Triazolyl tryptoline derivatives as ?-secretase inhibitors.
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ABSTRACT:
SUBMITTER: Jiaranaikulwanitch J
PROVIDER: S-EPMC3055559 | biostudies-literature | 2010 Nov
REPOSITORIES: biostudies-literature
Publications
Triazolyl tryptoline derivatives as β-secretase inhibitors.
Jiaranaikulwanitch Jutamas J Boonyarat Chantana C Fokin Valery V VV Vajragupta Opa O
Bioorganic & medicinal chemistry letters 20100922 22
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 ( ...[more]
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