Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine
Deng, H., Bannister, T.D., Jin, L., Babine, R.E., Quinn, J., Nagafuji, P., Celatka, C.A., Lin, J., Lazarova, T.I., Rynkiewicz, M.J., Bibbins, F., Pandey, P., Gorga, J., Meyers, H.V., Abdel-Meguid, S.S., Strickler, J.E.(2006) Bioorg Med Chem Lett 16: 3049-3054
- PubMed: 16524727 
- DOI: https://doi.org/10.1016/j.bmcl.2006.02.052
- Primary Citation of Related Structures:  
1ZPB, 1ZPC, 2FDA - PubMed Abstract: 
Using an alpha-ketothiazole arginine moiety as a key recognition element, a series of small peptidomimetic molecules was designed and synthesized, and their co-crystal structures with factor XIa were studied in an effort to develop smaller, less peptidic inhibitors as antithrombotic agents.
Organizational Affiliation: 
Department of Medicinal Chemistry, Daiichi Asubio Medical Research Laboratories, LLC (DAIAMED), One Kendall Square, Bldg 700, Cambridge, MA 02139, USA. hongfeng.deng@praecis.com