- 期刊
Structure Modification and Biological Activity of Some Griseofulvin Derivatives
合成Griseofulvin類似物之構造與活性相關研究
摘要
Griseofulvin 是一種口服有效的抗黴菌類抗生素，但其水溶性極差：為了探討griseofulvin構造之改變與抗黴菌活性及水溶性之影響，本研究合成了五種griseofulvin類似物。抗黴菌活性的評估是以Tricophyton mentagrophytes, T. rubrum, T. terrestre和Mircosporum canis等菌來檢測；其結果顯示griseofulvin的oxime修飾物是測試的五種化合物中最有效者，但其活性相當或略小於griseofulvin。這些結構修飾物與原化合物相較，對水的溶解性有所增加乃其優鐺，但其抗黴菌活性則不利地被降低。
關鍵字
無資料並列摘要
Griseofulvin is an orally acting anti-fungal antibiotic with very limited water solubility. Five chemical modifications were made on the griseofulvin structure in order to evasluate these changes on the antifungal and water solubility properties. Antifungal activity was measured against Tricophyton mentagrophytes, T. rubrum, T. terrestre, and Microsporum canis. The oxime of griseofulvin was the most potent of the five compounds tested, but it was only of equal or less potency than griseofulvin. The somewhat increased water solubility of some of these compounds was offset by the lower anti-fungal potency of the structural modification.