ANTIFUNGAL AZOLE COMPOUNDS HAVING FLUOROVINYL ETHER GROUP AS SIDE CHAIN, WHICH MINIMIZE LIVER TOXICITY DUE TO LONG TIME DOSAGE AND ARE STABLE IN RELATION TO ORAL DOSAGE TOXICITY AND ANTIFUNGAL COMPOSITION COMPRISING THE SAME

摘要

PURPOSE: Antifungal azole compounds having fluorovinyl ether group as a side chain and an antifungal composition comprising the same compounds are provided, which compounds have improved antifungal activity, especially against antifungal agent resistant fungi, and improved stability in relation to human CytP450 3A4 enzyme, so that they can minimize liver toxicity due to the long time dosage, and also be stable in relation to the oral dosage toxicity. CONSTITUTION: The antifungal azole compounds having fluorovinyl ether group represented by formula (I) or pharmaceutically acceptable salts, isomers or ester compounds thereof are provided, wherein A is oxygen(-O-) or 4-(1,2,4-triazol-3-yl) phenylether, 4-(1,2,4-triazol-5-one-4-yl) phenylether, 4-(imidazol-2-one-3-yl) phenylether, or 4-(imidazolidine-2-one-3-yl) phenylether; R is hydrogen or trifluoromethy; R' is hydrogen or C1-4 alkyl; and X is hydrogen, halogen, C1-4 alkyl, haloalkyl, alkoxy or 3,4-dioxyalkylene ring. The antifungal composition comprises the antifungal azole compounds having fluorovinyl ether group represented by formula (I) and pharmaceutically acceptable carriers.