Synthesis and SAR of methyl linked cyclohexyl thiophenyl triazoles for their Anti-Alzheimer activity

The present study, a series of N-[3-(4-Amino-5-mercapto-4H-[1,2,4]triazol-3-ylmethyl)-4,5,6,7- tetrahydro-benzo(b)thiophen-2-yl]-2-substituted amide derivatives (2A-D) were synthesized in good yields and characterized. Evaluation of the 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 (SPA) method. The cdk5/p25 inhibitor data of the tested compounds indicated that 5A, 5I, 7A, 7B, 7E, 7I, 9A and 9E showed better activity out of which 9A and 9E shows equally selective versus cdk2.

Author(s): Rajendra D. Dighe*, Mahendra R. Shiradkara, Sheetal S. Rohomb and Prashant D. Dighec

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