N-硫醇化β-内酰胺类药物抗真菌特性的研究。
Studies on the antifungal properties of N-thiolated beta-lactams.
作者信息
O'Driscoll Marci, Greenhalgh Kerriann, Young Ashley, Turos Edward, Dickey Sonja, Lim Daniel V
机构信息
Center for Molecular Diversity in Drug Design, Discovery, and Delivery, Department of Chemistry, 4202 East Fowler Avenue, CHE 205, University of South Florida, Tampa, FL 33620, USA.
出版信息
Bioorg Med Chem. 2008 Aug 15;16(16):7832-7. doi: 10.1016/j.bmc.2008.06.035. Epub 2008 Jun 25.
Abstract
N-thiolated beta-lactams had previously been shown to have antibacterial activity against a narrow selection of pathogenic bacteria including Staphylococcus aureus and Bacillus anthracis, as well as apoptotic-inducing activity in a variety of human cancer cell lines. We now have found that these lactams also possess antifungal activity against Candida and other fungi by exerting powerful cytostatic effects that disrupt the structural integrity of cytoplasmic membranes. The mode of action and structure-activity trends of these lactams as antifungals parallel that previously seen in our antibacterial studies.
摘要
N-硫醇化β-内酰胺此前已被证明对包括金黄色葡萄球菌和炭疽杆菌在内的少数几种病原菌具有抗菌活性，同时在多种人类癌细胞系中具有诱导凋亡的活性。我们现在发现，这些内酰胺类化合物还通过发挥强大的细胞生长抑制作用破坏细胞质膜的结构完整性，从而对念珠菌和其他真菌具有抗真菌活性。这些内酰胺类化合物作为抗真菌剂的作用方式和构效趋势与我们之前抗菌研究中观察到的情况相似。
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