Category: pyridine-derivatives

Macedo, Cicero Andre Ferreira published the artcileLippia origanoides essential oil induces tocolytic effect in virgin rat uterus and inhibits writhing in a dysmenorrhea mouse model, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Ethnopharmacology (2022), 115099, database is CAplus and MEDLINE.

The species Lippia origanoides Kunth, popularly known as “salva-de-marajo”, is used in Brazilian traditional “quilombola” communities to treat menstrual cramps and uterine inflammation. Evaluate the spasmolytic activity of Lippia origanoides essential oil (LOO) on exptl. models of uterine conditions related to menstrual cramps and investigate its mechanism of action. Virgin rat-isolated uterus was mounted in the organ bath apparatus to evaluate the spasmolytic effect of LOO on basal tonus and contractions induced by carbachol, KCl, or oxytocin. We used pharmacol. agents to verify the relaxation mechanism of LOO. The evaluation of uterine contractility in virgin rats, after treatment with LOO for three consecutive days, was carried out by the construction of a concentration-response curve with oxytocin or carbachol. The primary dysmenorrhea animal model was replicated with an injection of estradiol cypionate in female mice for three consecutive days, followed by i.p. application of oxytocin. LOO relaxed the rat uterus precontracted with 10-2 IU/mL oxytocin (logEC50 = 1.98 ± 0.07), 1μM carbachol (logEC50 = 1.42 ± 0.07) or 60 mM KCl (logEC50 = 1.53 ± 0.05). It was also able relax uterus on spontaneous contractions (logEC50 = 0.41 ± 0.05). Preincubation with glibenclamide, propranolol, phentolamine or L-NAME in contractions induced by carbachol did not alter significantly the relaxing effect of LOO. However, in the presence of 4-aminopyridine, CsCl or tetraethylammonium there was a reduction of LOO potency, whereas the blockers methylene blue, ODQ, aminophylline and heparin potentiated the LOO relaxing effect. Preincubation with LOO in a Ca2+ free medium at concentrations of 27μg/mL or 81μg/mL reduced the contraction induced by carbachol. The administration of LOO for 3 days did not alter uterus contractility. The treatment with LOO at 30 or 100 mg/kg i.p., or 100 mg/kg orally, inhibited writhing in female mice. The association of LOO at 10 mg/kg with nifedipine or mefenamic acid potentiated writhing inhibition in mice.The essential oil of L. origanoides has tocolytic activity in rat isolated uterus pre-contracted with KCl, oxytocin, or carbachol. This effect is possibly related to the opening of potassium channels (Kir, KV, and KCa), cAMP increase, and diminution of intracellular Ca2+. This relaxant effect, probably, contributed to reduce the number of writhings in an animal model of dysmenorrhea being potentiated by nifedipine or mefenamic acid. Taken together, the results here presented indicate that this species has a pharmacol. potential for the treatment of primary dysmenorrhea, supporting its use in folk medicine.

Journal of Ethnopharmacology published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Rao, Ashwin U. published the artcileSynthesis and structure-activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridines as H₃ receptor antagonists, Safety of (6-Hydroxypyridin-3-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(21), 6176-6180, database is CAplus and MEDLINE.

A series of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridines I (X = N, Y = CH; X = CH, Y = N; R = H, H₂N, CN, Cl, MeCONH, 4-NCC₆H₄, 2-fluoro-3-pyridyl, 5-pyrimidyl, etc.) was synthesized and evaluated as a new lead of non-imidazole histamine H₃ receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about 903899-13-8. 903899-13-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Alcohol,Boronic Acids,Boronic acid and ester, name is (6-Hydroxypyridin-3-yl)boronic acid, and the molecular formula is C5H6BNO3, Safety of (6-Hydroxypyridin-3-yl)boronic acid.

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

Liu, Xiaoqing published the artcileInfluence of Guest/Host Morphology on Room Temperature Phosphorescence Properties of Pure Organic Doped Systems, Name: Phenyl(pyridin-2-yl)methanone, the publication is Journal of Physical Chemistry Letters (2021), 12(30), 7357-7364, database is CAplus and MEDLINE.

Guest/host phosphorescence materials have attracted much attention; traditionally, researchers have focused on the influence of the electronic properties and energy levels of the mols. on the phosphorescence activities. The effects of the morphol. on the phosphorescence are ignored. Three isoquinoline guests with different aliphatic rings and 3 hosts are selected to construct guest/host materials. The guests are dispersed in the host as clusters. The morphols. of the guest/host directly affect the phosphorescence. In these systems, the guests have strong intermol. interactions, which are beneficial to stabilize the triplet excitons; meanwhile, the hosts should have weak intermol. interactions with easily changed morphol. to accept the guest clusters, which synergistically ensure that the doped materials have excellent RTP properties. This is the 1st work focusing on the effect of mol. morphol. on the phosphorescence of guest/host systems.

Journal of Physical Chemistry Letters 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, Name: Phenyl(pyridin-2-yl)methanone.

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

Zheng, Xiaowan published the artcileStructural Requirements of the ASBT by 3D-QSAR Analysis Using Aminopyridine Conjugates of Chenodeoxycholic Acid, Synthetic Route of 18437-58-6, the publication is Bioconjugate Chemistry (2010), 21(11), 2038-2048, database is CAplus and MEDLINE.

The human apical sodium-dependent bile acid transporter (ASBT) is a validated drug target and can be employed to increase oral bioavailability of various drug conjugates. The aim of the present study was to investigate the chem. space around the 24-position of bile acids that influences both inhibition and uptake by the transporter. A series of 27 aminopyridine and aminophenol conjugates of glutamyl-chenodeoxycholate were synthesized and their ASBT inhibition and transport kinetics (parametrized as K_i, K_t, and J_max) measured using stably transfected ASBT-MDCK cells. All conjugates were potent ASBT inhibitors. Monoanionic conjugates exhibited higher inhibition potency than neutral conjugates. However, neutral conjugates and chloro-substituted monoanionic conjugates were not substrates, or at least not apparent substrates. Kinetic anal. of substrates indicated that similar values for K_i and K_t implicate substrate binding to ASBT as the rate-limiting step. Using 3D-QSAR, four inhibition models and one transport efficiency model were developed. Steric fields dominated in CoMFA models, whereas hydrophobic fields dominated CoMSIA models. The inhibition models showed that a hydrophobic or bulky substitute on the 2 or 6 position of a 3-aminopyridine ring enhanced activity, while a hydrophobic group on the 5 position was detrimental. Overall, steric and hydrophobic features around the 24 position of the sterol nucleus strongly influenced bile acid conjugate interaction with ASBT. The relative location of the pyridine nitrogen and substituent groups also modulated binding.

Bioconjugate Chemistry published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C15H14O3, Synthetic Route of 18437-58-6.

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

Zhao, Bin published the artcileElectrochemical fluorosulfonylation of alkenes to access vicinal fluorinated sulfones derivatives, Quality Control of 91-02-1, the publication is Tetrahedron (2022), 132651, database is CAplus.

Herein, a practical and efficient fluorosulfonylation of the various alkenes with sulfonyl radical sources and Et₃N·3HF as cost-effective fluorination reagents under mild conditions is reported. Remarkably, this protocol features very green and sustainable conditions obviating the need of chem. oxidants and transition metal catalyst. A variety of substituents on both sulfonyl hydrazides and alkenes are tolerated to give vicinal fluorinated sulfones in moderate to excellent yields. Also, the synthetic utility of this transformation is further demonstrated by a gram-scale reaction and the late-stage functionalization of complex mols.

Tetrahedron 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 C20H17FO4S, Quality Control of 91-02-1.

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

Brem, Jurgen published the artcileImitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors, Computed Properties of 844501-00-4, the publication is Nature Chemistry (2022), 14(1), 15-24, database is CAplus and MEDLINE.

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential β-lactamase stable β-lactam mimics. Subsequent structure-activity relationship studies revealed InCs as a new class of potent MBL inhibitor, active against all MBL classes of major clin. relevance. Crystallog. studies revealed a binding mode of the InCs to MBLs that, in some regards, mimics that predicted for intact carbapenems, including with respect to maintenance of the Zn(II)-bound hydroxyl, and in other regards mimics binding observed in MBL-carbapenem product complexes. InCs restore carbapenem activity against multiple drug-resistant Gram-neg. bacteria and have a low frequency of resistance. InCs also have a good in vivo safety profile, and when combined with meropenem show a strong in vivo efficacy in peritonitis and thigh mouse infection models. [graphic not available: see fulltext]

Nature Chemistry published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Computed Properties of 844501-00-4.

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

Varghese, Hema Tresa published the artcileVibrational spectroscopic studies and ab initio calculations of pyridine-3-sulfonic acid, Synthetic Route of 636-73-7, the publication is Asian Journal of Chemistry (2007), 19(4), 2627-2632, database is CAplus.

FT-Raman and FT-IR spectra of pyridine-3-sulfonic acid were recorded and analyzed. The mol. geometry and vibrational wave numbers of pyridine-3-sulfonic acid have been calculated using the Hartree-Fock method with different basis sets. Comparison of the observed fundamental vibrational wavenumbers of pyridine-3-sulfonic acid with calculated results by Hartree-Fock method is found in agreement with the exptl. data.

Asian Journal of Chemistry 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 C10H15NO, Synthetic Route of 636-73-7.

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

Krommyda, Kalliopi published the artcileA Remarkable Effect of Aluminum on the Novel and Efficient Aqueous-Phase Hydrogenation of Levulinic Acid into γ-Valerolactone Using Water-Soluble Platinum Catalysts Modified with Nitrogen-Containing Ligands, SDS of cas: 636-73-7, the publication is Catalysis Letters (2019), 149(5), 1250-1265, database is CAplus.

The catalytic performance of novel water-soluble platinum catalysts modified with various nitrogen-containing and phosphine ligands in the hydrogenation reaction of levulinic acid (LA) into γ-valerolactone (GVL) has been studied in environmentally attractive, green, aqueous monophasic systems. The presence of the Lewis acid aluminum enormously increases the catalytic activity of water-soluble platinum catalysts modified with nitrogen-containing ligands in the LA hydrogenation reaction and high catalytic activities up to 3540 TOF’s per h with a quant. selectivity towards GVL have been achieved using Na₂PtCl₆·6H₂O precursors modified with the bidentate bathophenanthrolinedisulfonic acid disodium salt (BPhDS) ligand and low amounts of AlCl₃·6H₂O promotors (molar ratio of AlCl₃·6H₂O/Pt = 0.17) in aqueous media. This unprecedented increase in catalytic activity with aluminum promotors for water-soluble transition metal catalytic systems in aqueous-phase hydrogenation reactions has not been described until now in the literature. The apparent activation energy of platinum catalyst modified with the monodentate nitrilotriacetic acid trisodium salt ligand in aqueous medium was calculated and amounts to a relative low value of 73.04 kJ mol^-1 when one considers that in the LA hydrogenation reaction this catalyst reduces a less reactive keto group into alc. functionality. A recycling experiment of the Pt/BPhDS/Al catalyst from the aqueous monophasic LA hydrogenation reaction mixture followed by biphasic recovery of the catalyst in active form from organic reaction products by extraction and simple phase separation of an aqueous/organic two-phase system formed after addition of di-Et ether has shown that the Pt/BPhDS/Al catalyst is stable without loss of activity and selectivity in a consecutive run.

Catalysis 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, SDS of cas: 636-73-7.

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

Zhang, Lei published the artcileMetal-ligand binding interactions in rhodium/palladium-catalyzed synthesis of dihydroquinolines, HPLC of Formula: 612845-44-0, the publication is Journal of Organic Chemistry (2014), 79(24), 12159-12176, database is CAplus and MEDLINE.

A domino Rh- and Pd-catalyzed synthesis of dihydroquinolines is disclosed. Two metals and two ligands are placed in one reaction vessel along with the two reactive reagents to afford selective sequential coupling despite the potential for side reactions. In this report, we describe mechanistic investigations attempting to discern the catalyst-ligand interactions occurring in this domino reaction. Through these studies, the reactivity and relative catalyst ligand loadings were successfully tuned to efficiently access the heterocyclic products.

Journal of Organic 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 C15H20O6, HPLC of Formula: 612845-44-0.

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

Zupan, Marko published the artcileReactions of the N-F class of fluorinating reagents with solvents, Computed Properties of 107263-95-6, the publication is Journal of Fluorine Chemistry (1996), 78(2), 137-140, database is CAplus.

The transformations of various reagents of the N-F type in water, acetonitrile, alcs. and aqueous solutions of alkali hydroxides were investigated. First-order kinetics for 1-chloromethyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (F-TEDA) and 1-hydroxy-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (NFTh) transformations were established: F-TEDA is less stable in water at 60 °C than NFTh, while N-fluorobis(phenylsulfonyl)amine (NFS) is very stable. The addition of acetonitrile to an aqueous solution of F-TEDA enhanced the transformation (k = 1.3×10^-5 s^-1), while a reaction which was three-times faster was observed in water/methanol solution (k = 3.5×10^-5 s^-1 at 60 °C). The energy of activation for the transformation of F-TEDA in water was found to be 21.1 kcal mol^-1, 20.6 kcal mol^-1 in water/methanol solution and 13.8 kcal mol^-1 in a water/acetonitrile mixture

Journal of Fluorine Chemistry published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C7H13BrSi, Computed Properties of 107263-95-6.

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