Thu, 23 Nov 2017

A CYCLIN DEPENDENT KINASE-5 INHIBITORS: SYNTHESIS AND SAR OF CLUBBED TRIAZOLE.

Rajendra Dnyandeo Dighe*, Mahendra Ramesh Shiradkar

 

1. Dr. Reddy’s Laboratories, Bachupally, Hyderabad-502 325, Andhra Pradesh, India


ABSTRACT

 

The present study, a series of clubbed triazole generated by microwave organic reaction enhancement (MORE) method and examine for their cyclin dependent kinase-5 (cdk5) inhibitors, potentially useful for treatment of Alzheimer disease. Evaluation of the structure active relationship (SAR) of substitution with-in these series has allowed the identification of a range of compounds which significantly reduce brain cdk5/p25 by scintillation proximate assay method. The cdk5/p25 inhibitor data of the tested compounds indicated that 3E, 4E, 6E, 8E and 8I showed better activity out of which 8E and 8I shows equally selective versus cdk2.

Key words: Cyclohexyl thiophene, triazole, cdk5/p25, Alzheimer's disease, MORE.


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