SDS of cas: 40400-13-3. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-(Bromomethyl)-2-iodobenzene, is researched, Molecular C7H6BrI, CAS is 40400-13-3, about 4,8-Dimethylcoumarin Inhibitors of Intestinal Anion Exchanger slc26a3 (Downregulated in Adenoma) for Anti-Absorptive Therapy of Constipation. Author is Lee, Sujin; Cil, Onur; Haggie, Peter M.; Verkman, Alan S..
The chloride/bicarbonate exchanger SLC26A3 (down-regulated in adenoma, DRA) is expressed mainly in colonic epithelium where it dehydrates the stool by facilitating the final step of chloride and fluid absorption. SLC26A3 inhibition has predicted efficacy in various types of constipation including that associated with cystic fibrosis. We previously identified, by high-throughput screening, 4,8-dimethylcoumarin inhibitors of murine slc26a3 with IC50 down to ∼150 nM. Here, we synthesized a focused library of forty-three 4,8-dimethylcoumarin analogs. Structure-activity studies revealed the requirement of 4,8-dimethylcoumarin-3-acetic acid for activity. The most potent inhibitors were produced by replacements at C7, including 3-iodo- (4az(I)) and 3-trifluoromethyl- (4be(II)), with IC50 of 40 nM and 25 nM, resp. Pharmacokinetics in mice showed predicted therapeutic concentrations of I for >72 h following a single 10 mg/kg oral dose. I at 10 mg/kg fully normalized stool water content in a loperamide-induced mouse model of constipation. The favorable inhibition potency, selectivity within the SLC26 family and pharmacol. properties of I support its further preclin. development.
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Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate