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Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Short KM, Estiarte MA, Pham SM, Williams DC, Igoudin L, Dash S, Sandoval N, Datta A, Pozzi N, Di Cera E, Kita DB. Short KM, et al. Among authors: kita db. Eur J Med Chem. 2023 Jan 15;246:114855. doi: 10.1016/j.ejmech.2022.114855. Epub 2022 Oct 27. Eur J Med Chem. 2023. PMID: 36462436
Reversible covalent direct thrombin inhibitors.
Sivaraja M, Pozzi N, Rienzo M, Lin K, Shiau TP, Clemens DM, Igoudin L, Zalicki P, Chang SS, Estiarte MA, Short KM, Williams DC, Datta A, Di Cera E, Kita DB. Sivaraja M, et al. Among authors: kita db. PLoS One. 2018 Aug 2;13(8):e0201377. doi: 10.1371/journal.pone.0201377. eCollection 2018. PLoS One. 2018. PMID: 30071045 Free PMC article.
VE-1902-A direct thrombin inhibitor with reversible covalent mechanism of action shows efficacy with reduced bleeding in rodent models of thrombosis.
Sivaraja M, Clemens DM, Sizikov S, Dash S, Xu C, Rienzo M, Yang B, Ryan M, Chattopadhyay M, Igoudin L, Chang SS, Keutzer S, Zalicki P, Estiarte MA, Shiau TP, Short KM, Williams DC, Datta A, Pozzi N, Di Cera E, Gibson CM, Fox KAA, Kita DB. Sivaraja M, et al. Among authors: kita db. Thromb Res. 2020 Jun;190:112-121. doi: 10.1016/j.thromres.2020.04.020. Epub 2020 Apr 19. Thromb Res. 2020. PMID: 32339947 Free PMC article.