|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, Intratracheally active, Pyridone-Based trifluoromethyl ketone.
|
|
|
Authors
|
|
P.R.Bernstein,
B.C.Gomes,
B.J.Kosmider,
E.P.Vacek,
J.C.Williams.
|
|
|
Ref.
|
|
J Med Chem, 1995,
38,
212-215.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
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.
|
|
|
Secondary reference #1
|
|
|
Title
|
|
Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, Synthesis, And X-Ray crystallography of a series of orally active 5-Amino-Pyrimidin-6-One-Containing trifluoromethylketones
|
|
|
Authors
|
|
C.A.Veale,
P.R.Bernstein,
C.Bryant,
C.Ceccarelli,
J.R.Damewood,
R.Earley,
S.W.Feeney,
B.Gomes,
B.J.Kosmider,
G.B.Steelman,
R.M.Thomas,
E.P.Vacek,
J.C.Williams,
D.J.Wolanin,
S.Woolson.
|
|
|
Ref.
|
|
TO BE PUBLISHED ...
|
|
|
|
Secondary reference #2
|
|
|
Title
|
|
Non-Peptidic inhibitors of human leukocyte elastase. 4. Design, Synthesis, And in vitro and in vivo activity of a series of beta-Carbolinone-Containing trifluoromethyl ketones.
|
|
|
Authors
|
|
C.A.Veale,
J.R.Damewood,
G.B.Steelman,
C.Bryant,
B.Gomes,
J.Williams.
|
|
|
Ref.
|
|
J Med Chem, 1995,
38,
86-97.
|
|
|
PubMed id
|
|
|
|
|
Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
percentage match of
93%.
|
|
|
|
|
|
|
Secondary reference #3
|
|
|
Title
|
|
Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, Synthesis, X-Ray crystallographic analysis, And structure-Activity relationships for a series of orally active 3-Amino-6-Phenylpyridin-2-One trifluoromethyl ketones.
|
|
|
Authors
|
|
P.R.Bernstein,
D.Andisik,
P.K.Bradley,
C.B.Bryant,
C.Ceccarelli,
J.R.Damewood,
R.Earley,
P.D.Edwards,
S.Feeney,
B.C.Gomes.
|
|
|
Ref.
|
|
J Med Chem, 1994,
37,
3313-3326.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
Secondary reference #4
|
|
|
Title
|
|
Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, Synthesis, And in vitro activity of a series of 3-Amino-6-Arylopyridin-2-One trifluoromethyl ketones.
|
|
|
Authors
|
|
J.R.Damewood,
P.D.Edwards,
S.Feeney,
B.C.Gomes,
G.B.Steelman,
P.A.Tuthill,
J.C.Williams,
P.Warner,
S.A.Woolson,
D.J.Wolanin.
|
|
|
Ref.
|
|
J Med Chem, 1994,
37,
3303-3312.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
Secondary reference #5
|
|
|
Title
|
|
Nonpeptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-Containing inhibitors
|
|
|
Authors
|
|
P.Warner,
R.C.Green,
B.C.Gomes,
J.C.Williams.
|
|
|
Ref.
|
|
j med chem, 1994,
37,
3090.
|
|
|
|
Secondary reference #6
|
|
|
Title
|
|
Design of orally active, Non-Peptidic inhibitors of human leukocyte elastase.
|
|
|
Authors
|
|
F.J.Brown,
D.W.Andisik,
P.R.Bernstein,
C.B.Bryant,
C.Ceccarelli,
J.R.Damewood,
P.D.Edwards,
R.A.Earley,
S.Feeney,
R.C.Green.
|
|
|
Ref.
|
|
J Med Chem, 1994,
37,
1259-1261.
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
Secondary reference #7
|
|
|
Title
|
|
Design, Synthesis, And kinetic evaluation of a unique class of elastase inhibitors, The peptidyl alpha-Ketobenzoxazoles,And the x-Ray crystal structure of the covalent complex between porcine pancreatic elastase and ac-Ala-Pro-Val-2-Benzoxazole
|
|
|
Authors
|
|
P.D.Edwards,
E.F.Meyer,
J.Vijayalakshmi,
P.A.Tuthill,
D.A.Andisik,
B.Gomes,
A.Strimpler.
|
|
|
Ref.
|
|
j am chem soc, 1992,
114,
1854.
|
|
|
|
Secondary reference #8
|
|
|
Title
|
|
Crystal structure of the covalent complex formed by a peptidyl alpha,Alpha-Difluoro-Beta-Keto amide with porcine pancreatic elastase at 1.78-Angstrom resolution
|
|
|
Authors
|
|
L.H.Takahashi,
R.Radhakrishnan,
R.E.Rosenfield,
E.F.Meyer,
D.A.Trainor.
|
|
|
Ref.
|
|
j am chem soc, 1989,
111,
3368.
|
|
|
|
Secondary reference #9
|
|
|
Title
|
|
X-Ray diffraction analysis of the inhibition of porcine pancreatic elastase by a peptidyl trifluoromethylketone.
|
|
|
Authors
|
|
L.H.Takahashi,
R.Radhakrishnan,
R.E.Rosenfield,
E.F.Meyer,
D.A.Trainor,
M.Stein.
|
|
|
Ref.
|
|
J Mol Biol, 1988,
201,
423-428.
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
|
|
|
