Identification of novel quinazolin-4 (3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases

…, R Khan, Y Wuxiuer, M Arfan, M Ahmed, I Sylte

文献索引：Khan, Mahmud Tareq Hassan; Khan, Rasool; Wuxiuer, Yimingjiang; Arfan, Mohammad; Ahmed, Manzoor; Sylte, Ingebrigt Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 12 p. 4317 - 4327

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被引用次数: 27

摘要

A combinatorial series of novel quinazolin-4 (3H)-ones were synthesised and their structures were established based on spectroscopic data (IR, NMR, EI-MS, and FAB-MS). The compounds were tested for inhibition of the zinc metalloproteinase thermolysin (TLN) utilizing a chemical array-based approach. Some of the compounds were found to inhibit TLN, with IC50 values ranging from 0.0115 μM (compound 3) to 122,637 μM (compound ...