Departamento de Química, Universidade Estadual do Centro-Oeste , Guarapuava , Brazil.
Departamento de Química, Instituto Federal Mato Grosso do Sul-Campus de Nova Andradina, Fazenda Santa Bárbara , Nova Andradina , Brazil.
Nat Prod Res. 2019 Dec;33(23):3372-3377. doi: 10.1080/14786419.2018.1478829. Epub 2018 May 24.
In this work the aim of study was the synthesis and evaluation of anti- activity as well as the cytotoxicity in VERO cells of a series of 17 novel thiosemicarbazones derived from the natural monoterpene (-)-camphene by REMA and MTT methods. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of HRv, especially the derivatives , , , , , and . MIC values of 20 tested compounds ranged from 3.9 to > 250 μg/mL. It was found that when inserting new nitrogenous groups to the (-)-camphene increased the anti- activity of some compounds. The SI was calculated for all compounds that showed highly potent anti- activity and the best SI values were 21.36, 26.92 and 31.62 (, and ), and may be considered potential candidates for future antituberculosis drugs.
本工作的研究目的是通过 REMA 和 MTT 方法合成和评估一系列新型的 17 种源自天然单萜 (-)-莰烯的硫代缩氨基脲的抗活性和对 VERO 细胞的细胞毒性。总的来说，大多数测试化合物对 HRv 的生长表现出相当大的抑制作用，特别是衍生物 、 、 、 、 、 。20 种测试化合物的 MIC 值范围为 3.9 至 > 250 μg/mL。结果发现，当向 (-)-莰烯中插入新的含氮基团时，会提高一些化合物的抗活性。对所有表现出高效抗活性的化合物进行了 SI 计算，最佳 SI 值分别为 21.36、26.92 和 31.62（、和），它们可能被视为未来抗结核药物的潜在候选药物。
