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Hassan M. Faidallah,Sherif A. F. Rostom,Salem A. Basaif,Mohammed S. T. Makki,Khalid A. Khan 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.11
This study reports the synthesis of some novelisoxazolo[4,5-d]pyridazines and structurally related thiazolo[4,5-d]pyridazines, and their biological evaluation asantimicrobial agents. The proposed compounds weredesigned to contain pharmacophores such as urea, thiourea,sulfonylurea (thiourea) and some derived functionalities thatare believed to contribute to the anticipated biologicalactivities. The results revealed that 25 compounds displayedbroad spectrum of antibacterial activity, with greater inhibitoryeffect on the growth of the tested Gram positive strainscompared to Gram negative ones. Moreover, 14 compoundswere able to produce appreciable growth inhibitory activityagainst Candida albicans fungus when compared toClotrimazole. Most of the tested isoxazolo[4,5-d]pyridazinesdisplayed better antimicrobial profile than theircorresponding thiazolo[4,5-d]pyridazine congeners. Fourcompounds namely, p-(3,7-dimethyl-4-oxo-4H-isoxazolo[4,5-d]pyridazine-5-yl)benzenesulfonylthioureas (11c–d),3-substituted-2-[p-(3,7-dimethyl-4-oxo-4H-isoxazolo[4,5-d]pyridazine-5-yl)-benzene-sufonylimino]-4-oxothiazolidines(13d) and p-(2,7-dimethyl-4-oxo-4H-thiazolo[4,5-d]pyridazin-5-yl)benzenesulfonylthiourea (24c) werefound to be most active antimicrobial members in presentstudy.