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Synthesis and acetylcholinesterase inhibitory activity of Mannich base derivatives flavokawain B.
Liu, Hao-Ran; Huang, Xue-Qin; Lou, Ding-Hui; Liu, Xian-Jun; Liu, Wu-Kun; Wang, Qiu-An.
Afiliación
  • Liu HR; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • Huang XQ; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • Lou DH; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • Liu XJ; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • Liu WK; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China.
  • Wang QA; College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China. Electronic address: wangqa@hnu.edu.cn.
Bioorg Med Chem Lett ; 24(19): 4749-4753, 2014 Oct 01.
Article en En | MEDLINE | ID: mdl-25205193
A novel series of flavokawain B derivatives, chalcone Mannich bases (4-10) were designed, synthesized, characterized, and evaluated for the inhibition activity against acetylcholinesterase (AChE). Biological results revealed that four compounds displayed potent activities against AChE with IC50 values below 20µM. Moreover, the most promising compound 8 was 2-fold more active than rivastigmine, a well-known AChE inhibitor. The logP values of 4-10 were around 2 which indicated that they were sufficiently lipophilic to pass blood brain barriers in vivo. Enzyme kinetic study suggested that the inhibition mechanism of compound 8 was a mixed-type inhibition. Meanwhile, the molecular docking showed that this compound can both bind with the catalytic site and the periphery of AChE.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Flavonoides / Inhibidores de la Colinesterasa Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Flavonoides / Inhibidores de la Colinesterasa Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: China Pais de publicación: Reino Unido