Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis was written by Ko, Kwangseok;Kim, Hye-Jung;Ho, Pil-Su;Lee, Soon Ok;Lee, Ji-Eun;Min, Cho-Rong;Kim, Yu Chul;Yoon, Ju-Han;Park, Eun-Jung;Kwon, Young-Jin;Yun, Jee-Hun;Yoon, Dong-Oh;Kim, Jung-Sook;Park, Woul-Seong;Oh, Seung-Su;Song, Yu-Mi;Cho, Woon-Ki;Morikawa, Kazumi;Lee, Kyoung-June;Park, Chan-Hee. And the article was included in Journal of Medicinal Chemistry in 2018.Application In Synthesis of 5,6-Dichloro-3-nitropyridin-2-amine This article mentions the following:
The histamine H4 receptor (H4R), a member of the G-protein coupled receptor family, has been considered as a potential therapeutic target for treating atopic dermatitis (AD). A large number of H4R antagonists have been disclosed, but no efficient agents controlling both pruritus and inflammation in AD have been developed yet. Here, we have discovered a novel class of orally available H4R antagonists showing strong anti-itching and anti-inflammation activity as well as excellent selectivity against off-targets. A pharmacophore-based virtual screening system constructed in house successfully identified initial hit compound 9, and the subsequent homol. model-guided optimization efficiently led us to discover pyrido[2,3-e]tetrazolo[1,5-a]pyrazine analog 48 as a novel chemotype of a potent and highly selective H4R antagonist. Importantly, orally administered compound 48 exhibits remarkable efficacy on antipruritus and anti-inflammation with a favorable pharmacokinetic (PK) profile in several mouse models of AD. Thus, these data strongly suggest that our compound 48 is a promising clin. candidate for treatment of AD. In the experiment, the researchers used many compounds, for example, 5,6-Dichloro-3-nitropyridin-2-amine (cas: 203794-33-6Application In Synthesis of 5,6-Dichloro-3-nitropyridin-2-amine).
5,6-Dichloro-3-nitropyridin-2-amine (cas: 203794-33-6) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Application In Synthesis of 5,6-Dichloro-3-nitropyridin-2-amine