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Design, synthesis and antimicrobial activity of usnic acid derivatives
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-04-11 00:00:00 , DOI: 10.1039/c8md00076j Kartsev Victor 1 , Lichitsky Boris 2 , Geronikaki Athina 3 , Petrou Anthi 3 , Smiljkovic Marija 4 , Kostic Marina 4 , Radanovic Oliver 5 , Soković Marina 4
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-04-11 00:00:00 , DOI: 10.1039/c8md00076j Kartsev Victor 1 , Lichitsky Boris 2 , Geronikaki Athina 3 , Petrou Anthi 3 , Smiljkovic Marija 4 , Kostic Marina 4 , Radanovic Oliver 5 , Soković Marina 4
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Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting properties. Thus, the goal of this paper is the design of new usnic acid derivatives and evaluation of their antimicrobial activity. All newly synthesized compounds possess good antibacterial activity with MIC ranging from 1.02–50.93 × 10−2 mmol mL−1 and MBC from 2.05–70.57 × 10−2 mmol mL−1. The most sensitive bacterial species was Staphylococcus aureus, while Pseudomonas aeruginosa and Escherichia coli were the most resistant among the ATCC strains, and MRSA was the most resistant among all tested bacteria (ATCC and clinical isolates). Their antifungal activity was very strong (MIC = 0.35–7.53 × 10−2 mmol mL−1 and MFC = 0.70–15.05 × 10−2 mmol mL−1) – better than those of reference compounds and usnic acid itself. The most sensitive fungal species was Trichoderma viride, while Penicillium versicolor var. cyclopium appeared to be the most resistant. It should be mentioned that in general most of the compounds showed weaker antibacterial activity, but better antifungal properties than usnic acid itself. The results allow us to conclude that the title compounds are good lead compounds for novel more active antibacterial drugs. On the other hand, these compounds are very promising as antifungals.
中文翻译：
松萝酸衍生物的设计、合成及其抗菌活性
松萝酸是一种二苯并呋喃，最初是从产生次生代谢产物的地衣中分离出来的，作为一种抗生素而闻名，但还具有其他一些有趣的特性。因此，本文的目的是设计新的松萝酸衍生物并评估其抗菌活性。所有新合成的化合物均具有良好的抗菌活性，MIC范围为1.02–50.93 × 10 -2 mmol mL -1 ，MBC范围为2.05–70.57 × 10 -2 mmol mL -1 。最敏感的细菌种类是金黄色葡萄球菌，而铜绿假单胞菌和大肠杆菌是 ATCC 菌株中耐药性最强的，MRSA 是所有测试细菌（ATCC 和临床分离株）中耐药性最强的。它们的抗真菌活性非常强（MIC = 0.35–7.53 × 10 -2 mmol mL -1和 MFC = 0.70–15.05 × 10 -2 mmol mL -1 ）——优于参考化合物和松萝酸本身。最敏感的真菌物种是绿色木霉，而杂色青霉变种。 cyclopium似乎是最具抵抗力的。应该指出的是，一般来说，大多数化合物的抗菌活性较弱，但抗真菌性能优于松萝酸本身。结果使我们得出结论，标题化合物是新型活性更强的抗菌药物的良好先导化合物。 另一方面，这些化合物作为抗真菌剂非常有前途。
更新日期：2018-04-11
中文翻译：
松萝酸衍生物的设计、合成及其抗菌活性
松萝酸是一种二苯并呋喃，最初是从产生次生代谢产物的地衣中分离出来的，作为一种抗生素而闻名，但还具有其他一些有趣的特性。因此，本文的目的是设计新的松萝酸衍生物并评估其抗菌活性。所有新合成的化合物均具有良好的抗菌活性，MIC范围为1.02–50.93 × 10 -2 mmol mL -1 ，MBC范围为2.05–70.57 × 10 -2 mmol mL -1 。最敏感的细菌种类是金黄色葡萄球菌，而铜绿假单胞菌和大肠杆菌是 ATCC 菌株中耐药性最强的，MRSA 是所有测试细菌（ATCC 和临床分离株）中耐药性最强的。它们的抗真菌活性非常强（MIC = 0.35–7.53 × 10 -2 mmol mL -1和 MFC = 0.70–15.05 × 10 -2 mmol mL -1 ）——优于参考化合物和松萝酸本身。最敏感的真菌物种是绿色木霉，而杂色青霉变种。 cyclopium似乎是最具抵抗力的。应该指出的是，一般来说，大多数化合物的抗菌活性较弱，但抗真菌性能优于松萝酸本身。结果使我们得出结论，标题化合物是新型活性更强的抗菌药物的良好先导化合物。 另一方面，这些化合物作为抗真菌剂非常有前途。
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