Method for the preparation of conjugates of adenine-9-beta-arabi

Details Method for the preparation of conjugates of adenine-9-beta-arabi Method for the preparation of conjugates of adenine-9-beta-arabi

1985-12-11

1988-12-27

Chan, Nicky

Chemistry: natural resins or derivatives; peptides or proteins;

Proteins, i.e., more than 100 amino acid residues

Albumin

C07D 1506

Patent

active

047941707

ABSTRACT:
For the preparation of conjugates of adenine-9-beta-D-arabinofuranoside 5'monophosphate (ara-AMP) with lactosaminated human albumin (L-HSA) aqueous solutions of the two components to be conjugated are brought into contact in the presence of 1-ethyl-3-(dimethylaminopropyl)-carbodiimide, by adjusting the pH in the range from slightly acidic to alkaline and by carrying out the conjugate separation. The resulting conjugate, wherein the molar ratio, as determined through spectrophotometric route, between ara-AMP and L-HSA does vary between 5 and 20, remains soluble after lyophilization even at room temperature and shows biological activity at least equivalent to that of the conjugate as prepared according to the known art.

REFERENCES:
Fuime et al., Febs Lett; 116:185-188 (1980).
Fiume, Febs Letters vol. 129, pp. 261-264, Jul. 1981.
Fiume, Pharmaceutica Acta Helvetiae, No. 11, 1985 (Reprint).

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