Discovery of novel hydroxy pyrazole based factor IXa inhibitor

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 10, 2006, Pages 2796-2799

  Vijaykumar, Dange ^a   Sprengeler, Paul A ^a   Shaghafi, Michael ^a   Spencer, Jeffrey R ^a   Katz, Brad A ^a   Yu, Christine ^a   Rai, Roopa ^a   Young, Wendy B ^a   Schultz, Brian ^a   Janc, James ^a  

^a CELERA   (United States)

Author keywords

3 Hydroxy pyrazole; Active site; Amidine; Factor IXa inhibitors; Serine protease

Indexed keywords

5 AMIDINOBENZIMIDAZOLE; ANTICOAGULANT AGENT; BENZIMIDAZOLE DERIVATIVE; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 9A INHIBITOR; BLOOD CLOTTING INHIBITOR; HYDROXYL PYRAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANTICOAGULATION; ARTICLE; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG SYNTHESIS; PHARMACOPHORE; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

FACTOR IXA; HUMANS; MODELS, MOLECULAR; PYRAZOLES; SERINE PROTEINASE INHIBITORS;

EID: 33645859039     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.01.123     Document Type: Article

References (16)

1. Mckean M.-L., and Adelman S.J. Expert Opin. Investig. Drugs 7 (1998) 687
2. Weitz J.I., and Bates S.M. J. Thromb. Haemost. 3 (2005) 1843
3. Bajaj S.P., and Joist J.H. Semin. Thromb. Hemost. 25 (1999) 407
4. Young W.B., Kolesnikov A., Rai R., Sprengeler P.A., Leahy E.M., Shrader W.D., Sangalang J., Burgess-Henry J., Spencer J., Elrod K., and Cregar L. Bioorg. Med. Chem. Lett. 11 (2001) 2253
5. Rai R., Kolesnikov A., Li Y., Young W.B., Leahy E., Sprengeler P., Verner E., Shrader W., Burgess-Henry J., Sangalang J., Allen D., Chen Xi., Katz B., Luong C., Elrod K., and Cregar L. Bioorg. Med. Chem. Lett. 11 (2001) 1797
6. Young, W. B.; Mordenti, J.; Torkelson, S.; Shrader, W. D.; Kolesnikov, A.; Rai, R.; Liu, L.; Hu, H.; Leahy, E. M.; Green, M. J.; Sprengeler, P. A.; Katz, B.; Janc, J. W.; Marzec, U. M.; Hanson, S. R.; Bioorg. Med. Chem. Lett., in press.
7. Young, W. B.; Rai, R.; Shrader, W. D.; Burgess-Henry, J.; Hu, H.; Elrod, K.; Sprengeler, P. A.; Katz, B.; Sukbuntherng, J.; Mordenti, J. Bioorg. Med. Chem. Lett., in press.
8. 460).
9. Katz B.A., Elrod K., Verner E., Mackman R.L., Luong C., Shrader W.D., Sendzik M., Spencer J.R., Sprengeler P.A., Kolesnikov A., Tai V.W.-F., Hui H.C.G., Breitenbucher J., Allen D., and Janc J.W. J. Mol. Biol. 329 (2003) 93
10. PDB Entry Code 2flb.
11. PDB Entry Code 1rfn.
12. Katz B.A., Mackman R., Luong C., Radika K., Martelli A., Sprengeler P.A., Wang J., Chan H., and Wong L. Chem. Biol. 7 (2000) 299
13. Selwood D.L., Brummell D.G., Budworth J., Burtin G.E., Campbell R.O., Chana S.S., Charles I.G., Fernandez P.A., Glen R.C., Goggin M.C., Hobbs A.J., Kling M.R., Liu Q., Madge D.L., Meillerais S., Powell K.L., Reynolds K., Spacey G.D., Stables J.N., Tatlock M.A., Wheeler K.A., Wishart G., and Woo C. J. Med. Chem. 44 (2001) 78
14. Chen X., Schneller S.W., Ikeda S., Snoeck R., Andrei G., Jan B., and De Clercq E. J. Med. Chem. 36 (1993) 3727
15. Shrader, W. D.; Kolesnikov, A.; Burgess-Henry, J.; Rai, R.; Hu, H.; Torkelson, S.; Young, W. B.; Sprengeler, P. A.; Yu, C.; Katz, B.; Cabuslay, R.; Gjerstad, E.; Janc, J.; Bioorg. Med. Chem. Lett., in press.
16. Verner E., Katz B.A., Spencer J.R., Allen D., Hataye J., Hruzewicz W., Hui H.C., Kolesnikov A., Li Y., Luong C., Martelli A., Radika K., Rai R., She M., Shrader W., Sprengeler P.A., Trapp S., Wang J., Young W.B., and Mackman R.L. J. Med. Chem. 44 (2001) 2753