Raghav Neera, Singh Mamta
Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
Bioorg Chem. 2017 Dec;75:38-49. doi: 10.1016/j.bioorg.2017.08.006. Epub 2017 Aug 31.
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 value of the order of 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.
组织蛋白酶已成为包括阿尔茨海默病、炎症和癌症等多种疾病中颇具前景的分子靶点。组织蛋白酶水平升高和细胞内抑制剂浓度降低凸显了对新型组织蛋白酶抑制剂的研究需求。目前的工作聚焦于设计和合成一些基于苯乙酮苯腙的吡唑衍生物，作为组织蛋白酶B、H和L的新型非肽类抑制剂。合成的化合物经表征后，对其抑制组织蛋白酶B、H和L的效力进行了研究。结果表明，一些合成化合物表现出抗组织蛋白酶活性，其K值约为10M。观察到组织蛋白酶B、H和L存在不同的抑制作用。组织蛋白酶L受到的抑制比组织蛋白酶B和组织蛋白酶H更为明显，顺序依次如此。
