jiaranaikulwanitch, Chantana Boonyarat, Valery V. Fokin, Opa Vajragupta Triazolyl tryptoline derivatives as β-secretase inhibitors. Bioorganic and Medicinal Chemistry Letters. Vol.20, No.22 (2010), 6572-6576. doi:10.1016/j.bmcl.2010.09.043 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/28597
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Title
Triazolyl tryptoline derivatives as β-secretase inhibitors
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Abstract
Tryptoline, 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.