Category: 321438-86-2

Young, Summer E. published the artcileSynthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets, SDS of cas: 321438-86-2, the main research area is proteinase activated receptor PAR4.

Protease activated receptor-4 [PAR4, proteinase-activated receptor PAR-4] is one of thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. The authors sought to develop potent, selective and novel PAR4 antagonists to test the role of PAR4 in thrombosis and hemostasis. The development of an expedient three-step synthetic route to access a novel series of indole-based PAR4 antagonists also necessitated the development of a platelet based high-throughput screening assay. Screening and subsequent structure activity relationship anal. yielded several selective PAR4 antagonists as well as possible new scaffolds for future antagonist development. The title compounds thus formed included an indole benzoic acid ester (I) and related substances. I was evaluated against an indazole benzoic acid ester analog (II) [i.e., 4-[1-(phenylmethyl)-1H-indazol-3-yl]benzoic acid Et ester]. The synthesis of the target compounds was achieved using 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole as starting materials. The synthetic sequence involved an alkylation of 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole, formation of bromide derivatives and a subsequent coupling reaction with boronic acids.

PLoS One published new progress about Allosterism. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, SDS of cas: 321438-86-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fontaine, Fanny published the artcileFirst identification of boronic species as novel potential inhibitors of the Staphylococcus aureus NorA efflux pump, COA of Formula: C6H8BNO2S, the main research area is boron compound transport protein NorA Staphylococcus.

Overexpression of efflux pumps is an important mechanism of bacterial resistance that results in the extrusion of antimicrobial agents outside the bacterial cell. Inhibition of such pumps appears to be a promising strategy that could restore the potency of existing antibiotics. The NorA efflux pump of Staphylococcus aureus confers resistance to a wide range of unrelated substrates, such as hydrophilic fluoroquinolones, leading to a multidrug-resistance phenotype. Here, 150 heterocyclic boronic species were evaluated for their activity against susceptible and resistant strains of S. aureus. Twenty-four hit compounds, although inactive when tested alone, were found to potentiate ciprofloxacin activity by a 4-fold increase at concentrations ranging from 0.5 to 8 μg/mL against S. aureus 1199B, which overexpresses NorA. Boron-free analogs showed no biol. activity, thus revealing that the boron atom is crucial for biol. activity. This work describes the first reported efflux pump inhibitory activity of boronic acid derivatives

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, COA of Formula: C6H8BNO2S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Guo, Xuelei published the artcileNickel-Catalyzed Suzuki-Miyaura Cross-Coupling Facilitated by a Weak Amine Base with Water as a Cosolvent, Quality Control of 321438-86-2, the main research area is nickel catalyst preparation Suzuki coupling reaction amine water cosolvent; aryl chloride Suzuki coupling aryl boronic acid water cosolvent; pharmaceutical substrate nickel catalyzed Suzuki cross coupling.

The development of a Ni-catalyzed Suzuki-Miyaura cross-coupling that uses a weak amine base and performs optimally with H2O as a cosolvent is reported. The aqueous amine base facilitates an equilibrium between the Ni oxidative addition complex and Ni μ-hydroxo dimers, enabling productive catalysis at low metal loadings (typically 1 mol %). A practical catalytic system is enabled using a com. available Ni oxidative addition complex as a precatalyst. The mild conditions allow high functional group tolerance and application to complex pharmaceutical substrates, one of which was demonstrated on a 50 g scale with a catalyst loading of 0.5 mol %.

Organometallics published new progress about Amines Role: RGT (Reagent), RACT (Reactant or Reagent) (weak). 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, Quality Control of 321438-86-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Perez-Pineiro, Rolando published the artcileSynthesis of sulfur-containing aryl and heteroaryl vinyls via Suzuki-Miyaura cross-coupling for the preparation of SERS-active polymers, Product Details of C6H8BNO2S, the main research area is sulfur aryl heteroaryl viny Suzuki coupling.

The preparation of sulfur-containing aryl and heteroaryl vinyl co-monomers via Suzuki-Miyaura cross-coupling between the corresponding mercaptomethyl arylboronates and in situ-generated vinyl bromides is described. Surface-enhanced Raman scattering (SERS) studies of the target compounds on gold nanoparticles confirmed their potential as spectroscopic tags in the fabrication of SERS-encoded polymers for combinatorial screening and biomedical diagnostics.

Tetrahedron Letters published new progress about Aryl alkenes Role: SPN (Synthetic Preparation), PREP (Preparation). 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, Product Details of C6H8BNO2S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem