Pardin Christophe, Roy Isabelle, Lubell William D, Keillor Jeffrey W
Département de chimie, Université de Montréal, C.P. 6128, Succursale centre-ville, Montréal, QC H3C 3J7, Canada.
Chem Biol Drug Des. 2008 Sep;72(3):189-96. doi: 10.1111/j.1747-0285.2008.00696.x. Epub 2008 Aug 19.
A series of 15 cinnamoyl triazole derivatives was prepared by Cu(I)-catalyzed azide/alkyne [3+2]-cycloaddition reactions and examined as inhibitors of guinea-pig liver transglutaminase. Several compounds exhibited activity as reversible inhibitors that were competitive with acyl donor transglutaminase substrates. For example, triazole 4d has a K(i) value of 174 nM and represents one of the most potent reversible transglutaminase inhibitors reported to date.
通过铜（I）催化的叠氮化物/炔烃[3 + 2]环加成反应制备了一系列15种肉桂酰基三唑衍生物，并将其作为豚鼠肝脏转谷氨酰胺酶的抑制剂进行了研究。几种化合物表现出作为可逆抑制剂的活性，它们与酰基供体转谷氨酰胺酶底物具有竞争性。例如，三唑4d的K（i）值为174 nM，是迄今为止报道的最有效的可逆转谷氨酰胺酶抑制剂之一。
