Die Pharmazie is published by IMR Press from Volume 81 Issue 1 (2026). Previous articles were published by another publisher under the CC-BY licence, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement.
Synthesis of 1,3,4-thiadiazole derivatives as aminopeptidase N inhibitors
Shao-Hua Li 1, Shao-Hua Li 2, Gang Li 2, Hui-Ming Huang 2, Fang Xiong 3, Xi Mai 2, Bin-Hai Kuang 2, Cheng-Mei Liu 4, Guo-Gang Tu 5
Affiliations
Article Info
1 State Key Laboratory of Food Science and Technology, Nanchang University, NanChang, P.R. China
2 Department of Pharmacy, NanChang University Medical College, NanChang, P.R. China
3 Department of Cardiology, the Second Affiliated Hospital of Nanchang University, NanChang, P.R. China
4 State Key Laboratory of Food Science and Technology, Nanchang University, NanChang, 330047, P.R. China
5 Department of Pharmacy, NanChang University Medical College, NanChang, 330006, P.R. China, Email: tugg199@yahoo.com
Abstract
Aminopeptidase N (APN) is a zinc-dependent ectopeptidase which plays an important role in the invasion of metastatic tumors. In this study, we report the synthesis and in vitro enzyme inhibition assay of 1,3,4-thiadiazole scaffold compounds. These new compounds have potent inhibitory activities toward APN with IC50 values in the micromolar range.