Category: 22483-09-6

Heffernan, Michele L. R. published the artcileUlotaront: A TAAR1 Agonist for the Treatment of Schizophrenia, COA of Formula: C4H11NO2, the main research area is structure TAAR1 agonist ulotaront preparation schizophrenia.

Ulotaront (SEP-363856) is a trace-amine associated receptor 1 (TAAR1) agonist with 5-HT1A receptor agonist activity in Phase 3 clin. development, with FDA Breakthrough Therapy Designation, for the treatment of schizophrenia. TAAR1 is a G-protein-coupled receptor (GPCR) that is expressed in cortical, limbic, and midbrain monoaminergic regions. It is activated by endogenous trace amines, and is believed to play an important role in modulating dopaminergic, serotonergic, and glutamatergic circuitry. TAAR1 agonism data are reported herein for ulotaront and its analogs in comparison to endogenous TAAR1 agonists. In addition, a human TAAR1 homol. model was built around ulotaront to identify key interactions and attempt to better understand the scaffold-specific TAAR1 agonism structure-activity relationships.

ACS Medicinal Chemistry Letters published new progress about Antipsychotics. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hansen, Moritz E. published the artcileTotal synthesis of mutanobactins A, B from the human microbiome: Macrocyclization and thiazepanone assembly in a single step, Related Products of alcohols-buliding-blocks, the main research area is mutanobactin total synthesis human microbiome lipopeptide; aspartate substitution reduction Mutsunobu displacement phthalimide methanolysis cyclization; peptide coupling solid phase synthesis macrocyclization thiazepanone assembly; cyclization mechanism dehydration aldol addition; Cyclization; Macrocycles; Peptide Synthesis; Total Synthesis.

We report the first total syntheses of tricyclic mutanobactins A and B, lipopeptides incorporating a thiazepanone, isolated from Streptococcus mutans, a member of the human oral microbiome. A rapid, solid-phase peptide synthesis (SPPS) based route delivers these natural products from a cascade of cyclization reactions. This versatile process was also employed in a streamlined synthesis of mutanobactin D. Addnl., we provide an independent synthesis of a truncated mutanobactin A analog, utilizing a novel thiazepanone amino acid building block.

Angewandte Chemie, International Edition published new progress about Aldol addition. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Related Products of alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Newell, Grace E. published the artcilePreparation of a clickable monomer compatible with automated PNA synthesis, Category: alcohols-buliding-blocks, the main research area is peptide nucleic acid thymine monomer synthesis; reductive amination PNA monomer incorporation PNA Click chem.

A propargyl-containing Fmoc-protected (Fmoc = 9-fluorenylmethoxycarbonyl) thymine monomer was synthesized for possible use in the pre- or post-functionalization of PNA oligomers via Click chem. The monomer should be suitable for incorporation in normal automated solid phase PNA synthesis. The synthesis is suitable for the preparation of gram-quantities of monomers and uses reductive amination as the key step.

Tetrahedron Letters published new progress about Click chemistry. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Shad, Mastaneh Safarnejad published the artcileSynthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists, Application of 2,2-Dimethoxyethanamine, the main research area is isoquinoline synthesis CXCR antagonist antiHIV activity; CXCR4 antagonist; HIV; isoquinoline.

An expansion of the structure-activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and calcium mobilization assays, resp. In addition, the anti-HIV activity of all analogs was determined All compounds showed excellent activity, with compound 24c being the most promising one, since it displayed consistently low nanomolar activity in the various assays.

Molecules published new progress about Anti-HIV agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Application of 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Manolov, Stanimir P. published the artcileMicrowave-assisted synthesis of 1,2,3,4-tetrahydroisoquinoline sulfonamide derivatives and their biological evaluation, Computed Properties of 22483-09-6, the main research area is methylsulfonyl tetrahydroisoquinoline green preparation antioxidant antitryptic antibacterial lipophilicity antiinflammatory.

An alternative eco-friendly method for the synthesis of 2-(methylsulfonyl)-1,2,3,4-tetrahydroisoquinolines I [R = H, MeO; R1 = H, Ph, 3,4-di-MeOC6H3] was reported. All obtained compounds were screened for their in vitro inhibition of albumin denaturation, antioxidant, antitryptic and antibacterial activity, and havd shown significant results. The lipophilicity was established using both reversed-phase thin layer chromatog. and in silico calculations

Journal of the Serbian Chemical Society published new progress about Amidoalkylation. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Computed Properties of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Pichon, Maeva M. published the artcileTight-binding inhibition of jack bean α-mannosidase by glycoimidazole clusters, Quality Control of 22483-09-6, the main research area is tight binding jack bean mannosidase glycoimidazole cluster inhibition.

The best multivalent effects observed in glycosidase inhibition have been achieved so far with jack bean α-mannosidase (JBα-man) using iminosugar clusters based on weakly binding mismatching active-site-directed inhibiting epitopes (inhitopes) in the D-gluco series. Here, we synthesize and evaluate as JBα-man inhibitors a series of mono- to 14-valent glycoimidazoles with inhitopes displaying inhibition values up to the range of hundreds of nMs to study the impact of inhitope affinity on the multivalent effect. The most potent inhibitor of the series, a 14-valent mannoimidazole derivative, inhibits JBα-man with a nanomolar Ki value (2 ± 0.5 nM) and binding enhancements observed are, at best, relatively small (up to 25-fold on a valency-corrected basis). The results of this study support the fact that JBα-man-inhitope affinity and the strength of the inhibitory multivalent effect evolve in the opposite direction. The major impact of the glycoimidazole-based inhitope is found on the binding scenario; most of the synthesized mannoimidazole clusters as well as a 14-valent glucoimidazole derivative prove to be tight binding inhibitors of JBα-man.

Organic & Biomolecular Chemistry published new progress about Canavalia. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Quality Control of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zhang, Hong published the artcileCytotoxicity and degradation product identification of thermally treated ceftiofur, Name: 2,2-Dimethoxyethanamine, the main research area is ceftiofur cytotoxicity thermal treatment cell proliferation.

Ceftiofur (CEF) is a cephalosporin antibiotic and is a commonly used drug in animal food production As a heat-labile compound, the residual CEF toxicity after thermal treatment has rarely been reported. This study was to investigate the potential toxicity of thermally treated CEF and determine the toxic components. By cytotoxicity tests and liquid chromatog.-mass spectrometry (LC-MS) assays, the cytotoxicity of the thermally treated CEF (TTC) and the components of TTC was identified, resp. Our results showed that TTC exhibited significantly increased toxicity compared with CEF towards LO2 cells by inducing apoptosis. Through LC-MS assays, we identified that the toxic compound of TTC was CEF-aldehyde (CEF-1). The IC50 value of CEF-1 on LO2 cells treated for 24 h was 573.1μg mL-1, approx. 5.3 times lower than CEF (3052.0μg mL-1) and 3.4 times lower than TTC (1967.0μg mL-1). Moreover, we found that CEF-1 was also present in thermally treated desfuroylceftiofur (DFC), the primary metabolite of CEF, indicating that residual CEF or DFC could produce CEF-1 during the heating process. These findings suggest that CEF-1 is a newly identified toxic compound, and CEF-1 may pose a potential threat to food safety or public health.

RSC Advances published new progress about Apoptosis. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Name: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

He, Nianzhe published the artcileDiscovery of selective Mcl-1 inhibitors via structure-based design and structure-activity relationship analysis, Product Details of C4H11NO2, the main research area is cervical cancer Mcl1 Bcl2 anticancer apoptosis structure activity relationship; Apoptosis; Cancer; Mcl-1; Protein–protein interaction.

Based on Nap-1, a Mcl-1/Bcl-2 dual inhibitor reported by our group, we carried out a structure-guided mol. design and structure-activity relationship (SAR) anal. to study structural features contributing to Mcl-1 binding selectivity and affinity. A series of derivatives of Nap-1 with various pharmacophores were synthesized and among them a dual Mcl-1/Bcl-2 inhibitor A4 with enhanced affinities (IC50 = 0.15 μM for Mcl-1, 0.43 μM for Bcl-2) and a selective Mcl-1 inhibitor B9 with a 20-fold selectivity over Bcl-2 (IC50 = 0.51 μM vs 9.46 μM) were obtained by enzyme linked immunosorbent assay (ELISA). The SAR data and binding modes of A4 and B9 investigated by 2D-NMR derived docking study illustrated that p2 pockets exhibiting different geometry and binding features between Mcl-1 and Bcl-2 contribute to specific binding properties of Mcl-1. In addition, apoptosis-inducing potencies of A4 and B9 were consistent with their binding selectivity determined in vitro.

Biochemical and Biophysical Research Communications published new progress about Apoptosis. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Product Details of C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Gerdt, Philipp published the artcileAlternating Terpolymers through Cyclopolymerization and Subsequent Orthogonal Functionalization, Quality Control of 22483-09-6, the main research area is alternating terpolymer cyclopolymn orthogonal functionalization; Alternating Polymerization; Orthogonal Functionalization; Postmodification; RAFT Polymerization; Radical Polymerization.

A method for the synthesis of functionalized alternating copolymers by reversible deactivation radical polymerization was developed. Copolymerization by reversible addition-fragmentation chain transfer of hexenyl vinyl ether with a novel fluorinated divinyl monomer yields alternating cyclopolymers that can be chemoselectively modified by three distinct orthogonal functionalization reactions. Along the thiol-ene click reaction and amidation, a third functionalization was achieved via NHC-catalyzed transesterification or acylation resulting in a small library of ABC-type alternating terpolymers.

Angewandte Chemie, International Edition published new progress about Acylation. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Quality Control of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Howells, Rachel L. published the artcileSynthesis of Novel Pyrazine-Substituted-1H-Pyrrole-2-carboxamides and Related Tethered Heterocycles, Name: 2,2-Dimethoxyethanamine, the main research area is pyrazinyl pyrrole carboxamide preparation; fused bicyclic compound preparation.

The synthesis of a 4-(pyrazin-2-yl)-1H-pyrrole-2-carboxamide I and several fused bicyclic analogs, e.g., II all using standard procedures (SNAr, borylation, C-C cross couplings, hydrolysis, amide bond formation, cyclization, halogenation, and alkylation) from readily available starting materials is reported. The synthetic sequences range from 4-12 steps per final compound, with yields of isolated intermediates ranging from 20 to �00%.

Synthesis published new progress about Alkylation. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Name: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts