Electric Literature of 284028-89-3, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 284028-89-3, Name is XAV-939, SMILES is O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1, belongs to indole-building-block compound. In a article, author is Wu, Yong-Jin, introduce new discover of the category.
Discovery of new indole-based acylsulfonamide Na(v)1.7 inhibitors
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Na(v)1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led to the identification of 4 analogs with hNa(v)1.7 IC50 values under 50 nM. Fluorine substitution of the truncated compound 12 led to 34 with improved potency and isoform selectivity. The inverted indole 36 also maintained good activity. Both 34 and 36 exhibited favorable CYP inhibition profiles, good membrane permeability and a low efflux ratio and, therefore, represent new leads in the search for potent and selective Na(v)1.7 inhibitors to treat pain.
Electric Literature of 284028-89-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 284028-89-3 is helpful to your research.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles