Category: 913835-63-9

Kim, Jina published the artcileIdentification of selective ERRγ inverse agonists, Product Details of C7H7BN2O2, the publication is Molecules (2016), 21(1), 80/1-80/16, database is CAplus and MEDLINE.

GSK5182 (4) is currently one of the lead compounds for the development of estrogen-related receptor gamma (ERR) inverse agonists. Here, we report the design, synthesis, pharmacol. and in vitro absorption, distribution, metabolism, excretion, toxicity (ADMET) properties of a series of compounds related to 4. Starting from 4, a series of analogs were structurally modified and their ERR inverse agonist activity was measured. A key pharmacophore feature of this novel class of ligands is the introduction of a heterocyclic group for A-ring substitution in the core scaffold. Among the tested compounds, several of them are potent ERR inverse agonists as determined by binding and functional assays. The most promising compound, 15g, had excellent binding selectivity over related subtypes (IC50 = 0.44, >10, >10, and 10 μM at the ERR, ERRγ, ERR∝, and ERβ subtypes, resp.). Compound 15g also resulted in 95% transcriptional repression at a concentration of 10 _M, while still maintaining an acceptable in vitro ADMET profile. This novel class of ERR inverse agonists shows promise in the development of drugs targeting ERR-related diseases.

Molecules published new progress about 913835-63-9. 913835-63-9 belongs to imidazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is Imidazo[1,2-a]pyridine-6-boronic acid, and the molecular formula is C7H7BN2O2, Product Details of C7H7BN2O2.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Li, Shasha published the artcileMerging Late-Stage Diversification with Solid-Phase Peptide Synthesis Enabled by High-Throughput On-Resin Reaction Screening, HPLC of Formula: 913835-63-9, the publication is ACS Catalysis (2022), 12(5), 3201-3210, database is CAplus.

An integrated workflow is described that combines micromole-scale high-throughput experimentation (HTE) reaction screening and solid-phase peptide synthesis (SPPS) to enable rapid synthetic method development for on-resin peptide diversification. Using this new approach, we have identified several sets of robust Suzuki-Miyaura coupling conditions with complementary scope that collectively display broad coverage with respect to both resin-bound peptide substrates containing aryl halide side chains and (hetero)arylboronic acid coupling partners. We have also demonstrated the utility of this integrated SPPS/chem. diversification method by synthesizing a multidimensional library of diverse peptides in high yields.

ACS Catalysis published new progress about 913835-63-9. 913835-63-9 belongs to imidazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is Imidazo[1,2-a]pyridine-6-boronic acid, and the molecular formula is C7H7BN2O2, HPLC of Formula: 913835-63-9.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Estiarte, M. Angels published the artcile2-Amino-5-arylbenzoxazole derivatives as potent inhibitors of fatty acid amide hydrolase (FAAH), Recommanded Product: Imidazo[1,2-a]pyridine-6-boronic acid, the publication is MedChemComm (2012), 3(5), 611-619, database is CAplus.

2,5-Disubstituted benzoxazole derivatives were evaluated for their ability to inhibit hFAAH. Structure-activity studies indicated that an isoindoline group at the 2-position of the benzoxazole ring gave rise to particularly potent inhibitors. Further refinement resulted in compounds, such as 50, with low nanomolar potencies against hFAAH. Preliminary biochem. experiments revealed that model benzoxazole FAAH inhibitors inhibited the enzyme in a manner consistent with a reversible mechanism. Addnl., the species dependency of FAAH inhibition was measured. Of the species tested, inhibition of rabbit FAAH, but not rat and guinea pig FAAH, appeared to show close alignment to human FAAH. These results may suggest similarities between the active sites of the FAAH enzyme for these two species, and may also suggest that rabbit could be a viable species with which to conduct preclin. testing with benzoxazole FAAH inhibitors.

MedChemComm published new progress about 913835-63-9. 913835-63-9 belongs to imidazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is Imidazo[1,2-a]pyridine-6-boronic acid, and the molecular formula is C7H7BN2O2, Recommanded Product: Imidazo[1,2-a]pyridine-6-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem