Phosphonic peptide inhibitors of bacterial collagenases

Details Phosphonic peptide inhibitors of bacterial collagenases Phosphonic peptide inhibitors of bacterial collagenases

1992-09-23

1995-02-14

Walsh, Stephen G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 514 19, 530331, 530332, A61K 3764, A61K 3702, C07K 508, C07K 510

Patent

active

053896122

ABSTRACT:
The invention relates to novel derivatives of peptides usable as inhibitors of bacterial collagenases.
These derivatives comply with the formula: ##STR1## in which R.sup.1 is an optionally substituted aryl or aralkyl group or the group ##STR2## with R.sup.6 being the side chain of an .alpha.-amino acid and R.sup.7 R.sup.8 a protective group or a radical derived from an amino acid or a protected peptide, R.sup.2 is derived from proline, hydroxyproline, thiazolidine or dehydroproline, R.sup.3 is H or an alkyl, and R.sup.4 is the side chain of an amino acid and R.sup.5 and R'.sup.5 are H, a metal, an alkyl or benzyl.
The derivatives in which R'.sup.5 is a metal or hydrogen can be used as inhibitors of bacterial collagenases.

REFERENCES:
patent: 4472381 (1984-09-01), Sakakibara et al.
patent: 4558034 (1985-12-01), Galardy et al.
patent: 4935404 (1990-06-01), Hunter et al.
patent: 5100874 (1992-03-01), Odake et al.
Seifter et al, "The Collagenases", pp. 670-677 in The Enzymes, vol. III, 3rd Edition, Boyer (Academic Press 1971).
"Phosphorus-containing Inhibitors of Angiotensin-converting Enzyme", Thorsett et al., Proc. Natl. Acad. Sci. USA, vol. 79, pp. 2176-2180, Apr. 1982.
"Inhibition of Collagenase from Clostridium Histolyticm by Phosphoric and Phosphonic Amides", Galardy et al., Biochemistry 1983, vol. 22, pp. 4556-4561.
Eur. J. Biochem. 172, 761-766, 1988. New Thiol Inhibitors of Clostridium Histolyticum Collagenase, Yiotakis et al.
Eur. J. Biochem., 191, pp. 685-693, 1990. Inhibition of Chlostridium Histolyticum Collagenases by Phosphonamide Peptide Inhibitors, Dive et al.

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