ΝΕΟ ΠΑΡΑΓΩΓΟ ΑΡΥΛΑΜΙΔΙΝΗΣ Ή ΑΛΑΣ ΑΥΤΟΥ

Ένα παράγωγο αρυλαμιδίνης που παρίσταται από έναν γενικό τύπο που περιγράφεται κατωτέρω, ή ένα άλας αυτού έχει άριστη αντιμυκητική δράση και υψηλή ασφάλεια, και είναι χρήσιμο ως αντιμυκητικό μέσο με καλές φαρμακοκινητικές και φαρμακοδυναμικές ιδιότητες: Arylamide derivatives (I) are new. Arylamide derivatives of formula (I) and their salts are new. [Image] X : optionally substituted lower alkylene or alkenylene; G 1O, S or NH; G 2C or N; R aH, halo or optionally substituted alkyl, cycloalkyl or alkoxy; R 1optionally protected or substituted amidino; R 2NR 3R 4, NR 5YNR 6R 7 or a group of formula (i); R 3H, amino protecting group, a group of formula (ii) or optionally substituted cycloalkyl or alkenyl; W : a bond or optionally substituted alkylene; Y coptionally substituted 2-4C alkylene; Y c1optionally substituted 1-4C alkylene; R 7bH, amino protecting group, a group of formula (iii) or optionally substituted alkyl, cycloalkyl or alkenyl; Z : optionally substituted lower alkylene or alkenylene; G 3O, S, NH or bond; G 5C or N; R bH, halo or optionally substituted alkyl, cycloalkyl or alkoxy; R 8para or meta to G 3 and is optionally protected or substituted amidino; R 4-R 6H, amino protecting group or optionally substituted alkyl, cycloalkyl or alkenyl; Y : optionally substituted 2-6C alkyelene or 3-6C alkenylene; R 7R 4 or (iii); Y aoptionally substituted 2-4C alkylene; Y boptionally substituted 1-4C alkylene; G 4C or N; R 7aalkyl (optionally substituted by at least one CN, NO 2, halo, sulfo, phosphoryl, lower alkenyl, lower alkoxy, heterocyclyl, cycloalkyl, lower alkylidene, SH, amidinophenylaryloxy, aryloxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkylcarbamoyl, lower alkylsulfonylamino, lower alkylaminosulfonyl, lower carboxylalkenyl, lower alkoxyimino or optionally protected hydroxyl, amino, carbamoyl, hydrocarbamoyl, aminosulfonyl, cyclic amino or lower alkylamino), (iii) or optionally substituted phenyl, cycloalkyl or alkenyl, provided that when G 1 = NH, then X = optionally substituted 3-6C alkylene or alkenylene. [Image] ACTIVITY : Fungicide. In cytotoxicity assays, 4-[2-[1-(3-[4-[amino(imino)methyl]phenoxy]propyl)-4-piperidinyl]ethoxy]benzamidine hydrochloride (Ia) had an IC 50 value for Candida albicans TIMM1623 of 0.0039 mu g/ml. MECHANISM OF ACTION : None given.