2. Academic Validation
  3. Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites

  • J Med Chem. 2006 Jun 1;49(11):3421-5. doi: 10.1021/jm060257t.
Sandra Gemma 1,  Emanuele Gabellieri,  Paul Huleatt,  Caterina Fattorusso,  Marianna Borriello,  Bruno Catalanotti,  Stefania Butini,  Meri De Angelis,  Ettore Novellino,  Vito Nacci,  Tatyana Belinskaya,  Ashima Saxena,  Giuseppe Campiani
Affiliations

Affiliation

  • 1 Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, Universita' di Siena, 53100 Siena, Italy.
PMID: 16722663 DOI: 10.1021/jm060257t
Abstract

We describe herein the development of novel huperzine A-tacrine hybrids characterized by 3-methylbicyclo[3.3.1]non-3-ene scaffolds. These compounds were specifically designed to establish tight interactions, through different binding modes, with the midgorge recognition sites of human acetylcholinesterase (hAChE: Y72, D74) and human butyrylcholinesterase (hBuChE: N68, D70) and their catalytic or peripheral sites. Compounds 5a-c show a markedly improved biological profile relative to tacrine and huperzine A.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z