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Bioorg Med Chem ; 15(19): 6397-406, 2007 Oct 01.
Article in English | MEDLINE | ID: mdl-17643991

ABSTRACT

Based on the earlier results of our in-house database and compound library, a series of novel clubbed thienyl triazoles was designed which may emerge as potential cdk5/p25 inhibitors, for the treatment of Alzheimer's disease. A benign synthesis was planned so as to take an advantage of MAOS (Microwave Assisted Organic Synthesis) method. Evaluation of the SAR of this series has allowed the identification of compounds 4, 5, 7 and 8 from series I while 13, 14, 16 and 17 from series II as significant cdk5/p25 inhibitors and thus have potential as possible treatments for Alzheimer's disease.


Subject(s)
Brain/drug effects , Cyclin-Dependent Kinase 5/antagonists & inhibitors , Enzyme Inhibitors/pharmacology , Nerve Tissue Proteins/antagonists & inhibitors , Thiazoles/pharmacology , Ticrynafen/chemistry , Alzheimer Disease/drug therapy , Alzheimer Disease/pathology , Brain/metabolism , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/therapeutic use , Humans , Microwaves , Structure-Activity Relationship , Thiazoles/chemical synthesis
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