New discoveries in chemical research and development in 2021. The transformation of simple hydrocarbons into more complex and valuable products has revolutionised modern synthetic chemistry. In an article, author is Imaizumi, Takamichi, once mentioned the application of 2343-89-7, SDS of cas: 2343-89-7, Name is Methyl 2-fluoroacrylate, molecular formula is C4H5FO2, molecular weight is 104.0797, category is benzoxazole. Now introduce a scientific discovery about this category.
We previously reported 2-aminobenzoxazole analogue 1 as a potent ChemR23 inhibitor. The compound showed inhibitory activity against chemerin-induced calcium signaling through ChemR23 internalization in CAL-1 cells, which are cell lines of plasmacytoid dendric cells (pDCs). Furthermore, compound 2 inhibited chemotaxis of CAL-1 triggered by chemerin in vitro. However, we noted a difference in the ChemR23 response to our inhibitor between rodents and non-rodents in a previous study. To address this issue, we performed optimization of ChemR23 inhibitors using CAL-1 cells endogenously expressing human ChemR23 and conducted a pharmacokinetics study in cynomolgus monkeys. Various substituents at the 4-position of the benzoxazole ring exhibited potent in vitro bioactivity, while those at the 6-position were not tolerated. Among substituents, a carboxyl group was identified as key for improving the oral bioavailability in cynomolgus monkeys. Compound 38a with the acidic part changed from a tetrazole group to a 1,2,4-oxadiazol-5-one group to improve bioactivity and pharmacokinetic parameters exhibited inhibitory activity against chemerin-induced chemotaxis in vitro. In addition, we confirmed the ChemR23 internalization of pDCs by compound 38a orally administered to cynomolgus monkeys. These 2-aminobenzoxazole-based ChemR23 inhibitors may be useful as novel immunotherapeutic agents capable of suppressing the migration of pDCs, which are known to be major producers of type I interferons in the lesion area of certain autoimmune diseases, such as systemic lupus erythematosus and psoriasis.
I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 2343-89-7 help many people in the next few years. SDS of cas: 2343-89-7.
Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem