Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists was written by Miah, Afjal H.;Abas, Hossay;Begg, Malcolm;Marsh, Benjamin J.;O’Flynn, Daniel E.;Ford, Alison J.;Percy, Jonathan M.;Procopiou, Panayiotis A.;Richards, Steve A.;Rumley, Sally-Anne. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Safety of 2,6-Dibromo-3-hydroxypyridine This article mentions the following:
A knowledge-based library of 2,3-dichlorophenylsulfonyl derivatives of com. available aryl amines was synthesized and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimization program. Hits were required to be more potent than an existing indazole series, have better physicochem. properties (c log P <3.5, chromatog. log D7.4 <5.3 and CLND solubility >116 μg/mL), and be stable to acid and light. The benzimidazol-2-one core was identified as a hit suitable for further investigation. Substitution at N1 with small alkyl groups was tolerated; however, these analogs were inactive in the whole blood assay (pA2 <5). Azabenzimidazolone analogs were all found to be active, with compound I exhibiting whole blood activity of 6.1, low mol. weight (389) and chromatog. log D7.4 (2.4), high LE (0.43), and solubility (152 μg/mL). In addition, I had human serum albumin binding of around 93% and met all the criteria for progression to lead optimization. In the experiment, the researchers used many compounds, for example, 2,6-Dibromo-3-hydroxypyridine (cas: 6602-33-1Safety of 2,6-Dibromo-3-hydroxypyridine).
2,6-Dibromo-3-hydroxypyridine (cas: 6602-33-1) belongs to pyridine derivatives. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Halopyridines are particularly attractive synthetic building blocks in a variety of cross-coupling methods, including the Suzuki-Miyaura cross-coupling reaction.Safety of 2,6-Dibromo-3-hydroxypyridine