硫代碳酰肼和碳酰肼衍生物作为潜在生物活性剂的合成。
Synthesis of thiocarbohydrazide and carbohydrazide derivatives as possible biologically active agents.
作者信息
Gangarapu Kiran, Manda Sarangapani, Jallapally Anvesh, Thota Sreekanth, Karki Subhas S, Balzarini Jan, De Clercq Erik, Tokuda Harukuni
机构信息
Department of Pharmaceutical Chemistry, Kakatiya Institute of Pharmaceutical Sciences, Pembarthy (V), Hasanparthy (M), Warangal, 506 371 AP India.
2Center for Pharmaceutical Sciences, IST, JNTU, Kukatpally, Hyderabad, 500085 India.
出版信息
Med Chem Res. 2014;23(2):1046-1056. doi: 10.1007/s00044-013-0684-3. Epub 2013 Aug 23.
ABSTRACT
A series of new β-isatin aldehyde-,'-thiocarbohydrazone, bis-β-isatin thiocarbohydrazones, bis-β-isatin carbohydrazones was synthesized by condensation of 5-substituted isatin with thiocarbohydrazide or carbohydrazide. The chemical structures of the newly synthesized compounds were confirmed by FT-IR, H NMR, and mass spectral analysis. The synthesized compounds were evaluated for in vitro antiviral activity against various strains of DNA and RNA viruses, but exhibited moderate antiviral activity compared with the reference compounds. Among all the compounds exhibited the highest chemoprevention activity in a two-stage mouse-skin carcinogenesis test.
摘要
通过5-取代异吲哚酮与硫代碳酰肼或碳酰肼缩合，合成了一系列新型β-异吲哚酮醛'-硫代碳酰腙、双-β-异吲哚酮硫代碳酰腙、双-β-异吲哚酮碳酰腙。通过傅里叶变换红外光谱（FT-IR）、核磁共振氢谱（H NMR）和质谱分析确定了新合成化合物的化学结构。对合成的化合物进行了针对各种DNA和RNA病毒株的体外抗病毒活性评估，但与参考化合物相比，其抗病毒活性中等。在所有化合物中，[此处原文缺失具体化合物信息]在两阶段小鼠皮肤致癌试验中表现出最高的化学预防活性。
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