96747-25-0Relevant academic research and scientific papers
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity
Hangeland, Jon J.,Friends, Todd J.,Rossi, Karen A.,Smallheer, Joanne M.,Wang, Cailan,Sun, Zhong,Corte, James R.,Fang, Tianan,Wong, Pancras C.,Rendina, Alan R.,Barbera, Frank A.,Bozarth, Jeffrey M.,Luettgen, Joseph M.,Watson, Carol A.,Zhang, Ge,Wei, Anzhi,Ramamurthy, Vidhyashankar,Morin, Paul E.,Bisacchi, Gregory S.,Subramaniam, Srinath,Arunachalam, Piramanayagam,Mathur, Arvind,Seiffert, Dietmar A.,Wexler, Ruth R.,Quan, Mimi L.
, p. 9915 - 9932 (2015/02/05)
Novel inhibitors of FXIa containing an (S)-2-phenyl-1-(4-phenyl-1H-imidazol-2-yl)ethanamine core have been optimized to provide compound 16b, a potent, reversible inhibitor of FXIa (Ki = 0.3 nM) having in vivo antithrombotic efficacy in the rabbit AV-shunt thrombosis model (ID50 = 0.6 mg/kg + 1 mg kg-1 h-1). Initial analog selection was informed by molecular modeling using compounds 11a and 11h overlaid onto the X-ray crystal structure of tetrahydroquinoline 3 complexed to FXIa. Further optimization was achieved by specific modifications derived from careful analysis of the X-ray crystal structure of the FXIa/11h complex. Compound 16b was well tolerated and enabled extensive pharmacologic evaluation of the FXIa mechanism up to the ID90 for thrombus inhibition.
A novel and efficient method for cleavage of phenacylesters by magnesium reduction with acetic acid
Kokinaki, Stella,Leondiadis, Leondios,Ferderigos, Nikolas
, p. 1723 - 1724 (2007/10/03)
(Equation Presented) In the present study, we use magnesium turnings as a new deprotection reagent for the phenacyl group during orthogonal organic synthesis in the presence of other esters and sensitive protecting groups. By applying the new magnesium turnings/acetic acid deprotection method, phenacyl group can be more easily combined with other protecting groups that are not compatible with the zinc/acetic acid method.
Intramolecular triplet-triplet energy transfer in short flexible bichromophoric amino acids, dipeptides and carboxylic acid diester
Zabadal, Miroslav,Heger, Dominik,Klan, Petr,Kriz, Zdenek
, p. 776 - 796 (2007/10/03)
Efficiencies of the intramolecular triplet-triplet energy transfer (ITET) in various bichromophoric amino acids (glycine, valine, phenylalanine, and sarcosine), dipeptides (glycylglycine, phenylalanylphenylalanine), and a simple diester, with the benzoyl
