Garrett G S, McPhail S J, Tornheim K, Correa P E, McIver J M
Corporate Research Division, Miami Valley Laboratories, The Procter & Gamble Company, Cincinnati, OH 45253-8707, USA.
Bioorg Med Chem Lett. 1999 Feb 8;9(3):301-6. doi: 10.1016/s0960-894x(98)00562-9.
The synthesis and in vitro enzyme inhibition profile of a series of novel trifluoromethylketone (TFMK) inhibitors of human plasma kallikrein (PK) are described. We have developed an efficient method for the construction of peptide TFMKs that provides the final product devoid of compromised stereochemical integrity. Many of these compounds are potent inhibitors of PK and exhibit reduced inhibition of tissue kallikrein (TK) and plasmin (HP).
描述了一系列人血浆激肽释放酶（PK）新型三氟甲基酮（TFMK）抑制剂的合成及其体外酶抑制谱。我们开发了一种构建肽TFMK的有效方法，该方法提供的最终产物没有受损的立体化学完整性。这些化合物中的许多都是PK的有效抑制剂，并且对组织激肽释放酶（TK）和纤溶酶（HP）的抑制作用降低。
