Abstract:
The ambigols are cyanobacterial natural products characterized by three polychlorinated aromatic building blocks connected by biaryl and biaryl ether bridges. All ambigols known to date possess promising biological activities. Most significantly, ambigol A was reported to have antibacterial activity against Gram-positive bacteria, such as Bacillus megaterium and B. subtilis. We established a diverse compound library for in-depth biological evaluation building on our previous bio- and total synthetic research on this natural product family. To explore the antimicrobial potential in detail and to determine initial structure-activity relationships of this product class, a large set of dimeric and trimeric compounds were screened against selected bacterial and Candida target strains. Our results reveal exceptional antibiotic activity of the ambigols, especially against challenging clinical isolates.
摘要:
双歧杆菌是蓝细菌的天然产物,其特征是通过联芳基和联芳基醚桥连接的三个多氯芳族结构单元。迄今为止已知的所有歧义都具有有希望的生物活性。最重要的是,据报道,BigogolA对革兰氏阳性细菌具有抗菌活性,如巨大芽孢杆菌和枯草芽孢杆菌。我们建立了一个多样化的化合物库,用于深入的生物评估,建立在我们之前对这个天然产品家族的生物和全合成研究的基础上。为了详细探索抗菌潜力,并确定该产品类别的初始结构-活性关系,针对选定的细菌和念珠菌靶菌株筛选了大量二聚体和三聚体化合物.我们的结果揭示了歧义的特殊抗生素活性,特别是针对具有挑战性的临床分离株。