Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 40400-13-3, is researched, Molecular C7H6BrI, about Syntheses and evaluation of daphnetin derivatives as novel G protein-coupled receptor inhibitors and activators, the main research direction is chromenone preparation GPCR inhibitor activator human SAR; anhydride daphnetin acylation; daphnetin benzyl or alkyl bromide alkylation; dihydroxy chromenone preparation GPCR inhibitor activator human SAR; pyrogallol ester pechmann condensation; Daphnetin derivatives; G protein-coupled receptors; Structure-activity relationships; Synthesis.Name: 1-(Bromomethyl)-2-iodobenzene.
A series of daphnetin (7,8-dihydroxycoumarin) derivatives I [R = C(O)Et, Et, (2-iodophenyl)methyl, etc.; R1 = H, Me, CF3, MeO; R2 = H, Cl, Me, C≡N, Bn, m-tolylmethyl] were synthesized including some new and some known compounds I. Their pharmacol. activities on G protein-coupled receptors (GPCRs) were evaluated by double antibody sandwich ELISA (DAS-ELISA) in vitro. Daphnetin derivatives I [R = C(O)Et, Et, (2-iodophenyl)methyl, etc.; R1 = H; R2 = H] with various substitution patterns/groups were obtained from inhibitors to activators on GPCRs. Derivatives I [R = C(O)Et, C(O)(CH2)2CH3, C(O)(CH2)3CH3, C(O)(CH2)4CH3, n-Pr; R1 = H, Me, CF3, MeO; R2 = H, Cl, Bn] possessed moderate activation potency on GPCRs. Among them, derivatives I [R = C(O)(CH2)2CH3, C(O)(CH2)3CH3, C(O)(CH2)4CH3; R1 = H, Me, CF3; R2 = H, Cl] presented significant activation potency on GPCRs with EC50 values in the range of 1.18-1.91 nM. Derivatives I [R = Me, (2-chlorophenyl)methyl, o-tolylmethyl; R1 = H, Me; R2 = H, Bn] showed significant inhibitory potency on GPCRs with IC50 values in the range of 1.26-1.38 nM. Moreover, the structure-activity relationships (SARs) of daphnetin derivatives I were discussed in detail. The new daphnetic-based GPCRs activators and inhibitors had potentials as future drug candidates for the treatment of metabolic diseases.
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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