Biaryl substituted alkylboronate esters as thrombin inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 13, 1997, Pages 1595-1600

  Quan, M L ^a   Wityak, J ^a   Dominguez, C ^a   Duncia, J V ^a   Kettner, C A ^a   Ellis, C D ^a   Liauw, A Y ^a   Park, J M ^a   Santella, J B ^a   Knabb, R M ^a   Thoolen, M J ^a   Weber, P C ^a,b   Wexler, R R ^a  

^a DUPONT COMPANY   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYL DEXTRO PHENYLALANYLPROLYLBOROARGININE; BORONIC ACID DERIVATIVE; THROMBIN INHIBITOR;

ARTICLE; DRUG ACTIVITY; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION;

EID: 17644432096     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00254-0     Document Type: Article

References (10)

1. Luchtman-Jones, L.; Broze, G. J. Ann. Med. 1995, 27, 47.
2. (a). Knabb, R. M.; Kettner, C. A.; Timmermans, P. B. M. W. M.; Reilly, T. M. Thromb. Haemostas. 1992, 67, 56.
3. (b). Kettner, C. A.; Mersinger, L. J.; Knabb, R. M. J. Biol. Chem. 1990, 265, 18289.
4. Burley, S. K.; Petsko, G. A. Science 1985, 229, 23.
5. Weber, P. unpublished results.
6. Crystals were prepared and inhibitors were added using the procedure of Weber, et. al. (Weber, P. C.; Lee, S.; Lewandowski, F. A.; Schadt, M. C.; Chang, C; Kettner, C. A. Biochemistry, 1995, 34, 3750). Diffraction data was obtained to a resolution of 2.1 Angstrom and data were refined to a crystallographic R-factor of 0.200.
7. Wityak, J.; Earl, R. A.; Abelman, M. M.; Bethel, Y. B.; Fisher, B. N.; Kauffman, G. S.; Kettner, C.A.; Ma, P.; McMillian, J. L.; Mersinger, L. J.; Pesti, J.; Pierce, M. E.; Rankin, F. W.; Chorvat, R. J.; Confalone, P. N. J. Med. Chem. 1995, 60, 3717.
8. Matteson, D. S.; Jesthi, P. K.; Sadhu, K. M. Organometallics 1984, 3, 1284.
9. Miyaura, N.; Yanagi, T.; Suzuki, A. Synth. Commun. 1981, 11, 513.
10. Schenone, P.; Sansebastiano, L.; Mosti, L. J. Het. Chem. 1990, 27, 302.