Nonpeptidic Inhibitors of Human Leukocyte Elastase. 3.1 Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of Orally Active 3-Amino-6-phenylpyridin-2-one Trifluoromethyl Ketones

Journal of Medicinal Chemistry

Volumn 37, Issue 20, 1994, Pages 3313-3326

  Bernstein, Peter R ^a,b   Andisik, Don ^a,b   Bradley, Prudence K ^a,c   Bryant, Craig B ^a,b   Ceccarelli, Christopher ^a,c   Damewood, James R ^a,c   Earley, Roger ^a,d   Edwards, Philip D ^a,b   Feeney, Scott ^a,b   Gomes, Bruce C ^a,b   Kosmider, Benedict J ^a,b   Steelman, Gary B ^a,b   Thomas, Roy M ^a,b   Vacek, Edward P ^a,b   Veale, Chris A ^a,b   Williams, Joseph C ^a,b   Wolanin, Donald J ^a,b   Woolson, Sheila A ^a,b  

^a ASTRAZENECA   (United Kingdom)

^b Department of Medicinal Chemistry ^*  (United States)

^c Department of Medicinal Chemistry ^*  (United States)

^d AstraZeneca   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1,2 DIHYDRO 2 OXO 6 PHENYL 3 PHENYLACETAMIDO 1 PYRIDYL) N (3,3,3 TRIFLUORO 1 ISOPROPYL 2 OXOPROPYL)ACETAMIDE; 2 [3 [(BENZYLOXYCARBONYL)AMINO] 1,2 DIHYDRO 2 OXO 6 PHENYL 1 PYRIDYL] N (3,3,3 TRIFLUORO 2 HYDROXY 1 ISOPROPYL)ACETAMIDE; ELASTASE INHIBITOR; LEUKOCYTE ELASTASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DOSE RESPONSE; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; HAMSTER; HUMAN; LUNG HEMORRHAGE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ACETAMIDES; AMINO ACID SEQUENCE; ANIMAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HAMSTERS; HEMORRHAGE; HUMAN; LEUKOCYTE ELASTASE; LUNG DISEASES; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MOLECULAR STRUCTURE; PANCREATIC ELASTASE; PYRIDONES; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 0027945808     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm00046a016     Document Type: Article

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