Department of Biomedical Science, University of Cagliari, 09042 Monserrato, Italy.
Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
Molecules. 2018 Oct 7;23(10):2554. doi: 10.3390/molecules23102554.
A series of 2-(1-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1-indol-3-yl)ethanamine with appropriate aryl/alkylisothiocyanates in anhydrous media. The structures of the newly synthesized compounds were confirmed by spectroscopic analysis and the molecular structures of and were confirmed by X-ray crystallography. All obtained compounds were tested for antimicrobial activity against Gram-positive cocci, Gram-negative rods and for antifungal activity. Microbiological evaluation was carried out over 20 standard strains and 30 hospital strains. Compound showed significant inhibition against Gram-positive cocci and had inhibitory effect on the topoisomerase IV decatenation activity and DNA gyrase supercoiling activity. Compounds were tested for cytotoxicity and antiviral activity against a large panel of DNA and RNA viruses, including HIV-1 and other several important human pathogens. Interestingly, derivative showed potent activity against HIV-1 wild type and variants bearing clinically relevant mutations. Newly synthesized tryptamine derivatives showed also a wide spectrum activity, proving to be active against positive- and negative-sense RNA viruses.
一系列 2-(1-吲哚-3-基)乙基硫脲衍生物是通过 2-(1-吲哚-3-基)乙胺与适当的芳基/烷基异硫氰酸酯在无水介质中缩合得到的。新合成化合物的结构通过光谱分析得到证实， 和 的分子结构通过 X 射线晶体学得到证实。所有获得的化合物都进行了抗革兰氏阳性球菌、革兰氏阴性杆菌的抗菌活性测试和抗真菌活性测试。微生物评估在 20 个标准菌株和 30 个医院菌株上进行。化合物 对革兰氏阳性球菌表现出显著的抑制作用，并且对拓扑异构酶 IV 解链活性和 DNA 回旋酶超螺旋活性具有抑制作用。这些化合物还针对包括 HIV-1 和其他几种重要人类病原体在内的一大组 DNA 和 RNA 病毒进行了细胞毒性和抗病毒活性测试。有趣的是，衍生物 对 HIV-1 野生型和具有临床相关突变的变体表现出很强的活性。新合成的色胺衍生物还表现出广谱活性，对正链和负链 RNA 病毒均有活性。
