Concepedia

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of βII tryptase

Julian Levell, Peter C. Astles, Paul Eastwood, Jennifer Cairns, Olivier Houille, Suzanne C. Aldous, Gregory H. Merriman, Brian Whiteley, James Pribish, Mark Czekaj,

Bioorganic & Medicinal Chemistry · 2005 · 29 citations · 17 references

DOI

Concepts

References

17

Human β-tryptase is a ring-like tetramer with active sites facing a central pore

Pedro José Barbosa Pereira, Andreas Bergner, Sandra Macedo‐Ribeiro et al. · Nature · 1998 · 299 citations

, , +8

Discovery of 1-[3-(Aminomethyl)phenyl]-<i>N</i>-[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1<i>H</i>-pyrazole-5-carboxamide (DPC423), a Highly Potent, Selective, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa

Donald Pinto, Michael J. Orwat, Shuaige Wang et al. · Journal of Medicinal Chemistry · 2001 · 172 citations · Full text

, , +11

HT29‐MTX and Caco‐2/TC7 Monolayers as Predictive Models for Human Intestinal Absorption: Role of the Mucus Layer

Catherine Pontier, Jean I. Pachot, Roger P. Botham et al. · Journal of Pharmaceutical Sciences · 2001 · 148 citations

, , +16

Crystal Structures of Human Factor Xa Complexed with Potent Inhibitors

S. Maignan, J.P. Guilloteau, Stéphanie Pouzieux et al. · Journal of Medicinal Chemistry · 2000 · 139 citations · Full text

, , +16

Molecular Structures of Human Factor Xa Complexed with Ketopiperazine Inhibitors:  Preference for a Neutral Group in the S1 Pocket

S. Maignan, J.P. Guilloteau, Yong Mi Choi-Sledeski et al. · Journal of Medicinal Chemistry · 2003 · 119 citations · Full text

, , +11