Liu Yuxiu

Anti-TMV and Insecticidal Potential of Four Iridoid Glycosides from Gardenia Jasminoides Fruit

——————————— *Corresponding authors. Email: liling@jxas.ac.cn; wangqm@nankai.edu.cn Received June 13, 2018; accepted July 9, 2018. Supported by the National Natural Science Foundation of China(Nos.21562023, 21561014) and the Key Research Project of Jiangxi Province, China(No.20171BBF60074).

Synthesis of tetrahydro-β-carboline-3-carbohydrazide derivatives based on Pictet-Spengler reaction and their bioactivities

According to our previous research on the antiviral activity of β-carboline and tetrahydro-β-carboline derivatives, series of novel tetrahydro-β-carboline derivatives containing acylhydrazone moiety and different substituents at 1 position were designed, synthesized via Pictet-Spengler reaction, and evaluated for their biological activities. Most of these compounds exhibited excellent antiviral activity both in vitro and in vivo . The in vivo inactivation, curative, and protection activities of part of these compounds were much higher than that of ribavirin (36.5%, 35.2%, and 37.1% at 500 μg/mL) and harmine (40.5%, 38.6% and 42.4% at 500 μg/mL). Especially, the in vivo activities of compounds VI-1 (61.4%, 57.2%, and 68.1%) and compound VI-2 (74.5%, 69.0%, and 68.1%) at 500 μg/mL, which were nearly twofold of that of ribavirin at 500 μg/mL. At the same time, the fungicidal results showed that compound IV-2 exhibited more than 60% fungicidal activities against 5 kinds of phytopathogens. Additionally, compound IV-5 exhibited more than 60% larvicidal activity against C. pipiens pallens at 0.25 mg/kg.

Reduction of pyrimidine derivatives by LiAlH4

The reduction of ethyl 2-methylthio-(or 2-ethoxy)pyrimidine-5-carboxylate by LiAlH4 afforded ethyl 2-methylthio-(or 2-ethoxy)-1,6-dihydropyrimidine-5-carboxylate as the main product. Similarly, the reduction of 2-methylthio-(or 2-methoxy)pyrimidine-5-carboxamide by LiAlH4 gave 2-methylthio-(or 2-methoxy)-1,6-dihydropyrimidine-5-carbonitrile as main product.