Tag: M.W=150-200

March, J. G. published the artcileFluorimetric determination of phytic acid based on the activation of the oxidation of 2,2′-dipyridyl ketone hydrazone catalyzed by Cu(II), Product Details of C11H10N4, the publication is Analyst (Cambridge, United Kingdom) (1999), 124(6), 897-900, database is CAplus and MEDLINE.

Phytic acid exerts an activation effect on the oxidation of 2,2′-dipyridyl ketone hydrazone catalyzed by Cu(II) ion and the oxidation product is highly fluorescent. A fixed time method for the fluorometric determination of phytic acid based on this effect is described. The calibration graph is linear over the range 0.05-0.6 mg L^-1 phytic acid, resulting in a limit of detection of 0.03 mg L^-1 phytic acid. The relative standard deviation is in the range 1.4-1.8%, depending on the sample analyzed. The method was successfully applied to the determination of phytic acid in human urine (20 samples) and food samples (nine different products). The results obtained for urine samples ranged from 0.31 to 3.6 mg L^-1 phytic acid and for food samples from 3.8 to 22 mg g^-1 phytic acid. This is the 1st procedure to be reported for the determination of phytic acid based on fluorometric measurements.

Analyst (Cambridge, United Kingdom) published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, Product Details of C11H10N4.

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

Laha, Joydev K. published the artcileSynthesis of unsymmetrical urea from aryl- or pyridyl carboxamides and aminopyridines using PhI(OAc)₂via in situ formation of aryl- or pyridyl isocyanates, Name: 2-Bromopyridin-3-amine, the publication is New Journal of Chemistry (2021), 45(40), 18815-18823, database is CAplus.

A tandem synthesis of unsym. ureas (N-aryl-N’-pyridylurea and N,N’-bipyridylurea) from aryl- or pyridyl carboxamides and aminopyridines via Hofmann rearrangement has been reported. In particular, benzamides, picolinamide, nicotinamide, and isonicotinamide generate reactive intermediate isocyanates, in situ, in the presence of PhI(OAc)₂, which upon further reaction with aminopyridines form urea derivatives As the formation of pyridylisocyanates from their corresponding carboxamides via Hofmann rearrangement remained unexplored previously, attempts have been made to trap the isocyanates. While the three pyridylisocyanates were trapped as their corresponding carbamates, 3-pyridylisocyanate was isolated and characterized. Unlike closely related previous methods reported for urea synthesis, the current method avoids direct use of isocyanates or eliminates the use of toxic phosgene for the in situ generation of isocyanates.

New Journal of 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 C5H5BrN2, Name: 2-Bromopyridin-3-amine.

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

Mayer, Nicole published the artcileStructure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL), COA of Formula: C7H10BNO3, the publication is Bioorganic & Medicinal Chemistry (2020), 28(16), 115610, database is CAplus and MEDLINE.

High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alc. fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure-activity relationship (SAR) studies of small mol. inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.

Bioorganic & Medicinal Chemistry published new progress about 612845-44-0. 612845-44-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Boronic Acids,Boronic acid and ester, name is (6-Ethoxypyridin-3-yl)boronic acid, and the molecular formula is C7H10BNO3, COA of Formula: C7H10BNO3.

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

Jayakumar, K. published the artcileSpectral, thermal and DFT studies of novel nickel(II) complexes of 2-benzoylpyridine-N⁴-methyl-3- thiosemicarbazone: Crystal structure of a square planar azido-nickel(II) complex, COA of Formula: C12H9NO, the publication is Journal of Molecular Structure (2022), 132257, database is CAplus.

Novel six Ni(II) complexes of an NNS donor 2-benzoylpyridine-N⁴-methyl-3- thiosemicarbazone(HL) were synthesized and characterized. Various physicochem. techniques are applied for the study of the coordination behavior of the thiosemicarbazone to the nickel center. In all the complexes, thiosemicarbazone is coordinated in the thiolate form. A four coordinated Ni(II) complex [NiLN₃] is crystallized and its mol. and crystal structures are determined by single-crystal x-ray crystallog. Single-crystal XRD reveals that the complex got crystallized in the monoclinic space group P2₁/n and nickel(II) has a square planar environment. Intramol. hydrogen bonding interactions make the complex more rigid and in the crystal lattice, the intermol. hydrogen bonding interactions generate a supramol. 1 D chain. The chem. reactivity behavior of the HL and six Ni(II) complexes was evaluated with the CAM-B3LYP quantum chem. calculations The validity of electronic structure principles like Maximum Hardness, Min. Polarizability, and Min. Electrophilicity Principle in the study is discussed.

Journal of Molecular Structure 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, COA of Formula: C12H9NO.

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

Yoshida, Hiroto published the artcileDirect Suzuki-Miyaura Coupling with Naphthalene-1,8-diaminato (dan)-Substituted Organoborons, Safety of 5-Methyl-2-(p-tolyl)pyridine, the publication is ACS Catalysis (2020), 10(1), 346-351, database is CAplus.

The direct Suzuki-Miyaura coupling with “protected” R-B(dan) (dan = naphthalene-1,8-diaminato) (R = Ph, 4-MeOC₆H₄, 2-pyridyl) was demonstrated to smoothly occur without in situ deprotection of the B(dan) moiety. The use of KOt-Bu (Ba(OH)₂ in some cases) as a base under anhydrous conditions is the key to the successful cross-coupling, where R-B(dan) is readily converted into a transmetalation-active borate-form, regardless of the well-accepted diminished boron-Lewis acidity.

ACS Catalysis published new progress about 85237-71-4. 85237-71-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 5-Methyl-2-(p-tolyl)pyridine, and the molecular formula is C10H12BF3KNO2, Safety of 5-Methyl-2-(p-tolyl)pyridine.

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

Joshi, Abhisek published the artcileRu-Catalyzed Selective C-H Functionalization of Pyridotriazoles with Acrylates, Quality Control of 91-02-1, the publication is SynOpen (2021), 5(4), 294-300, database is CAplus.

Ruthenium-catalyzed efficient and selective C-H alkenylation of pyridotriazoles with acrylates is described. The combination of metals (Ru and Fe) plays a crucial role in achieving quant. yields of the desired products. The reaction is proposed to involve the formation of a ruthenium cyclometalated intermediate.

SynOpen 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, Quality Control of 91-02-1.

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

Mahajan, Dinesh published the artcileDiscovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3Kα and mTOR Kinases for the Treatment of Solid Tumors, Recommanded Product: (6-Amino-5-methylpyridin-3-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2020), 63(19), 11121-11130, database is CAplus and MEDLINE.

Herein, we report the identification and preclin. profile of a lead compound 10, (SPR519) as an equally potent dual inhibitor of PI3Kα and mTOR kinases. SPR519 exhibits an EC₅₀ of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23μM), PC3 (0.48μM), and SKOV3 (0.50μM). When administrated orally, it shows a considerably high plasma exposure (area under curve: 26,858 nM/h at 1 mg/kg) in mice. Moreover, it is found to be safe in animals with a dose of 30 mg/kg BID for 12 days in the dose tolerance study. SPR519 did not show any CYP or hERG liability. The identified lead compound demonstrates significant efficacy and bioavailability in ovarian and colon cancer xenograft models when evaluated for dose-ranging efficacy studies, at a dose as low as 2.5 mg/kg.

Journal of Medicinal Chemistry published new progress about 1032759-01-5. 1032759-01-5 belongs to pyridine-derivatives, auxiliary class Boronic acid and ester,Boronic acid and ester, name is (6-Amino-5-methylpyridin-3-yl)boronic acid, and the molecular formula is C6H9BN2O2, Recommanded Product: (6-Amino-5-methylpyridin-3-yl)boronic acid.

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

Frosini, Maria published the artcileInteractions of taurine and structurally related analogues with the GABAergic system and taurine binding sites of rabbit brain, Quality Control of 636-73-7, the publication is British Journal of Pharmacology (2003), 138(6), 1163-1171, database is CAplus and MEDLINE.

The aim of this study was to find taurinergic compounds that do not interact with brain GABAergic systems. Washed synaptic membranes (SM) from whole rabbit brain were able to bind [³H]muscimol. Saturation experiments of the binding of [³H]GABA to GABA_B receptors showed that SM possess two binding components; twice Triton X-100-treated SM contained 0.048 mmol endogenous taurine/kg protein and bound [³H]taurine in a saturable manner (K_d = 249.0 nM and B_max = 3.4 pmol mg^-1 prot). Among the 19 structural analogs of taurine, 6-aminomethyl-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide (TAG), 2-aminoethylarsonic (AEA), 2-hydroxyethanesulfonic (ISE) and (±)cis-2-aminocyclohexane sulfonic acids (CAHS) displaced [³H]taurine binding (K_i = 0.13, 0.13, 13.5 and 4.0 μM, resp.). These analogs did not interact with GABA_A and GABA_B receptors and did not affect taurine- and GABA-uptake systems and GABA-transaminase activity. 3-Aminopropanesulfonic acid (OMO), β-alanine, pyridine-3-sulfonic acid, N,N,N-trimethyltaurine (TMT), 2-(guanidino)ethanesulfonic acid (GES), ethanolamine-O-sulfate, N,N-dimethyltaurine (DMT), taurine and (±)piperidine-3-sulfonic acid (PSA) inhibited [³H]muscimol binding to GABA_A receptors with different affinities (K_i = 0.013, 7.9, 24.6, 47.5, 52.0, 91.0, 47.5, 118.1 and 166.3 μM, resp.). Taurine, 2-aminoethylphosphonic acid, DMT, TMT and OMO inhibited the binding of [³H]GABA to GABA_B receptors with K_i‘s in the μM range (0.8, 3.5, 4.4, 11.3 and 5.0, resp.). GES inhibited taurine uptake (IC₅₀ = 3.72 μM) and PSA GABA transaminase activity (IC₅₀ = 103.0 μM). In conclusion, AEA, TAG, ISE and CAHS fulfill the criteria for taurinergic agents.

British Journal of Pharmacology 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, Quality Control of 636-73-7.

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

Frosini, Maria published the artcileEffects of taurine and some structurally related analogues on the central mechanism of thermoregulation: A structure-activity relationship study, Product Details of C5H5NO3S, the publication is Advances in Experimental Medicine and Biology (2000), 273-282, database is CAplus and MEDLINE.

There is large body of evidences on the role of taurine in the central mechanisms of thermoregulation in mammals, but it is not clear, whether the hypothermic effect of taurine depends on its interaction with GABA receptors or with a specific receptor. In order to answer this question, the authors have performed a structure-activity relationship study by using both in vitro and in vivo preparations μM amounts of taurine or each of 20 analogs were injected intracerebroventricularly in conscious, restrained rabbits while rectal temperature was recorded. Receptor-binding studies, with synaptic membrane preparations from rabbit brain were used to determine the affinities of these compounds for GABA_A and GABA_B receptors. Furthermore, the interaction with presynaptic GABA and taurine uptake systems was studied using crude synaptosomal preparations from rabbit brain. Among the compounds tested, (±)-cis-2-aminocyclohexane sulfonic acid, induced hypothermia, but did not interact with GABA_A and GABA_B receptors neither did it affect GABA and taurine uptake, thus suggesting that its effect on body temperature is not mediated by the central GABA-ergic system. Interestingly, the trans-isomer was devoid of effects either in vivo or in vitro. In order to explain (±)-cis-2-aminocyclohexane sulfonic acid-induced hypothermia, a stereoscopic model was produced showing its possible interactions with a putative taurine brain receptor.

Advances in Experimental Medicine and Biology 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, Product Details of C5H5NO3S.

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

Emami, Marzieh published the artcileSynthesis, Study, and Application of Pd(II) Hydrazone Complexes as the Emissive Components of Single-Layer Light-Emitting Electrochemical Cells, Product Details of C12H9NO, the publication is Inorganic Chemistry (2021), 60(2), 982-994, database is CAplus and MEDLINE.

For the first time, square planar Pd(II) complexes of hydrazone ligands have been investigated as the emissive components of light-emitting electrochem. cells (LECs). The neutral transition metal complex, [Pd(L¹)₂]·2CH₃OH (1), (HL¹ = (E)-Nâ€?(phenyl(pyridin-2-yl)methylene)isonicotinhydrazide), was prepared and structurally characterized. Complex 1 displays quasireversible redox properties and is emissive at room temperature in solution with a λ_max of 590 nm. As a result, it was subsequently employed as the emissive material of a single-layer LEC with configuration FTO/1/Ga/In, where studies reveal that it has a yellow color with CIE(x, y) = (0.33, 0.55), a luminance of 134 cd cm^-2, and a turn-on voltage of 3.5 V. Protonation of the pendant pyridine nitrogen atoms of L¹ afforded a second ionic complex [Pd(L¹H)₂](ClO₄)₂ (2) which is also emissive at room temperature with a λ_max of 611 nm, resulting in an orange LEC with CIE(x, y) = (0.43, 0.53). The presence of mobile anions and cations in the second inorganic transition metal complex resulted in more efficient charge injection and transport which significantly improved the luminance and turn-on voltage of the device to 188.6 cd cm^-2 and 3 V, resp. This study establishes Pd(II) hydrazone complexes as a new class of materials whose emissive properties can be chem. tuned and provides proof-of-concept for their use in LECs, opening up exciting new avenues for potential applications in the field of solid state lighting. The emissive properties of two Pd(II) hydrazone complexes have been exploited for the fabrication of single-layer light-emitting electrochem. cells. We demonstrate that a neutral Pd(II) complex capable of undergoing proton transfer with the solvent can support a suitable ionic medium for LECs. Furthermore, selective protonation of the hydrazone ligands and the introduction of perchlorate counterions afford a second LEC device with increased c.d., a red-shifted emission, and significantly improved brightness.

Inorganic 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, Product Details of C12H9NO.

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