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自从1967年合成第一种咪唑类衍化物克霉唑,并于1970年临床应用以来,不断有新的咪唑类衍化物的合成,目前广泛应用于临床的除克霉唑外,有咪康唑,益康唑,以及近年应用的酮康唑和硫康唑等,为真菌病的治疗开辟了一条新的途径。抗菌作用咪唑类衍化物都是广谱抗真菌药物,体外对皮肤癣菌,念珠菌属,新形隐球菌及粗球孢子菌,荚膜组织胞浆菌,皮炎芽生菌,着色真菌,曲菌有抑制作用。体外对革兰氏阳性球菌亦有活力,其中益康唑似乎更明显。Odds应用体外试验比较各种咪唑类衍化物的抗菌作用,发现:克霉唑和益康唑对皮肤癣菌和曲菌作用最强,对酵母菌具中等作用;咪康唑和硫康唑对酵母菌作用最强,对其他真菌具中等作用;而酮康唑活力最小。Lefler和Stevens体外比较硫康唑,克霉唑,酮康唑,咪康唑和益康唑对11株白念珠菌的MIC(mg/L)分别为3.0,7.4,9.7,27.3和>100。
Since the first imidazole derivative, clotrimazole, was synthesized in 1967 and has been used clinically since 1970, new imidazole derivatives have been synthesized and are now widely used in clinic. In addition to clotrimazole, miconazole , Econazole, as well as the recent applications of ketoconazole and sulconazole, etc., for the treatment of fungal diseases has opened up a new way. Antibacterial activity Imidazole derivatives are broad-spectrum antifungal agents against dermatophytes, Candida, Cryptococcus neoformans and Coccidioides, Histoplasma capsulatum, Blastomyces dermatitidis, Pigmented fungi, Aspergillus Inhibit effect. In vitro Gram-positive bacteria also have vitality, which seems more obvious econazole. Odds In vitro tests comparing the antibacterial effect of various imidazole derivatives, found that: clotrimazole and econazole on dermatophytes and aspergillosis the strongest role in yeast with a moderate effect; miconazole and sulconazole pairs Yeast has the strongest effect and has moderate effects on other fungi; ketoconazole has the lowest activity. Lefler and Stevens compared the MICs (mg / L) of 3.0, 7.4, 9.7, 27.3, and> 100 for 11 C. albicans isolates of sulconazole, clotrimazole, ketoconazole, miconazole and econazole, respectively.