Wang, Pingyuan published the artcileSynthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists, Product Details of C19H28BNO4, the publication is ACS Medicinal Chemistry Letters (2019), 10(5), 792-799, database is CAplus and MEDLINE.
Noncatechol heterocycles have recently been discovered as potent and selective G protein biased dopamine 1 receptor (D1R) agonists with superior pharmacokinetic properties. To determine the structure-activity relations centered on G protein or β-arrestin signaling bias, systematic medicinal chem. was employed around three aromatic pharmacophores of the lead compound PF2334, generating a series of new mols. that were evaluated at both D1R Gs-dependent cAMP signaling and β-arrestin recruitment in HEK293 cells. Here, the authors report the chem. synthesis, pharmacol. evaluation, and mol. docking studies leading to the identification of two novel noncatechol D1R agonists that are a subnanomolar potent unbiased ligand 6-(4-(Furo[3,2-c]pyridin-4-yloxy)-2-methylphenyl)-1,5-dimethylpyrimidine-2,4(1H,3H)dione (PW0441) and a nanomolar potent complete G protein biased ligand 6-(4-((3-(Difluoromethoxy)pyridin-2-yl)oxy)-2-methylphenyl)-1,5-dimethylpyrimidine-2,4(1H,3H)-dione (PW0464), resp. These novel D1R agonists provide important tools to study D1R activation and signaling bias in both health and disease.
ACS Medicinal Chemistry Letters published new progress about 837392-67-3. 837392-67-3 belongs to indole-building-block, auxiliary class Indoline,Boronic acid and ester,Amide,Boronate Esters,Aliphatic Heterocyclic, name is tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, and the molecular formula is C19H21N3O, Product Details of C19H28BNO4.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles