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1eau

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[[Image:1eau.jpg|left|200px]]
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{{Seed}}
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{{STRUCTURE_1eau| PDB=1eau | SCENE= }}
{{STRUCTURE_1eau| PDB=1eau | SCENE= }}
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'''NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE'''
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===NONPEPTIDIC INHIBITORS OF HUMAN LEUKOCYTE ELASTASE. 6. DESIGN OF A POTENT, INTRATRACHEALLY ACTIVE, PYRIDONE-BASED TRIFLUOROMETHYL KETONE===
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==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.
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(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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:53:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 00:25:37 2008''

Revision as of 21:25, 30 June 2008

Image:1eau.png

Template:STRUCTURE 1eau

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

Template:ABSTRACT PUBMED 7837235

About this Structure

1EAU is a Single protein structure of sequence from Sus scrofa. Full crystallographic information is available from OCA.

Reference

Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone., Bernstein PR, Gomes BC, Kosmider BJ, Vacek EP, Williams JC, J Med Chem. 1995 Jan 6;38(1):212-5. PMID:7837235

Page seeded by OCA on Tue Jul 1 00:25:37 2008

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