Clubbed thiazoles by MAOS: A novel approach to cyclin-dependent kinase 5/p25 inhibitors as a potential treatment for Alzheimer’s disease

A novel clubbed triazolyl thiazole series of cdk5/p25 inhibitors, potentially useful for the treatment of Alzheimer’s disease, is disclosed. Evaluation of the SAR of substitution within these series has allowed the identification of a range of compounds which significantly reduce brain cdk5/p25 and thus have potential as possible treatments for Alzheimer’s disease.

The synthesis of a new series of triazolyl-thiazole derivatives under microwave assisted organic synthesis is described. They were tested as cdk5/p25 inhibitors. It was also observed that 8b possesses 17-fold selectivity for cdk5/cdk2. Compounds 8a and 8c have shown appreciable cdk5/p25 inhibitory potency. Few compounds were good inhibitors while others were inactive.Figure optionsDownload as PowerPoint slide