Cover Feature: Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors (ChemMedChem 24/2021)

• Published in: ChemMedChem 2021-12, Vol.16 (24), p.3627-3627
• Main Authors: Platte, Simon, Korff, Marvin, Imberg, Lukas, Balicioglu, Ilker, Erbacher, Catharina, Will, Jonas M., Daniliuc, Constantin G., Karst, Uwe, Kalinin, Dmitrii V.
• Format: Article
• Language: English
• Subjects: aminotriazoles; covalent inhibitors; enzyme inhibitors; FXIIa; microscale synthesis; parallel synthesis; qNMR; thrombin; thrombosis
• ISSN: 1860-7179; 1860-7187
• DOI: 10.1002/cmdc.202100741

The Cover Feature illustrates a microscale parallel synthetic approach leading to novel N‐acylated aminotriazoles having anticoagulant properties. The bottom part of the picture demonstrates the life‐threatening thrombus, whereas the upper part shows the developed covalent inhibitor of the blood coagulation factor XIIa. Inhibitors of this class transfer their acyl moiety to the catalytic Ser195 of an enzyme such as FXIIa or thrombin. This disrupts the enzymes’ catalytic properties causing the anticoagulant effect. Synthesized inhibitors are a promising starting point for the development of novel antithrombotic drugs. Cover design by Jenni Stocksmeier and Marvin Korff. More information can be found in the Full Paper by Dmitrii V. Kalinin et al.