Category: 91678-81-8

Woll, Matthew G. published the artcileDiscovery and Optimization of Small Molecule Splicing Modifiers of Survival Motor Neuron 2 as a Treatment for Spinal Muscular Atrophy, Product Details of C6H9N3, the main research area is survival motor neuron SMN2 splicing modifier spinal muscle atrophy; piperazinylcoumarin preparation structure activity SMN2 splicing modifier muscle atrophy.

The underlying cause of spinal muscular atrophy (SMA) is a deficiency of the survival motor neuron (SMN) protein. Starting from hits identified in a high-throughput screening campaign and through structure-activity relationship investigations, we have developed small mols. that potently shift the alternative splicing of the SMN2 exon 7, resulting in increased production of the full-length SMN mRNA and protein. Three novel chem. series, represented by compounds 9, 14, and 20, have been optimized to increase the level of SMN protein by >50% in SMA patient-derived fibroblasts at concentrations of <160 nM. Daily administration of these compounds to severe SMA Δ7 mice results in an increased production of SMN protein in disease-relevant tissues and a significant increase in median survival time in a dose-dependent manner. Our work supports the development of an orally administered small mol. for the treatment of patients with SMA. Journal of Medicinal Chemistry published new progress about Drug discovery. 91678-81-8 belongs to class pyrazines, name is 3,5-Dimethylpyrazin-2-amine, and the molecular formula is C6H9N3, Product Details of C6H9N3.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Gajjar, Jinal A. published the artcileOcta-Substituted Resorcinarene Based Supramolecules and Its Liquid Crystalline and Biological Applications, Name: 3,5-Dimethylpyrazin-2-amine, the main research area is resorcinarene liquid crystalline thermal property antibacterial antioxidant.

Resorcin[4]arenes functionalized amide based supramol. derivatives (E1-E9) were produced in high yield using microwave irradiation (MWI) and characterized using spectroscopic techniques such as 1H-NMR, IR spectroscopy, and Mass spectrometry. Antimicrobial, anti-malarial, anti-tuberculosis, and anti-oxidant properties of amide-based supramol. hosts were investigated. The majority of the compounds showed exceptional antibacterial activity. Some compounds showed promising antifungal, antimalarial, antituberculosis, and antioxidant properties. Additions to this, few selected derivatives were further tested for their mesomorphic study with formation of columnar type self-assembly. The liquid crystalline properties were studied by using polarizing optical microscope (POM), differential scanning calorimetry (DSC) and further confirmed by PXRD techniques. All the synthesized supramols. showed good thermal properties with respect to liquid crystalline mesophase range.

ChemistrySelect published new progress about Antibacterial agents. 91678-81-8 belongs to class pyrazines, name is 3,5-Dimethylpyrazin-2-amine, and the molecular formula is C6H9N3, Name: 3,5-Dimethylpyrazin-2-amine.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Almansa, Carmen published the artcileSynthesis and SAR of a new series of COX-2-selective inhibitors: pyrazolo[1,5-a]pyrimidines, Formula: C6H9N3, the main research area is pyrazolopyrimidine preparation COX2 inhibitor; pyrimidine pyrazolo preparation COX2 inhibitor; structure activity pyrazolopyrimidine COX2 inhibitor.

The synthesis and pharmacol. activity of a series of bicyclic pyrazolo[1,5-a]pyrimidines, e.g., I (R1, R2, R3 = H, Me), as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema and air-pouch model). Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6,7-dimethyl-2-[4-(methylsulfonyl)phenyl]pyrazolo[1,5-a]pyrimidine I (R1 = H, R2 = R3 = Me) as one of the most potent and selective COX-2 inhibitors in this series.

Journal of Medicinal Chemistry published new progress about Nonsteroidal anti-inflammatory agents. 91678-81-8 belongs to class pyrazines, name is 3,5-Dimethylpyrazin-2-amine, and the molecular formula is C6H9N3, Formula: C6H9N3.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Wang, Jingxin published the artcileMechanistic studies of a small-molecule modulator of SMN2 splicing, Quality Control of 91678-81-8, the main research area is SMN2 gene splicing FUBP1 cloning sequence spinal muscular atrophy; SMNC2 SMNC3 drug synthesis RG7916 therapy SMA human; RG-7916; RNA binding; RNA splicing; chemical proteomics; spinal muscular atrophy.

RG-7916 is a first-in-class drug candidate for the treatment of spinal muscular atrophy (SMA) that functions by modulating pre-mRNA splicing of the SMN2 gene, resulting in a 2.5-fold increase in survival of motor neuron (SMN) protein level, a key protein lacking in SMA patients. RG-7916 is currently in three interventional phase 2 clin. trials for various types of SMA. In this report, we show that SMN-C2 and -C3, close analogs of RG-7916, act as selective RNA-binding ligands that modulate pre-mRNA splicing. Chem. proteomic and genomic techniques reveal that SMN-C2 directly binds to the AGGAAG motif on exon 7 of the SMN2 pre-mRNA, and promotes a conformational change in two to three unpaired nucleotides at the junction of intron 6 and exon 7 in both in vitro and in-cell models. This change creates a new functional binding surface that increases binding of the splicing modulators, far upstream element binding protein 1 (FUBP1) and its homolog, KH-type splicing regulatory protein (KHSRP), to the SMN-C2/C3-SMN2 pre-mRNA complex and enhances SMN2 splicing. These findings underscore the potential of small-mol. drugs to selectively bind RNA and modulate pre-mRNA splicing as an approach to the treatment of human disease.

Proceedings of the National Academy of Sciences of the United States of America published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (TSL1). 91678-81-8 belongs to class pyrazines, name is 3,5-Dimethylpyrazin-2-amine, and the molecular formula is C6H9N3, Quality Control of 91678-81-8.

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem