Design, synthesis and anti-HBV activity evaluation of new substituted imidazo[4,5-b]pyridines was written by Gerasi, Maria;Frakolaki, Efseveia;Papadakis, Georgios;Chalari, Anna;Lougiakis, Nikolaos;Marakos, Panagiotis;Pouli, Nicole;Vassilaki, Niki. And the article was included in Bioorganic Chemistry in 2020.Synthetic Route of C5H3Cl2N3O2 This article mentions the following:
The design and synthesis of a number of new imidazo[4,5-b]pyridines is described. The heterocyclic scaffold possesses 6-chloro- or 5,6-dichloro-substitution and bears various 2-alkylamino-Me or Et groups. The corresponding N1 and N3-tosylates are also presented. The anti-HBV activity of the compounds was evaluated in HBV infectious system at the level of HBV rcDNA secretion and CC50, EC50 and selectivity index values were determined The tosylates showed low antiviral potency and relatively high cytotoxicity, on the contrary, a number of 2,5 and/or-6-substituted imidazopyridines, mainly those belonging to the 6-chloroimidazo[4,5-b]pyridine series, were endowed with a very interesting profile and were further investigated. The most promising among them, along with the reduction of the secreted HBV rcDNA, also caused a reduction in HBV cccDNA and pgRNA levels, with a concomitant accumulation of the intracellular encapsidated rcDNA. Surprisingly, the most active 6-chloro-2-[2-(diethylamino)ethyl]imidazo[4,5-b]pyridine was highly competitive to interferon. In the experiment, the researchers used many compounds, for example, 5,6-Dichloro-3-nitropyridin-2-amine (cas: 203794-33-6Synthetic Route of C5H3Cl2N3O2).
5,6-Dichloro-3-nitropyridin-2-amine (cas: 203794-33-6) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Synthetic Route of C5H3Cl2N3O2