16-decarboxy-16-hydroxy derivatives of amphotericin B

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

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536 65, A61K 3170, C07H 1708

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active

051008769

ABSTRACT:
Compounds of the formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is --CH.sub.2 OH; R.sub.2 is hydrogen or C.sub.1-8 alkyl; R.sub.3 is hydrogen or an amine protection group; and each R.sub.4 is hydrogen; their preparation, compositions containing them and their use in the treatment of fungal infections are described.

REFERENCES:
patent: 4223130 (1980-09-01), Weinstein
patent: 4235993 (1980-11-01), Sipos et al.
Nicolau et al., J. Am. Chem. Soc. 1988, 110, 4660-4672, "Chemistry of Amphotericin B".
Nicolau et al., J. Am. Chem. Soc. 1988 110, 4696-4705, "Total Synthesis of Ampletricin B".
Cram et al., Organic Chemistry, 2nd ed. (1964) p. 556.

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