Franciskovich Jeffry B, Masters John J, Weber Wayne W, Klimkowski Valentine J, Chouinard Michael, Sipes Philip R, Johnson Lea M, Snyder David W, Chastain Marcia K, Craft Trelia J, Towner Richard D, Gifford-Moore Donetta S, Froelich Larry L, Smallwood Jeffrey K, Foster Ronald S, Smith Gerald F, Liebeschuetz John W, Murray Christopher W, Young Stephen C
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Bioorg Med Chem Lett. 2007 Dec 15;17(24):6910-3. doi: 10.1016/j.bmcl.2007.09.105. Epub 2007 Oct 24.
Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats.
合成了基于d-苯甘氨酰胺的通用支架（2）的几种P4结构域衍生物，并评估了它们与丝氨酸蛋白酶因子Xa结合的能力。对一些活性更强的化合物进行了体外抗凝作用评估。对一个包含各种P1吲哚构建体的选定子集进行了口服给药大鼠后的药代动力学性质进一步评估。
