Antifungal formulation comprising protoberberine derivatives and

Details Antifungal formulation comprising protoberberine derivatives and Antifungal formulation comprising protoberberine derivatives and

1998-12-10

2000-02-29

Robinson, Allen J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514284, A61K 3144

Patent

active

060309784

ABSTRACT:
The antifungal formulation comprising the novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The formulation of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylamino, acetylamino, C.sub.1 -C.sub.8 trialkyl ammonium, guanidinyl, methylthio, ethylthio, trifluoromethoxy, hydroxy, phenoxy, vinyl, carboxyl and C.sub.1 -C.sub.2 alkoxycarbonyl group.

REFERENCES:
patent: 4749708 (1988-06-01), Maroko
patent: 4761417 (1988-08-01), Maroko
patent: 4980344 (1990-12-01), Maroko
patent: 5153178 (1992-10-01), Maroko
V.M. Mahajan, et al., "Antimycotic Activity of Berberine Sulphate: An Alkaloid From an Indian Medicinal Herb," Sabouraudia (1982), 20, 79-81.

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