Day: October 21, 2022

Zhou, Xin-Yue; Zhang, Ming; Liu, Zhong; He, Jia-Hao; Wang, Xiao-Chen published the artcile< C3-Selective Trifluoromethylthiolation and Difluoromethylthiolation of Pyridines and Pyridine Drugs via Dihydropyridine Intermediates>, Related Products of 93-60-7, the main research area is trifluoromethylthiopyridine preparation one pot regioselective; pyridine trifluoromethylthiolation difluoromethylthiolation hydroboration oxidative aromatization; difluoromethylthiopyridine preparation regioselective one pot.

Herein, authors report a method for unprecedented C3-selective C-H tri- and difluoromethylthiolation of pyridines. The method relies on borane-catalyzed pyridine hydroboration for generation of nucleophilic dihydropyridines; these intermediates react with trifluoromethylthio and difluoromethylthio electrophiles to form functionalized dihydropyridines, which then undergo oxidative aromatization. The method can be used for late-stage functionalization of pyridine drugs for the generation of new drug candidates.

Journal of the American Chemical Society published new progress about Aromatization. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Related Products of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hu, Ziwei; Banothu, Janardhan; Beesu, Mallesh; Gustafson, Collin J.; Brush, Michael J. H.; Trautman, Kathryn L.; Salyer, Alex C. D.; Pathakumari, Balaji; David, Sunil A. published the artcile< Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides>, Formula: C7H7F3N2, the main research area is dihydropyridine quinolone carboxamide synthesis SAR TLR2 vaccine adjuvant.

Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-N-(pyridin-3-ylmethyl)-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxamide as a TLR2 agonist. Preliminary structure-activity relationship studies on the carboxamide moiety led to the identification of analogs that induce chemokines and cytokines in a TLR2-dependent manner. These results represent new leads for the development of vaccine adjuvants.

ACS Medicinal Chemistry Letters published new progress about Chemokines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 387350-39-2 belongs to class pyridine-derivatives, and the molecular formula is C7H7F3N2, Formula: C7H7F3N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lamani, Devappa S.; Badiger, Srikant G.; Singh, Mamata published the artcile< Formation of diaryl sulfides and sulfoxides: Synthesis, characterization and structure activity correlation studies>, Related Products of 3731-53-1, the main research area is diarylsulfide preparation glutathione peroxidase mimetic activity; diarylsulfoxide preparation glutathione peroxidase mimetic activity.

The synthesis of a series of diarylsulfides I [R = C(Me)2CH2OH, 3-pyridyl, 4-MeOC6H4CH2, etc.; X= S] was achieved by reaction of 2,2′-thiobis[benzoyl chloride] with amines followed by the presence of H2O2/t-BuOOH to afford corresponding sulfoxides II [X= S=O]. All the newly synthesized compounds were characterized by 1H, 13C NMR and mass spectroscopic techniques. A detailed mechanistic study indicated that the formation of sulfoxides followed oxidation In addition to synthesis, characterization and mechanistic studies, the glutathione peroxidase(GPx) mimetic activity of the newly synthesized compounds was described. It was observed that the diaryl sulfides having a heterocyclic ring attached to the nitrogen atom facilitated the oxidation of the sulfur center to form the corresponding sulfoxides. The substituents attached to the nitrogen atom played an important role in the catalytic activity of substituted diaryl sulfides. The obtained data supported for the higher antioxidant activity of diaryl sulfides than that of the corresponding sulfoxides.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Related Products of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Filla, Sandra A.; Mathes, Brian M.; Johnson, Kirk W.; Phebus, Lee A.; Cohen, Marlene L.; Nelson, David L.; Zgombick, John M.; Erickson, Jon A.; Schenck, Kathryn W.; Wainscott, David B.; Branchek, Theresa A.; Schaus, John M. published the artcile< Novel Potent 5-HT1F Receptor Agonists: Structure-Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides>, Formula: C6H7N3O2, the main research area is pyrrolopyridine amido sulfonamido preparation 5HT receptor agonist migraine; pyrrolopyrimidine amido preparation 5HT receptor agonist migraine.

5-Amidoindole I [X = Y = CH, R = 4-FC6H4; (II)] (LY334370), a selective 5-HT1F receptor agonist (SSOFRA), inhibited dural inflammation in the neurogenic plasma protein extravasation model of migraine and demonstrated clin. efficacy for the acute treatment of migraine. Although II was greater than 100-fold selective over both the 5-HT1B and 5-HT1D receptors, it exhibited appreciable 5-HT1A receptor affinity. Thus, a series of pyrrolo[2,3-c]pyridines I (X = N; Y = CH; R = Me, 4-FC6H4) and pyrrolo[3,2-b]pyridines I (X = CH; Y = N; R = Me, Et, Ph, 3-thienyl, 2-furyl, 2-pyridyl, cyclopropyl, etc.) as well as pyrrolo[3,2-d]pyrimidines I (X = Y = N; R = Me, 4-FC6H4) were synthesized as analogs of II and evaluated in an effort to identify SSOFRAs with improved selectivity over other 5-HT1 receptor subtypes. I (X = CH, Y = N, R = 4-FC6H4) showed high 5-HT1F receptor affinity but offered no improvement in selectivity compared to II; however, I (X = CH, Y = N, R = Me) was greater than 100-fold selective over the 5-HT1A, 5-HT1B, and 5-HT1D receptors. SAR studies of this series determined that alkylamides in particular exhibited high selectivity for the 5-HT1F receptor. These SAR studies identified SSOFRAs that demonstrated oral activity in the neurogenic plasma protein extravasation model, a model indicative of antimigraine activity.

Journal of Medicinal Chemistry published new progress about 5-HT1 agonists. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Formula: C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Aboonajmi, Jasem; Panahi, Farhad; Hosseini, Mina Aali; Aberi, Mahdi; Sharghi, Hashem published the artcile< Iodine-catalyzed synthesis of benzoxazoles using catechols, ammonium acetate, and alkenes/alkynes/ketones via C-C and C-O bond cleavage>, Reference of 350-03-8, the main research area is phenylbenzooxazole preparation; alkene catechol ammonium acetate coupling iodine catalyst; alkyne catechol ammonium acetate coupling iodine catalyst; ketone catechol ammonium acetate coupling iodine catalyst.

An efficient metal-free synthesis strategy of phenylbenzo[d]oxazoles of formula I [R1 = 4-OMe, 5,7-di-tert-bu, 5,7-di-tert-butyl-4-Me, etc.; R2 = Ph, 4-BrC6H4, 4-FC6H4, etc.] was developed via coupling of catechols, ammonium acetate, and alkenes/alkynes/ketones using mol. iodine as the catalyst. The developed methodol. represents an operationally simple, one-pot and large-scale procedure for the preparation of benzoxazole derivatives using mol. iodine as the catalyst.

RSC Advances published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Reference of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Canakci, Mine; Singh, Khushboo; Munkhbat, Oyuntuya; Shanthalingam, Sudarvili; Mitra, Ankita; Gordon, Mallory; Osborne, Barbara A.; Thayumanavan, S. published the artcile< Targeting CD4+ Cells with Anti-CD4 Conjugated Mertansine-Loaded Nanogels>, Related Products of 2127-03-9, the main research area is tumor antitumor T cell antibody CD4 mertansine.

CD4+ T lymphocytes play an important role in controlling many malignancies. The modulation of CD4+ T cells through immunomodulatory or cytotoxic drugs could change the course of disease progression for disorders such as autoimmunity, immunodeficiency, and cancer. Here, we demonstrate that anti-CD4 conjugated polymeric nanogels can deliver a small mol. cargo to primary CD4+ T cells and a CD4high T cell lymphoma. The antibody conjugation not only increased the uptake efficiency of the nanogel (NG) by CD4+ T cells but also decreased the non-specific uptake of the NG by CD4- lymphocytes. For T lymphoma cell lines, the mertansine-loaded conjugate displayed a dose-dependent cell growth inhibition at 17 ng/mL antibody concentration On the other hand, antibody-drug conjugate (ADC)-type formulation of the anti-CD4 reached similar levels of cell growth inhibition only at the significantly higher concentration of 1.8μg/mL. NG and antibody conjugates have the advantage of carrying a large payload to a defined target in a more efficient manner as it needs far less antibody to achieve a similar outcome.

Biomacromolecules published new progress about Antibodies and Immunoglobulins Role: BPN (Biosynthetic Preparation), PAC (Pharmacological Activity), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses) (mertansine-polymer conjugates). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Related Products of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gupta, Shivangi; Maji, Ankur; Panja, Dibyajyoti; Halder, Mita; Kundu, Sabuj published the artcile< CuO NPs catalyzed synthesis of quinolines, pyridines, and pyrroles via dehydrogenative coupling strategy>, Recommanded Product: 1-(Pyridin-3-yl)ethanone, the main research area is hydroxymethyl aniline ketone copper nanocatalyst oxidative coupling reaction; quinoline preparation; hydroxypropanamine ketone copper nanocatalyst oxidative coupling reaction; pyridine preparation; hydroxyethanamine ketone copper nanocatalyst oxidative coupling reaction; pyrrole preparation.

Copper oxide nanoparticles catalyzed efficient synthesis of quinolines, pyridines, and pyrroles via alc. dehydrogenative coupling strategy are reported. Employing this catalytic system, various functionalized quinolines, pyridines, and pyrroles were synthesized efficiently from different amino alcs. with a diverse range of ketones. A number of control experiments were performed to shed light on the mechanism. This catalyst was recycled up to 6th run and notably, no significant loss was observed in its catalytic activity.

Journal of Catalysis published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Recommanded Product: 1-(Pyridin-3-yl)ethanone.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bej, Somnath; Nandi, Mandira; Ghosh, Pradyut published the artcile< Development of fluorophoric [2]pseudorotaxanes and [2]rotaxane: selective sensing of Zn(II)>, Name: 2,2′-Bipyridine, the main research area is .

Fluorophoric [2]pseudorotaxanes {NiPR1(ClO4)2-NiPR3(ClO4)2} are synthesized by utilizing newly designed fluorophoric bidentate ligands (L1-L3) and a heteroditopic naphthalene containing macrocycle (NaphMC) with high yields via Ni(II) templation and π-π stacking interactions. Subsequently, a fluorophoric [2]rotaxane (NAPRTX) is established through a Cu(I) catalyzed click reaction between an azide terminated pseudorotaxane, {NiPR4(ClO4)2}, which contains the newly designed fluorophoric ligand L4, and alkyne terminated bulky stopper units. All these fluorophoric [2]pseudorotaxanes and the [2]rotaxane were characterized using numerous techniques such as mass spectrometry, NMR, UV/Vis, PL, and elemental anal., wherever applicable. Furthermore, to investigate the effect of the fluorophoric moieties, the coordinating ability of chelating units, and size and shape of the three dimensional cavity generated by the mech. bond in the interlocked [2]rotaxane (NAPRTX), we have performed a sensing study of various metal ions. Thus, the interlocked [2]rotaxane is found to have potential as a selective fluorescent sensor for Zn(II) metal ions over other transition, alkali and alk. earth metal ions, where the 2,2′-bipyridyl arylvinylene moiety of the axle acts as a fluorescence signalling unit.

Organic & Biomolecular Chemistry published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Name: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Haemmerle, Michael; Le, Minh Hien; Hekmat, Omid published the artcile< GC-FID-based quantification of the sum of the three forms of vitamin B3 from animal liver>, Reference of 93-60-7, the main research area is gas chromatog flame ionization detector vitamin B3 liver; Flame ionization detection; Gas chromatography; Nicotinamide; Nicotinamide adenine dinucleotide; Nicotinic acid; Vitamin B(3).

Vitamin B3 (nicotinic acid, nicotinamide) is an essential water-soluble vitamin and cellular energy metabolism depends on the vitamin B3-derived cofactors. Inaccessible covalently-linked nicotinic acid in food such as maize can cause vitamin B3 deficiency in animals since maize is also deficient in tryptophan, the precursor of nicotinic acid. A sensitive and reproducible GC-FID-based method for the quantification of the sum of the three forms of vitamin B3 from animal liver was developed. Free nicotinic acid, free nicotinamide and nicotinamide moiety of NAD+/NADP+ (and their riboside precursors) were simultaneously derivatized as Me nicotinate. Reaction time and temperature and the extraction procedure for Me nicotinate were optimized. Starting from wild boar liver, removal of proteins, solvent exchange, derivatization, and chloroform extraction resulted in sufficient enrichment and baseline separation of Me nicotinate. The within-laboratory reproducibility of the full procedure was determined with relative standard deviation <10%. On-column limit of detection and lower limit of quantification for Me nicotinate were both sub-picomole. The accuracy of the method was determined from the recoveries of the pre-extraction spiked-in vitamin B3 standards The overall recovery for the full procedure was 16% but very consistent (relative standard deviation = 7%), enabling determination of apparent vitamin B3 concentrations for relative quant. comparison. Analytical Biochemistry published new progress about Esterification (methyl-). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Reference of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Simmons, Bryan J.; Hoffmann, Marie; Champagne, Pier Alexandre; Picazo, Elias; Yamakawa, Katsuya; Morrill, Lucas A.; Houk, K. N.; Garg, Neil K. published the artcile< Understanding and Interrupting the Fischer Azaindolization Reaction>, Reference of 832735-54-3, the main research area is Fischer Azaindolization Reaction mechanism.

Exptl. and computational studies pertaining to the Fischer azaindolization reaction are reported. These studies explain why pyridylhydrazines are poorly reactive in Fischer indolization reactions, in addition to the origin of hydrazine substituent effects. Addnl., an interrupted variant of Fischer azaindolization methodol. is disclosed, which provides a synthetic entryway into fused azaindoline scaffolds.

Journal of the American Chemical Society published new progress about Fischer indole synthesis. 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, Reference of 832735-54-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem