Synergistine derivatives, their preparation and pharmaceutical c

Details Synergistine derivatives, their preparation and pharmaceutical c Synergistine derivatives, their preparation and pharmaceutical c

1984-07-12

1986-10-14

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530317, A61K 3702, C07K 512

Patent

active

046172904

ABSTRACT:
The invention provides novel synergistine derivatives of the formula: ##STR1## in which Y=H or N(CH.sub.3).sub.2 : and R.sub.1 =H and R.sub.2 =OH or alkyl optionally substituted by COOH, alkoxycarbonyl or OH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 =cycloalkyl (of 3 to 7 carbons) or a heterocycle chosen from azetidine, pyrrolidine, piperidine or azepine (optionally substituted on the nitrogen by alkyl), or R.sub.1 =formyl or alkylcarbonyl and R.sub.2 =alkyl substituted by COOH or by alkylamino or dialkylamino the alkyl radicals of which can form a heterocycle, or R.sub.2 is a heterocycle as defined above, or R.sub.1 and R.sub.2, which are identical or different, represent alkyl optionally substituted by COOH, alkoxycarbonyl, OH, alkylamino, or dialkylamino of which the alkyl radicals can form a heterocycle, or R.sub.1 and R.sub.2 form an azetidine, pyrrolidine, piperidine, morpholine or piperazine ring (optionally substituted by alkyl), all the alkyls having 1 to 5 carbon atoms. These compounds are useful as antibacterial agents.

REFERENCES:
J. Preud'homme, P. Tarridec et A. Belloc, pp. 585-591 (1967).
Chem. Abstr., vol. 99 (1983) 212905.
Chem. Abstr., vol. 76 (1972) 127404.
Chem. Abstr., vol. 63 (1965) 13408.
Merck Index, 9th edition (1976) "Mikamycin and Vinginiamycin", Preud'homme et al., article.
La Presse Medicale, 14-21 Juillet 1984, 13 No. 29, by Mollin.
Chemotherapy 29: 218-224 (1983), by Mutton et al.

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