S D Lewis

Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.

J. Vacca, S. Gardell, T. Tucker, 1997, Journal of medicinal chemistry.

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.

S. Brady, J. Vacca, S. Gardell, 1998, Journal of medicinal chemistry.

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.

M. Bock, R. Freidinger, J. Vacca, 1997, Journal of medicinal chemistry.

Crystal structure of human alpha-thrombin complexed with hirugen and p-amidinophenylpyruvate at 1.6 A resolution.

Y Li, Z. Chen, Y. Li, 1995, Archives of biochemistry and biophysics.

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

J. Vacca, J. Shafer, Z. Chen, 1998, Bioorganic & medicinal chemistry letters.

Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.

S. Brady, J. Vacca, S. Gardell, 1998, Journal of medicinal chemistry.

Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.

S. Brady, J. Vacca, T. Tucker, 1998, Journal of medicinal chemistry.