[HTML][HTML] From ancient leech to direct thrombin inhibitors and beyond: New from old

MR Montinari, S Minelli - Biomedicine & pharmacotherapy, 2022 - Elsevier
Medicinal leeches have been used in health care since before written history, with widely
varying popularity over the centuries. Nowadays, medicinal leech therapy is mainly used in …

Factor XII (a) inhibitors: a review of the patent literature

DV Kalinin - Expert Opinion on Therapeutic Patents, 2021 - Taylor & Francis
Introduction: Blood coagulation factor XII (FXII) is an emerging and potentially safe drug
target, which dysregulation is associated with thrombosis, hereditary angioedema, and …

Microscale parallel synthesis of acylated aminotriazoles enabling the development of factor XIIa and thrombin inhibitors

S Platte, M Korff, L Imberg, I Balicioglu… - …, 2021 - Wiley Online Library
Herein we report a microscale parallel synthetic approach allowing for rapid access to
libraries of N‐acylated aminotriazoles and screening of their inhibitory activity against factor …

Amide-functionalized 1, 2, 4-Triazol-5-amines as covalent inhibitors of blood coagulation factor XIIa and thrombin

L Imberg, S Platte, C Erbacher… - ACS Pharmacology & …, 2022 - ACS Publications
To counteract thrombosis, new safe and efficient antithrombotics are required. We herein
report the design, synthesis, and biological activity of a series of amide-functionalized …

Pyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties

L Imberg, AI Siutkina, C Erbacher… - ACS Pharmacology & …, 2024 - ACS Publications
This study presents a novel series of N-acylated 1, 2, 4-triazol-5-amines and 1 H-pyrazol-5-
amines, featuring a pyrazin-2-yl moiety, developed as covalent inhibitors of thrombin. These …

Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors

KM Short, MA Estiarte, SM Pham, DC Williams… - European Journal of …, 2023 - Elsevier
Direct oral anticoagulants (DOACs), which includes thrombin and factor Xa inhibitors, have
emerged as the preferred therapeutics for thrombotic disorders, penetrating a market …

Drugs in phase I and II clinical development for the prevention of stroke in patients with atrial fibrillation

R Bentley, LJ Hardy, LJ Scott, P Sharma… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction Atrial fibrillation is the most frequently diagnosed cardiac arrhythmia globally
and is associated with ischemic stroke and heart failure. Patients with atrial fibrillation are …

An automated analysis method enabling the screening of covalent thrombin and factor XIIa inhibitors via liquid chromatography‐mass spectrometry

C Erbacher, M Athmer, E Kröger… - Drug Testing and …, 2024 - Wiley Online Library
An automated sample preparation and separation method for the analysis of various
enzyme‐inhibitor combinations using liquid chromatography (LC) coupled to mass …

Pyrazole-based thrombin inhibitors with a serine-trapping mechanism of action: synthesis and biological activity

C Dunker, L Imberg, AI Siutkina, C Erbacher… - Pharmaceuticals, 2022 - mdpi.com
New antithrombotic drugs are needed to combat thrombosis, a dangerous pathology that
causes myocardial infarction and ischemic stroke. In this respect, thrombin (FIIa) represents …