Inhibitors of bacterial collagenase

Details Inhibitors of bacterial collagenase Inhibitors of bacterial collagenase

1984-01-31

1985-12-10

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125R, A61K 3700, C07C10352

Patent

active

045580340

ABSTRACT:
This invention relates to amino acid derivatives that are useful as inhibitors of bacterial collagenase. The compounds of this invention have a general formula: ##STR1## wherein R is alkyl, aralkyl, aryl, alkoxy, aryloxy, hydroxy or pharmaceutically acceptable salts thereof; R.sub.1 is hydrogen, alkali metal, lower alkyl, phenyl lower alkyl, or phenyl, or substituted phenyl wherein the substituent is halo, lower alkoxy or lower alkyl or nitro or carboxy or cyano, and pharmaceutically acceptable salts thereof; R.sub.2, R.sub.3 and R.sub.4 is hydrogen or alkyl; R.sub.2 and R.sub.4 may be the side groups found on the 20 common .alpha.-amino acids; R.sub.3 and R.sub.4 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms; Y is alkoxy, aryloxy, primary amide, amino acid derivative or ##STR2## where R.sub.5 and R.sub.6 is hydrogen or alkyl; R.sub.5 and R.sub.6 may be connected together to form an alkylene bridge of from 2 to 4 carbon atoms; X is hydroxyl or pharmaceutically acceptable salts thereof, or an amino acid derivative.

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Chem. Abstr., vol. 95, (1981) 25603y.
Proc. Natl. Acad. Sci., vol. 79, pp. 2176-2180, Apr. 1982.
Galardy, Richard, "Inhibition of Angiotensin Converting Enzyme with N.sup..alpha. -Phosphoryl-L-Ananyl-L-Proline and N.sup..alpha. -Phosphoryl-L-Valyl-L-Tryptophan", Biochemical and Biophysical Research Communications, vol. 97, pp. 94-99 (1980).
Galardy et al., "Inhibition of Collagenase from Clostridum histolyticum by Phosphoric and Phosphonic Amides", American Chemical Society, Biochemistry, vol. 22, pp. 4561-4567 (1983).

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