Pass M, Bolton R E, Coote S J, Finch H, Hindley S, Lowdon A, McDonald E, McLaren J, Owen M, Pegg N A, Mooney C J, Tang C M, Parry S, Patel C
Glaxo Wellcome Research and Development, Stevenage, Herts, United Kingdom.
Bioorg Med Chem Lett. 1999 Feb 8;9(3):431-6. doi: 10.1016/s0960-894x(99)00002-5.
Synthesis of trans-fused lactones containing the indane nucleus has resulted in a series of potent acylating inhibitors of thrombin. As an example compound 11e has an apparent second order rate constant of 11 x 10(6) M(-1)sec(-1) for the inhibition of thrombin. The anticoagulant activity of these compounds is discussed.
含茚满核的反式稠合内酯的合成已产生了一系列有效的凝血酶酰化抑制剂。例如，化合物11e对凝血酶抑制的表观二级速率常数为11×10⁶ M⁻¹秒⁻¹。讨论了这些化合物的抗凝血活性。
