Medical Pharmacology and Toxicology, Department of Medical Biology, Faculty of Health Science, University of Tromsø, N-9037 Tromsø, Norway.
Bioorg Med Chem. 2010 Jun 15;18(12):4317-27. doi: 10.1016/j.bmc.2010.04.083. Epub 2010 Apr 29.
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 IC(50) values ranging from 0.0115 microM (compound 3) to 122,637 microM (compound 29). Compound 3 [3-phenyl-2-(trifluoromethyl) quinazolin-4(3H)-one] (IC(50)=0.0115 microM) and compound 35 [3-(isopropylideneamino)-2,2-dimethyl-2,3-dihydroquinazolin-4 (1H)-one] (IC(50)=0.2477 microM) were found to be the most potent inhibitors.
合成了一系列新型的喹唑啉-4(3H)-酮，并基于光谱数据（IR、NMR、EI-MS 和 FAB-MS）确定了它们的结构。利用基于化学阵列的方法测试了这些化合物对锌金属蛋白酶胰凝乳蛋白酶（TLN）的抑制作用。发现一些化合物具有抑制 TLN 的作用，IC50 值范围从 0.0115 μM（化合物 3）到 122,637 μM（化合物 29）。化合物 3 [3-苯基-2-(三氟甲基)喹唑啉-4(3H)-酮]（IC50=0.0115 μM）和化合物 35 [3-（异亚丙基氨基）-2,2-二甲基-2,3-二氢喹唑啉-4(1H)-酮]（IC50=0.2477 μM）是最有效的抑制剂。
