Peptide elastase inhibitors and methods

Details Peptide elastase inhibitors and methods Peptide elastase inhibitors and methods

1984-12-18

1987-02-17

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530331, A61K 3764, C07K 508

Patent

active

046439919

ABSTRACT:
Compounds useful as inhibitors of the enzyme elastase are of the following general formula: ##STR1## wherein Z is selected from the group consisting of R"O--Suc-- where R" is lower alkyl of 1 to 3 carbon atoms and CF.sub.3 CO--; X is oxygen or sulfur; R' is selected from the group consisting of straight or secondary branch-chained alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 3 carbon atoms, alkynyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, and benzyl, and R is selected from the group consisting of susbstituted or unsubstituted phenyl wherein the substituents are selected from the group consisting of nitro, and pentafluoro; benzyl, CH.sub.2 CF.sub.2 CF.sub.2 CF.sub.3, 1-lower alkyl tetrazolyl, 1-phenyltetrazolyl, 2-thioxo-3-thiazolidinyl-, pyridyl and benzothiazolyl, provided that when R is paranitrophenyl, R' is other than tertiary-butyl, benzyl or cyclohexyl, and when X is sulfur, R is other than benzyl.

REFERENCES:
patent: 4155914 (1979-05-01), Batz et al.
patent: 4248883 (1981-02-01), Sawayama et al.
F. Conti et al, "Cyclols-Formation from Tripeptide Systems and Structure Assignment by Carbon-13 Nuclear Magnetic Resonance", Int. J. Peptide Protein Res. 5, 1973, 353-357.
K. Tsuji et al, "Peptidyl Carbamate Esters: A New Class of Specific Elastase Inhibitors", Biochemical and Biophysical Research Communications, vol. 122, No. 2, 1984, pp. 571-576.

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