Antibiotics

Details Antibiotics Antibiotics

1997-05-16

1999-08-24

Peselev, Elli

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 65, A61K 3270, C07H 1708

Patent

active

059424958

ABSTRACT:
The invention relates to an N-alkyl-N-glycosyl derivative of antifungal antibiotics of the polyene macrolide group of general formula 1(a), wherein M represents polyene macrolide antibiotics residues, R represents a variable part of sugar residue, R.sup.1 represents a C.sub.1-4 alkyl group and R.sup.2 represents hydrogen or a C.sub.1-4 alkyl group; their salts of general formula 2(a), wherein R, R.sup.1, R.sup.2 and M are as herein defined and A represents an anion of organic or inorganic acid. Compounds of formula 1(b) and 2(b) wherein the N-alkyl and alkyl ester groups are represented by methyl are of particular interest.
The invention relates also to processes for preparation of the compounds, to compositions containing these compounds and to their use in therapy and the treatment of external and internal fungal infections in humans and animals. ##STR1##

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DN&P 10(10), p. 617, Dec. 1997.
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Pleskoff et al, "Amphotericin B Derivative Blocks Human Immunodeficiency Virus Type 1 Entry after CD4 Binding: Effect on Virus-Cell Fusion but Not on Cell-Cell Fusion", J. Virology vol. 69 N.sup.o 1 (1995) pp. 570-574.
Cefai et al "MS-8209, A New Amphotericin B Derivative that Inhibits HIV-1 Replication in vitro and Restores T-Cell Activation via the CD3/TcR in HIV-infected CD4+ Cells" AIDS vol. 5 N.sup.o 12 (1991) pp. 1453-1461.
Saint-Julien et al "Activity of MS-8209, a Nonester Amphotericin B Derivative, in Treatment of Experimental Systemic Mycoses" Antimicrobial Agents and Chemotherapy, vol. 36 N.sup.o 12 (1992) pp. 2722-2728.

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