Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, 44121 Ferrara, Italy.
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, 44121 Ferrara, Italy.
Molecules. 2020 Sep 21;25(18):4324. doi: 10.3390/molecules25184324.
In the search for scaffolds for multifunctional compounds we investigated the structure activity relationship of a class of benzimidazole derivatives bearing 5-membered ring. The newly synthesized and the already known compounds were divided into three classes that present different substituent at 5 position of the benzimidazole ring (-H, -COOH or -SOH) and different heterocycle at position 2 (thiophene, furan or pyrrole). All the derivatives were synthesized and tested to determine their photoprotective profile against UV rays, in vitro antioxidant capacity against different radicals (DPPH and FRAP test), antifungal inhibitory activity (dermatophytes and ), antiviral and antiproliferative activity. A Structure-Activity Relationship study indicated compound , bearing a pyrrole heterocycle on the benzimidazole ring, as the best multifunctional derivative of the series and as potential candidate for the development of drugs especially in case of melanoma.
在寻找多功能化合物的支架过程中，我们研究了一类含有 5 元环的苯并咪唑衍生物的结构活性关系。新合成的和已知的化合物被分为三组，它们在苯并咪唑环的 5 位具有不同的取代基（-H、-COOH 或 -SOH），在 2 位具有不同的杂环（噻吩、呋喃或吡咯）。所有的衍生物都被合成并测试了它们对紫外线的光保护特性，体外对不同自由基（DPPH 和 FRAP 测试）的抗氧化能力，抗真菌抑制活性（皮肤真菌和），抗病毒和抗增殖活性。结构-活性关系研究表明，苯并咪唑环上带有吡咯杂环的化合物 ，是该系列中最好的多功能衍生物，也是开发药物的潜在候选物，特别是在黑色素瘤的情况下。
