1eau: Difference between revisions

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[[Image:1eau.jpg|left|200px]]
{{Seed}}
[[Image:1eau.png|left|200px]]


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{{STRUCTURE_1eau|  PDB=1eau  |  SCENE=  }}  
{{STRUCTURE_1eau|  PDB=1eau  |  SCENE=  }}  


'''NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE'''
===NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE===




==Overview==
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Further modification of the 3-amino substituent in a trifluoromethyl ketone-based series of 3-amino-6-phenylpyridin-2-ones that had been optimized for oral activity led to analogs that were potent intratracheal inhibitors in a model of HLE-induced lung damage in the hamster. The best 3-amino substituent for intratracheal activity is [4-[N-[(4-chlorophenyl)sulfonyl]-carbamoyl]phenyl]sulfonyl. At a 30 min prechallenge interval, compound 9, which incorporates this substituent, had an ED50 of approximately 2 nmol/animal and, qualitatively, afforded a very similar dose-response relationship to that found with a peptidic trifluoromethyl ketone inhibitor, ICI 200,355.
The line below this paragraph, {{ABSTRACT_PUBMED_7837235}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 7837235 is the PubMed ID number.
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{{ABSTRACT_PUBMED_7837235}}


==About this Structure==
==About this Structure==
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[[Category: Sus scrofa]]
[[Category: Sus scrofa]]
[[Category: Ceccarelli, C.]]
[[Category: Ceccarelli, C.]]
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