• Bioorganic chemistry · Dec 2017

    SAR studies of some acetophenone phenylhydrazone based pyrazole derivatives as anticathepsin agents.

    • Neera Raghav and Mamta Singh.
    • Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India. Electronic address: nraghav.chem@gmail.com.
    • Bioorg. Chem. 2017 Dec 1; 75: 38-49.

    AbstractCathepsins have emerged as promising molecular targets in a number of diseases such as Alzeimer's, inflammation and cancer. Elevated cathepsin's levels and decreased cellular inhibitor concentrations have emphasized the search for novel inhibitors of cathepsins. The present work is focused on the design and synthesis of some acetophenone phenylhydrazone based pyrazole derivatives as novel non peptidyl inhibitors of cathepsins B, H and L. The synthesized compounds after characterization have been explored for their inhibitory potency against cathepsins B, H and L. The results show that some of the synthesized compounds exhibit anti-catheptic activity with Ki value of the order of 10-10M. Differential inhibitory effects have been observed for cathepsins B, H and L. Cathepsin L is inhibited more pronounced than cathepsin B and cathepsin H in that order.Copyright © 2017 Elsevier Inc. All rights reserved.

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