Anhydro- and isomer-A-21978C cyclic peptides

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 2, 530317, A61K 3812, C07K 1100

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active

059122269

ABSTRACT:
Two new groups of A-21978C cyclic peptides, anhydro- and isomer-A21978C peptide derivatives, have antibacterial activity and are useful as intermediates. The two groups are prepared via transpeptidation of the parent cyclic peptides. Pharmaceutical formulations containing the new peptides as active ingredients and methods of treating infections caused by susceptible Gram-positive bacteria with the formulations are also provided.
The invention also provides an antibacterial composition containing the new drug substance LY 146032 in substantially pure form.

REFERENCES:
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patent: 4399067 (1983-08-01), Debono
patent: 4537717 (1985-08-01), Abbott et al.
Goodman et al, American Chemical Society, vol. 12, No. 1, (Jan. 1979), pp. 1-7.
Organic Chemistry, 3rd ed., Morrison & Boyd, p. 225.
T. Geiger et al., "Deamidation, Isomerization, and Racemization at Asparaginyl and Aspartyl Residues in Peptides," J. Biol. Chem. 262 (2), 785-794 (1987).
M. Bodansky et al., "Side Reactions in Peptide Synthesis," Synthesis 1981 (May), 333-338, 351-356.
E. A. Hagan et al., "Synthesis of Ac-Asp-Gly-Ser and Ac-Asp-Pro-Leu-Gly-NH.sub.2," Int. J. Peptide Protein Res. 23, 642-649 (1984).
M. Bodanszky et al., "Side Reactions in Peptide Synthesis," Int. J. Peptide Protein Res. 12, 69-74 (1978).
B. A. Johnson et al., "Enzymatic Protein Carboxyl Methylation at Physiological pH: Cyclic Imide Formation Explains Rapid Methyl Turnover," Biochemistry 24, 2581-2586 (1985).

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