Tag: M.W=150-200

Wang, Lei published the artcileElectrochemical Reduction of Aldehydes and Ketones for the Synthesis of Alcohols and Diols under Ambient Conditions, Safety of Phenyl(pyridin-2-yl)methanone, the publication is Synlett (2022), 33(13), 1302-1308, database is CAplus.

A sustainable, practical, and direct strategy for the reduction of carbonyl compounds, including aldehydes and ketones, by an electrochem. pathway is presented, affording a variety of alcs. or diols as major products with decent yields. The reaction proceeds smoothly in the air at ambient temperatures with DABCO as the sacrificial reductant. Mechanistic studies revealed that direct electrochem. reduction followed by either protonation or radical-radical homocoupling is the main pathway.

Synlett published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C14H26O2, Safety of Phenyl(pyridin-2-yl)methanone.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zhao, Bing published the artcileDiscovery of thiosemicarbazone derivatives as effective New Delhi metallo-β-lactamase-1 (NDM-1) inhibitors against NDM-1 producing clinical isolates, Formula: C12H9NO, the publication is Acta Pharmaceutica Sinica B (2021), 11(1), 203-221, database is CAplus and MEDLINE.

In this study, structure-activity relationship based on thiosemicarbazone derivatives (E)-R¹C(S)NHN=C(R²)(R³) (I) (R¹ = phenylamino, Ph, cyclohexylamino, morpholin-4-yl, etc.; R² = H, Me; R³ = Ph, pyridin-2-yl, 3,4,5-trimethoxyphenyl, etc.) was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds (I).HCl [R¹ = piperazin-1-yl, R² = H, R³ = 2-hydroxyphenyl (II); R¹ = 4-methylpiperazin-1-yl, R² = H, R³ = 2-hydroxyphenyl (III)] exhibited excellent activity against 10 NDM-pos. isolate clin. isolates in reversing MEM resistance. Further studies demonstrated that compounds II and III were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44μmol/L, resp. Mol. docking speculated that compounds II and III were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities were found even at concentrations of 1000 mg/mL against red blood cells. In vivo exptl. results showed that a combination of MEM and compound III was markedly effective in treating infections caused by NDM-1 pos. strain and prolonging the survival time of sepsis mice. The finding showed that compound III might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug.

Acta Pharmaceutica Sinica B published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C4H3Cl2N3, Formula: C12H9NO.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Li, Zhibin published the artcileSelective electrochemical oxidation of aromatic hydrocarbons and preparation of mono/multi-carbonyl compounds, Recommanded Product: Phenyl(pyridin-2-yl)methanone, the publication is Science China: Chemistry (2021), 64(12), 2134-2141, database is CAplus.

A selective electrochem. oxidation was developed under mild condition. Various mono-carbonyl and multi-carbonyl compounds can be prepared from different aromatic hydrocarbons with moderate to excellent yield and selectivity by virtue of this electrochem. oxidation The produced carbonyl compounds can be further transformed into α-ketoamides, homoallylic alcs. and oximes in a one-pot reaction. In particular, a series of α-ketoamides were prepared in a one-pot continuous electrolysis. Mechanistic studies showed that 2,2,2-trifluoroethan-1-ol (TFE) can interact with catalyst species and generate the corresponding hydrogen-bonding complex to enhance the electrochem. oxidation performance.

Science China: Chemistry published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C12H9NO, Recommanded Product: Phenyl(pyridin-2-yl)methanone.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yang, Limin published the artcileLow-frequency vibrational modes of DL-homocysteic acid and related compounds, Synthetic Route of 636-73-7, the publication is Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy (2009), 73A(5), 884-891, database is CAplus and MEDLINE.

Several polycrystalline mols. with sulfonate groups and some of their metal complexes, including DL-homocysteic acid (DLH) and its Sr- and Cu-complexes, pyridine-3-sulfonic acid and its Co- and Ni-complexes, sulfanilic acid and -cysteic acid were studied using THz time-domain methods at room temperature The results of THz absorption spectra show that the mols. have characteristic bands at 0.2-2.7 THz (6-90 cm^-1). THz technique can be used to distinguish different mols. with sulfonate groups and to determine the bonding of metal ions and the changes of H bond networks. In the THz region DLH has three bands: 1.61, 1.93 and 2.02 THz; and 0.85, 1.23 and 1.73 THz for Sr-DLH complex, 1.94 THz for Cu-DLH complex, resp. The absorption bands of pyridine-3-sulfonic acid are located at 0.81, 1.66 and 2.34 THz; the bands at 0.96, 1.70 and 2.38 THz for its Co-complex, 0.76, 1.26 and 1.87 THz for its Ni-complex. Sulfanilic acid has three bands: 0.97, 1.46 and 2.05 THz; and the absorption bands of -cysteic acid are at 0.82, 1.62, 1.87 and 2.07 THz, resp. The THz absorption spectra after complexation are different from the ligands, which indicate the bonding of metal ions and the changes of H bond networks. M-O and other vibrations appear in the FIR region for those metal-ligand complexes. The bands in the THz region were assigned to the rocking, torsion, rotation, wagging and other modes of different groups in the mols. Preliminary assignments of the bands were carried out using Gaussian program calculation

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C11H21BF4N2O2, Synthetic Route of 636-73-7.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wang, Yaxin published the artcileTunable System for Electrochemical Reduction of Ketones and Phthalimides, Application of Phenyl(pyridin-2-yl)methanone, the publication is Chinese Journal of Chemistry (2021), 39(12), 3297-3302, database is CAplus.

An efficient, tunable system for electrochem. reduction of ketones R¹C(O)R² (R¹ = Ph, pyridin-2-yl, 4-chlorophenyl, etc.; R² = H, t-Bu, thiophen-2-yl, 3-bromophenyl, etc.) and phthalimides I (R³ = prop-2-en-1-yl, phenoxymethyl, Bn, etc.) at room temperature without the need for stoichiometric external reductants was reported. By utilizing NaN₃ as the electrolyte and graphite felt as both the cathode and the anode, it was able to selectively reduce the carbonyl groups of the substrates to alcs. R¹C(OH)R², pinacols (R¹C(OH)R²)₂, or methylene groups e.g., 13-chloro-4-azatricyclo[9.4.0.0 (3,8)]pentadeca-1(11),3,5,7,12,14-hexaene by judiciously choosing the solvent and an acidic additive. The reaction conditions were compatible with a diverse array of functional groups, and phthalimides I could undergo one-pot reductive cyclization to afford products with indolizidine scaffolds e.g., 10-azatetracyclo[8.7.0.0(2,7).0(12,17)]heptadeca-2,4,6,12(17),13,15-hexaen-11-one. Mechanistic studies showed that the reactions involved electron, proton, and hydrogen atom transfers. Importantly, an N₃/HN₃ cycle operated as a hydrogen atom shuttle, which was critical for reduction of the carbonyl groups to methylene groups e.g., 13-chloro-4-azatricyclo[9.4.0.0 (3,8)]pentadeca-1(11),3,5,7,12,14-hexaene.

Chinese Journal of Chemistry published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C9H13NO2, Application of Phenyl(pyridin-2-yl)methanone.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zeng, Kui published the artcileAnomeric Stereoauxiliary Cleavage of the C-N Bond of D-Glucosamine for the Preparation of Imidazo[1,5-a]pyridines, Category: pyridine-derivatives, the publication is Chemistry – A European Journal (2022), 28(29), e202200648, database is CAplus and MEDLINE.

An anomeric stereoauxiliary approach for the synthesis of a wide range of imidazo[1,5-a]pyridines I (R¹ = Me, 2-methylphenyl, pyridin-2-yl, etc.; R² = 4-methoxyphenyl, naphthalen-1-yl, thiophen-2-yl, etc.) after cleaving the C-N bond of D-glucosamine (α-2° amine) from biobased resources was reported . This new approach expands the scope of readily accessible imidazo[1,5-a]pyridines I relative to existing state-of-the-art methods. A key strategic advantage of this approach is that the α-anomer of D-glucosamine enables C-N bond cleavage via a seven-membered ring transition state. By using this novel method, a series of imidazo[1,5-a]pyridine derivatives (>80 examples) was synthesized from 2-acylpyridines (including para-dipyridine ketone) and aldehydes (including para-dialdehyde) R²CHO. Imidazo[1,5-a]pyridine I derivatives containing diverse important deuterated C(sp²)-H and C(sp³)-H bonds were also efficiently achieved.

Chemistry – A European Journal published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C15H10O2, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wu, Jing-wei published the artcileSynthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout, Formula: C5H5BrN2, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(3), 383-388, database is CAplus and MEDLINE.

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC₅₀ value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

Bioorganic & Medicinal Chemistry Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C12H10FeO4, Formula: C5H5BrN2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zhu, Heping published the artcileDiscovery of novel 2-aryl-3-sulfonamido-pyridines (HoAns) as microtubule polymerization inhibitors with potent antitumor activities, Related Products of pyridine-derivatives, the publication is European Journal of Medicinal Chemistry (2021), 113117, database is CAplus and MEDLINE.

In this study, a series of novel 2-aryl-3-sulfonamido-pyridines had been designed, synthesized, and evaluated for their antiproliferative activities in vitro and in vivo. Among them, compound I exhibited the most potent activity with IC₅₀ values ranging from 0.170 to 1.193μM in a panel of cancer cell lines. Mechanistic studies indicated that compound I bound to the colchicine site of β-tubulin, resulting in colony formation inhibition, G2/M phase cell cycle arrest, cell apoptosis as well as increased the generation of ROS in both RKO and SW620 cells. In addition, compound I showed potent anti-vascular activity in vitro. Furthermore, compound I also exhibited outstanding antitumor activity in SW620 xenograft tumor models without observable toxic effects, which was more potent than that of ABT-751. In conclusion, these findings suggest that compound I may be a promising microtubule destabilizing agent and deserves for further development in cancer therapy.

European Journal of Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C9H7F3O3, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yamada, Mamoru published the artcileMicrobial conversion of 5-sulfoisophthalic acid into 5-hydroxyisophthalic acid by Ochrobactrum anthropi S9, Related Products of pyridine-derivatives, the publication is Biotechnology Letters (2010), 32(3), 445-450, database is CAplus and MEDLINE.

5-Hydroxyisophthalic acid-producing microorganisms were isolated from enrichment cultures using 5-sulfoisophthalic acid as a sulfur source. One bacterium, Ochrobactrum anthropi S9, had the highest 5-sulfoisophthalic acid-degrading activity, and stoichiometrically formed 5-hydroxyisophthalic acid, a raw material for polymer synthesis. Under optimum culture conditions, 1.3 mM 5-hydroxyisophthalic acid accumulated in the medium by 60 h. The addition of Na₂SO₄, l-methionine or l-cysteine at 2 mM inhibited the conversion of 5-sulfoisophthalic acid. O. anthropi S9 cells converted 5-sulfoisophthalic acid, benzenesulfonic acid, 3-sulfobenzoic acid, 4-aminobenzenesulfonic acid, naphthalene-1-sulfonic acid and naphthalene-2-sulfonic acid into the corresponding hydroxylated compounds

Biotechnology Letters published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C16H12O, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Owa, Takashi published the artcileSynthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents, Formula: C5H5NO3S, the publication is Bioorganic & Medicinal Chemistry Letters (2002), 12(16), 2097-2100, database is CAplus and MEDLINE.

The synthesis and antitumor activity of E7070 analogs containing a 3-pyridinesulfonamide moiety is reported. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clin. trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogs examined, ER-35745 (I), a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice.

Bioorganic & Medicinal Chemistry Letters published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Formula: C5H5NO3S.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem