Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa

Bioorganic & Medicinal Chemistry Letters
2010.0

Abstract

The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.

Knowledge Graph

Similar Paper

Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa
Bioorganic & Medicinal Chemistry Letters 2010.0
Clavatadine A, A Natural Product with Selective Recognition and Irreversible Inhibition of Factor XIa
Journal of Medicinal Chemistry 2008.0
Engineering the Cyclization Loop of MCoTI-II Generates Targeted Cyclotides that Potently Inhibit Factor XIIa
Journal of Medicinal Chemistry 2022.0
Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors
Journal of Medicinal Chemistry 1994.0
Factor XIIIa inhibitors as potential novel drugs for venous thromboembolism
European Journal of Medicinal Chemistry 2020.0
PRO_SELECT:  Combining Structure-Based Drug Design and Array-Based Chemistry for Rapid Lead Discovery. 2. The Development of a Series of Highly Potent and Selective Factor Xa Inhibitors
Journal of Medicinal Chemistry 2002.0
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors
ACS Medicinal Chemistry Letters 2016.0
Dysinosins B−D, Inhibitors of Factor VIIa and Thrombin from the Australian Sponge<i>Lamellodysidea</i><i>c</i><i>hlorea</i>
Journal of Natural Products 2004.0
Dysinosins B−D, Inhibitors of Factor VIIa and Thrombin from the Australian Sponge<i>Lamellodysidea</i><i>c</i><i>hlorea</i>
Journal of Natural Products 2004.0
From natural products to achiral drug prototypes: Potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs
Bioorganic &amp; Medicinal Chemistry Letters 2009.0