New Triazole-Based Potent Inhibitors of Human Factor XIIa as Anticoagulants.

ABSTRACT: Factor XIIa (FXIIa) functions as a plasma serine protease within the contact activation pathway. Various animal models have indicated a substantial role for FXIIa in thromboembolic diseases. Interestingly, individuals and animals with FXII deficiency seem to maintain normal hemostasis. Consequently, inhibiting FXIIa could potentially offer a viable therapeutic approach for achieving effective and safer anticoagulation without the bleeding risks associated with the existing anticoagulants. Despite the potential, only a limited number of small molecule inhibitors targeting human FXIIa have been documented. Thus, we combined a small library of 32 triazole and triazole-like molecules to be evaluated for FXIIa inhibition by using a chromogenic substrate hydrolysis assay under physiological cond

SUBMITTER: Woodland MD 

PROVIDER: S-EPMC10918664 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature