Inhibition of Human Neutrophil Elastase. 4. Design, Synthesis, X-ray Crystallographic Analysis, and Structure−Activity Relationships for a Series of P2-Modified, Orally Active Peptidyl Pentafluoroethyl Ketones

1998 ◽  
Vol 41 (14) ◽  
pp. 2461-2480 ◽  
Author(s):  
Robert J. Cregge ◽  
Sherrie L. Durham ◽  
Robert A. Farr ◽  
Steven L. Gallion ◽  
C. Michelle Hare ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Crystallographic Analysis ◽  
Human Neutrophil Elastase ◽  
Design Synthesis ◽  
X Ray ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Orally Active

Inhibition of Human Neutrophil Elastase with Peptidyl Electrophilic Ketones. 2. Orally Active PG-Val-Pro-Val Pentafluoroethyl Ketones

1994 ◽  
Vol 37 (26) ◽  
pp. 4538-4553 ◽  
Author(s):  
Michael R. Angelastro ◽  
Larry E. Baugh ◽  
Philippe Bey ◽  
Joseph P. Burkhart ◽  
Teng-Man Chen ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Orally Active

Discovery and Biological Activity of Orally Active Peptidyl Trifluoromethyl Ketone Inhibitors of Human Neutrophil Elastase

1997 ◽  
Vol 40 (12) ◽  
pp. 1876-1885 ◽  
Author(s):  
Philip D. Edwards ◽  
Donald W. Andisik ◽  
Craig A. Bryant ◽  
Barbara Ewing ◽  
Bruce Gomes ◽  
...  
Keyword(s):  
Biological Activity ◽  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Orally Active

Design and Synthesis of New Orally Active Nonpeptidic Inhibitors of Human Neutrophil Elastase

2000 ◽  
Vol 43 (26) ◽  
pp. 4927-4929 ◽  
Author(s):  
Kazuyuki Ohmoto ◽  
Tetsuya Yamamoto ◽  
Toshihide Horiuchi ◽  
Hirotoshi Imanishi ◽  
Yoshihiko Odagaki ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Design And Synthesis ◽  
Orally Active

scholarly journals Benzylaminoethyureido-Tailed Benzenesulfonamides: Design, Synthesis, Kinetic and X-ray Investigations on Human Carbonic Anhydrases

2020 ◽  
Vol 21 (7) ◽  
pp. 2560 ◽  
Author(s):  
Majid Ali ◽  
Murat Bozdag ◽  
Umar Farooq ◽  
Andrea Angeli ◽  
Fabrizio Carta ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Design Strategy ◽  
Binding Mode ◽  
Crystallographic Analysis ◽  
Carbonic Anhydrases ◽  
Detailed Structure ◽  
Design Synthesis ◽  
X Ray ◽  
Structure Activity ◽  
New Compounds

A drug design strategy of carbonic anhydrase inhibitors (CAIs) belonging to sulfonamides incorporating ureidoethylaminobenzyl tails is presented. A variety of substitution patterns on the ring and the tails, located on para- or meta- positions with respect to the sulfonamide warheads were incorporated in the new compounds. Inhibition of human carbonic anhydrases (hCA) isoforms I, II, IX and XII, involving various pathologies, was assessed with the new compounds. Selective inhibitory profile towards hCA II was observed, the most active compounds being low nM inhibitors (KIs of 2.8–9.2 nM, respectively). Extensive X-ray crystallographic analysis of several sulfonamides in an adduct with hCA I allowed an in-depth understanding of their binding mode and to lay a detailed structure-activity relationship.

Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine- trans -lactams

2001 ◽  
Vol 11 (2) ◽  
pp. 243-246 ◽  
Author(s):  
Simon J.F Macdonald ◽  
Michael D Dowle ◽  
Lee A Harrison ◽  
Julie E Spooner ◽  
Pritom Shah ◽  
...  
Keyword(s):  
Neutrophil Elastase ◽  
Human Neutrophil ◽  
Human Neutrophil Elastase ◽  
Orally Active ◽  
Intracellular Inhibition
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