STRUCTURE-ACTIVITY RELATIONSHIP OF 5,6-DIHYDRO-TETRAZOLO[1,5-c]QUINAZOLINES TARGETING CANDIDA GLABRATA

Lyudmyla Antypenko, O. Antypenko, Inna Vasilieva, Valentyna P. Kozyrieva
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Abstract

Candida species cause both disseminated and superficial fungal infections in humans. Although azole antifungals have historically proven effective in treating such infections, recent epidemiological studies highlight a crucial concern in the clinical context. Some Candida species exhibit inherent resistance to azoles and echinocandins, and the emergence of high-level resistance poses a significant problem. Consequently, derivatives of 5,6-dihydrotetrazolo[1,5-c]quinazolines have shown potent inhibitory properties against C. glabrata at concentrations range of 0.4 – 55.0 μM, leading to the identification of a structure-activity relationship.
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5,6-DIHYDRO-TETRAZOLO[1,5-c]QUINAZOLINES TARGETING CANDIDA GLABRATA 的结构-活性关系
念珠菌既可引起人类播散性真菌感染,也可引起表皮真菌感染。尽管唑类抗真菌药历来被证明对治疗此类感染有效,但最近的流行病学研究突出了临床中的一个重要问题。某些念珠菌对唑类和棘白菌素具有固有抗药性,高水平抗药性的出现构成了一个重大问题。因此,5,6-二氢四唑并[1,5-c]喹唑啉类衍生物在 0.4 - 55.0 μM 的浓度范围内显示出对光滑念珠菌的强效抑制特性,从而确定了一种结构-活性关系。
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