Martinez_2000_Eur.J.Med.Chem_35_913

Reference

Title : N-Benzylpiperidine derivatives of 1,2,4-thiadiazolidinone as new acetylcholinesterase inhibitors - Martinez_2000_Eur.J.Med.Chem_35_913
Author(s) : Martinez A , Fernandez E , Castro A , Conde S , Rodriguez-Franco I , Banos JE , Badia A
Ref : Eur Journal of Medicinal Chemistry , 35 :913 , 2000
Abstract :

A new family of 1,2,4-thiadiazolidinone derivatives containing the N-benzylpiperidine fragment has been synthesised. The acetylcholinesterase (AChE) inhibitory activity of all compounds was measured using Ellman's method and some of them turned out to be as potent as tacrine. Furthermore, compound 13 was as active as tacrine in reversing the blockade induced by tubocurarine at rat neuromuscular junction. Additionally, receptor binding studies provided new lead compounds for further development of alpha2-adrenergic and sigma-receptor antagonists. Molecular dynamic simulation using X-ray crystal structure of AChE from Torpedo californica was used to explain the possible binding mode of these new compounds.

PubMedSearch : Martinez_2000_Eur.J.Med.Chem_35_913
PubMedID: 11121617

Related information

Citations formats

Martinez A, Fernandez E, Castro A, Conde S, Rodriguez-Franco I, Banos JE, Badia A (2000)
N-Benzylpiperidine derivatives of 1,2,4-thiadiazolidinone as new acetylcholinesterase inhibitors
Eur Journal of Medicinal Chemistry 35 :913

Martinez A, Fernandez E, Castro A, Conde S, Rodriguez-Franco I, Banos JE, Badia A (2000)
Eur Journal of Medicinal Chemistry 35 :913