Design, synthesis and evaluation of novel hydroxyethylamine derivatives with nitrogen heterocyclic moiety at N-terminal as BACE1 inhibitors / 国际药学研究杂志
Journal of International Pharmaceutical Research
; (6): 377-381, 2010.
Article
in Zh
| WPRIM
| ID: wpr-845932
Responsible library:
WPRO
ABSTRACT
Objective: To develop a new series of hydroxy ethylamine (HEA) BACE1 inhibitors with nitrogen heterocyclic moiety at N-terminal and find new N-terminal moiety for enhancing BACE1 inhibition activity. Methods: New HEA compounds with nitrogen heterocyclic moiety at N-terminal were synthesized and evaluated as BACE1 inhibitors,with (-)-epigallocatechin-3-gallate EGCG as a positive control. Results: All new compounds were characterized by 1H NMR and ESI-MS. Evaluation of BACE1 inhibition activity showed that the compound I6 with indole moiety at N-terminal had BACE1 inhibition activity. Conclusion: The results suggested that the indole moiety at N-terminal interact with S2 pocket of BACE1 and be favorable for enhancing BACE1 inhibition activity, Thus, the indole moiety at N-terminal can be used as lead structure for further finding more effient BACE1 inhibitors.
Full text:
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Database:
WPRIM
Language:
Zh
Journal:
Journal of International Pharmaceutical Research
Year:
2010
Document type:
Article