Pharmaceutically available protoberberine salts derivatives, and protoberberine salts derivatives, and protoberberine derivatives and salts thereof

摘要

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 compounds of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 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.