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The Fkbps Structure Neurodegenerative Disease Therapy Pilot Structure-based Discovery And Optimization

Posted on:2002-11-12Degree:DoctorType:Dissertation
Country:ChinaCandidate:L Q ZhaoFull Text:PDF
GTID:1114360155976259Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
32 N-arylsulfonyl α-alkyl L-amino acid esters were synthesized and tested for their neurotrophic activities in vitro. The results showed that compound 3, 5, 10, 12, 13, 14, 15, 20, 21 and 28 exert potent enhancement of the effects of NGF of promoting the survival of PC12 cells; And, compound 12, 13, 15, 20 and 28 display good augmentation on neurite outgrowth in chick dorsal root ganglion (DRG) cultures, of them, compound 12 和 15 exhibit higher activities than GPI-1046.
Keywords/Search Tags:neurodegenerative disease, FKBP12, nerve growth factor, GPI-1046, neurotrophic, dorsal root ganglion, immunophilins, FKBPs, neurodegenerative diseases, molecular docking, structure-based drug design, computer-aided drug design, synthesis
PDF Full Text Request
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