Varghese, Hema Tresa’s team published research in Asian Journal of Chemistry in 19 | CAS: 636-73-7

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.

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

Brem, Jurgen’s team published research in Nature Chemistry in 14 | CAS: 844501-00-4

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.

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

Zhao, Bin’s team published research in Tetrahedron in 106-107 | CAS: 91-02-1

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.

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

Zheng, Xiaowan’s team published research in Bioconjugate Chemistry in 21 | CAS: 18437-58-6

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.

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 Ki, Kt, and Jmax) 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 Ki and Kt 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

Liu, Xiaoqing’s team published research in Journal of Physical Chemistry Letters in 12 | CAS: 91-02-1

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.

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

Rao, Ashwin U.’s team published research in Bioorganic & Medicinal Chemistry Letters in 19 | CAS: 903899-13-8

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.

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

Macedo, Cicero Andre Ferreira’s team published research in Journal of Ethnopharmacology in 290 | CAS: 21829-25-4

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.

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

Nguyen, Phuhai’s team published research in European Journal of Medicinal Chemistry in 82 | CAS: 39856-58-1

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 C5H5BrN2, COA of Formula: C5H5BrN2.

Nguyen, Phuhai published the artcileEvaluation of the antiprion activity of 6-aminophenanthridines and related heterocycles, COA of Formula: C5H5BrN2, the publication is European Journal of Medicinal Chemistry (2014), 363-371, database is CAplus and MEDLINE.

Several 6-(amino)phenanthridine derivatives and related heterocyclic compounds such as benzonaphtyridine derivatives were prepared A reduction of one of the three aromatic rings was also performed. The compounds were first tested for their antiprion activity in a previously described yeast-based colorimetric prion assay. The most potent derivatives were then assayed ex-vivo against the mammalian prion PrPSc in a cell-based assay. Several of the new compounds were found more potent than the parent lead 6-aminophenanthridine. The most promising compounds against yeast and mammalian prions were 8-azido-6-aminophenanthridine and 7,10-dihydrophenanthridin-6-amine. In the mammalian cell-based assay, the IC50 of these two compounds were around 5 μM and 1.8 μM, resp. The synthesis of the target compounds was achieved by a coupling reaction of boronic acid esters, such as 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzenamine, 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile with suitable aryl bromides or aryl chlorides. The tilte compounds thus formed included 6-phenanthridinamine derivatives and analogs, such as benzo[c][2,6]naphthyridin-5-amine, benzo[h][1,6]naphthyridin-5-amine, benzo[c][1,8]naphthyridin-6-amine, benzo[c][1,6]naphthyridine, benzo[c]-1,5-naphthyridine.

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 C5H5BrN2, COA of Formula: C5H5BrN2.

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

Loh, Yean Chun’s team published research in Biomedicine & Pharmacotherapy in 150 | CAS: 21829-25-4

Biomedicine & Pharmacotherapy 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.

Loh, Yean Chun published the artcileThe predominance of endothelium-derived relaxing factors and beta-adrenergic receptor pathways in strong vasorelaxation induced by 4-hydroxybenzaldehyde in the rat aorta, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Biomedicine & Pharmacotherapy (2022), 112905, database is CAplus and MEDLINE.

4-Hydroxybenzaldehyde (4HB), known as ρ-hydroxybenzaldehyde, is commonly present in traditional Chinese medicine herb, most frequently used for hypertension treatment. This research aims to determine the potency of 4HB’s vasorelaxant action. In the study, the vasodilation effect of 4HB was evaluated using in vitro isolated rat aortic rings assay. The aortic rings were pre-incubated with resp. antagonists before being pre-contracted with phenylephrine (PE) and challenged with various concentrations of 4HB for mechanistic action studies. Rmax (maximal vasodilation) and pEC50 (neg. logarithm of half-maximal effective concentration) values of each experiment were determined for comparison purposes. 4HB caused vasodilation on endothelium-intact aortic rings which pre-contracted with PE (pEC50 = 3.53 ± 0.05, Rmax = 100.95 ± 4.25%) or potassium chloride (pEC50 = 2.96 ± 0.13, Rmax = 72.13 ± 4.93%). The vasodilation effect of 4HB was significantly decreased in the absence of an endothelium (pEC50 = 2.21 ± 0.25, Rmax = 47.96 ± 4.16%). The atropine, 4-aminopyridine, Nω-nitro–arginine Me ester, glibenclamide, and propranolol significantly reduced the vasorelaxation effect of 4HB. Besides that, 4HB blocked the voltage-operated calcium channel (VOCC) and regulated the intracellular Ca2+ release from the sarcoplasmic reticulum (SR) in the aortic ring. Thus, the results indicated that 4HB exerted its vasodilatory effect via cGMP and β2 pathways, M3-dependent PLC/IP3 pathways, and potassium and calcium channels.

Biomedicine & Pharmacotherapy 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

Mochida, Kazuhiko’s team published research in Marine Pollution Bulletin in 64 | CAS: 971-66-4

Marine Pollution Bulletin published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, SDS of cas: 971-66-4.

Mochida, Kazuhiko published the artcileUse of species sensitivity distributions to predict no-effect concentrations of an antifouling biocide, pyridine triphenylborane, for marine organisms, SDS of cas: 971-66-4, the publication is Marine Pollution Bulletin (2012), 64(12), 2807-2814, database is CAplus and MEDLINE.

We used species sensitivity distributions (SSDs) and a Bayesian statistical model to carry out a primary risk assessment for pyridine triphenylborane (PTPB) in Hiroshima Bay, Japan. We used SSDs derived from toxicity values, such as EC50 and LC50, obtained from this study and previous work to calculate hazardous concentrations that should protect 95% and 99% of species (HC5 and HC1) and demonstrated that the medians of the HC5 and HC1 were 0.78 and 0.17 μg/L, resp. We also used liquid chromatog./mass spectrometry to investigate the occurrence of PTPB in seawater from several coastal sites of Hiroshima Bay and detected PTPB at concentrations of 4.8-21 pg/L. Comparison of environmental concentrations to the HC values suggests that the current ecol. risk posed by PTPB in Hiroshima Bay is low. This is the first report of the detection of PTPB in the natural marine environment.

Marine Pollution Bulletin published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, SDS of cas: 971-66-4.

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