| 摘要 |
<p>Cpds. of formula (I) and their salts are new, where R is phenyl (opt. substd. by 1-3 F, Cl, Br, I, CF3, 1-4C alkyl or 1-4C alkoxy) or 5-chloropyridin-2-yl; R1 is CN, CSNH2 or CONR2R3; either (a) R2 is H or 1-6C alkyl and R3 is H, 1-6C alkyl, benzyl, phenethyl, Ph, CH2CF3, adamantyl, pyridinylmethyl, 3-7C cycloalkyl, carbamoylmethyl, (2-4C)alkenylmethyl, 2-hydroxyethyl, 2-dimethyl-aminoethyl, 2-methylthioethyl, 2-methylsulphinylethyl or 2-methylsulphonylethyl or 2-phenoxyethyl (the benzyl, phenethyl, Ph and PhO gps. are opt. ring substd. by 1 or 2, F, Cl, Br, I, CF3, 1-4C alkyl or 1-4C alkoxy); (b) R2 + R3 form (CH2), (CH2)4, (CH2)5, (CH2)2-O-(CH2)2 or (CH2)2-NR4-(CH2)2; (c) R2 is H or 1-4C alkyl and R3 is 2-4C alkanoyl or PhCO (opt. ring substd. by 1 or 2 F, Cl, Br, I, CF3, 1-4C alkyl or 1-4C alkoxy); or (d) R2 and R3 are (1-4C) alkoxycarbonyl; and R5 and R6 are H or Me). Intermediates of formula (II) are new. Cpds. (I( are antifungal agents effective against topical and systemic fungal infections in man and against phytopathogenic fungi. Dose is 0.1-5 mg/kg. orally or parenterally daily.</p> |
