Electric Literature of C6H8N2On June 11, 2020, Wang, Chunting; Pei, Yameng; Wang, Lin; Li, Shuo; Jiang, Chao; Tan, Xu; Dong, Yi; Xiang, Ye; Ma, Yao; Liu, Gang published an article in Journal of Medicinal Chemistry. The article was 《Discovery of (1H-Pyrazolo[3,4-c]pyridin-5-yl)sulfonamide Analogues as Hepatitis B Virus Capsid Assembly Modulators by Conformation Constraint》. The article mentions the following:
Hepatitis B virus (HBV) capsid assembly modulators (CAMs) have been suggested to be effective anti-HBV agents in both preclin. and clin. studies. In addition to blocking HBV replication, CAMs could reduce the formation of covalently closed circular DNA (cccDNA), which accounts for the persistence of HBV infection. Here, we describe the discovery of (1H-indazole-5-yl)sulfonamides and (1H-pyrazolo[3,4-c]pyridin-5-yl)sulfonamides as new CAM chemotypes by constraining the conformation of the sulfamoylbenzamide derivatives Lead optimization resulted in compound 56 with an EC50 value of 0.034μM and good metabolic stability in mouse liver microsomes. To increase the solubility, the amino acid prodrug (65) and its citric acid salt (67) were prepared Compound 67 dose dependently inhibited HBV replication in a hydrodynamic injection-based mouse model of HBV infection, while 56 did not show in vivo anti-HBV activity, likely owing to its suboptimal solubility This class of compounds may serve as a starting point to develop novel anti-HBV drugs. In addition to this study using 4-Amino-2-picoline, there are many other studies that have used 4-Amino-2-picoline(cas: 18437-58-6Electric Literature of C6H8N2) was used in this study.
4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Electric Literature of C6H8N2