| 摘要 |
<p>A new diaminoacid, designated 32232RP, has probable structure (I). It can exist in the form of an inner salt. Also new are the metal salts and acid-addn. salts of (I) and its lactam (35391 RP) of formula (II). (I) is an amorphous white powder readily soluble in water, sparingly soluble in methanol or DMF and almost insoluble in acetone. It has m.pt. 281 degrees C, analysis C 48.0%, H 5.8%, 0 21.0% and N 25.2% and has characteristic UV, IR, 'H-NMR and 13C-NMR Spectra (reproduced). On silica gel t.l.c. plates developed with 60:30:10 v/v/v methanol-1,2-dichloroethane-11N NH3 it has Rf = 0.20 (II) is a white microcrystalline powder soluble in water at 10mg/cc and analyses C 49.6%; H 5.8%, 0 17.6%, N 27.0% with empirical formula (mass spectroscopy) C15H2N7O4. Its spectra are also reproduced and in the t.i.c. system specified it has Rf = 0.70. (I) and (II) are active in vivo and in vitro against fungi and yeasts. their oral LD50 in mice is >=1g/kg. and they are esp. useful in human medicine for treating condidosis (of the mouth, mucosa, intestines or genitalia) or internal mycoses. The usual oral adult dose is 1-10g/day.</p> |
