Cathepsins 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 K_i value of the order of 10⁻¹⁰ M. 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.

组织蛋白酶已成为许多疾病如Alzeimer病，炎症和癌症的有希望的分子靶标。组织蛋白酶水平的升高和细胞抑制剂浓度的降低，都强调了对组织蛋白酶新型抑制剂的研究。目前的工作集中于设计和合成一些基于乙酰苯苯基hydr的吡唑衍生物，作为组织蛋白酶B，H和L的新型非肽基抑制剂。对合成后的化合物进行了表征，探讨了它们对组织蛋白酶B，H和L的抑制作用。结果表明，某些合成的化合物表现出抗结节病活性，K _i值为10 ^{-10数量级。} M.已观察到对组织蛋白酶B，H和L的差异抑制作用。与组织蛋白酶B和组织蛋白酶H相比，组织蛋白酶L的抑制作用更为明显。