Day: November 30, 2022

Cheng, Sixue published the artcileNanoconfinement Effects on the Glass Transition and Crystallization Behaviors of Nifedipine, Synthetic Route of 21829-25-4, the main research area is glass transition crystallization nifedipine; amorphous pharmaceutical; cold-crystallization; glass transition; nifedipine; polymorphism.

The impact of nanoconfinement on the crystallization and glass transition behaviors of nifedipine (NIF) has been investigated using differential scanning calorimetry. Nanoconfinement was provided by imbibing the NIF into a porous medium (controlled pore glass, CPG), and results were compared with the unconfined bulk material. Consistent with previous results from the literature, both glass transition temperature Tg and melting temperature Tm decrease with decreasing pore size. The melting temperature was found to decrease with the reciprocal of pore diameter and could be analyzed with the Gibbs-Thomson equation. In addition, for confinement sizes of 7.5 and 12 nm, it was found that no cold-crystallization occurs upon heating from the glassy state to above the expected melting transition. Finally, at intermediate confinements we find evidence of a possible new, confinement-induced polymorph of NIF.

Molecular Pharmaceutics published new progress about Crystal polymorphism. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Synthetic Route of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Limanjaya, Ivan published the artcileL-selectin activation regulates Rho GTPase activity via Ca+2 influx in Sertoli cell line, ASC-17D cells, Product Details of C17H18N2O6, the main research area is L selectin Rho GTPase calcium channel sertoli cell; ASC-17D cells; Calcium influx; L-selectin; Rho GTPase.

In seminiferous epithelium, tight junctions (TJs) between adjacent Sertoli cells constitute the blood-testis barrier and must change synchronically for germ cells to translocate from the basal to the adluminal compartment during the spermatogenic cycle. Rho GTPase activation through stimulation with specific L-selectin ligands has been proposed to modulate tight junctional dynamics. However, little is known regarding the role of Ca+2 dynamics in Sertoli cell and how Ca+2 relays L-selectin signals to modulate Rho GTPase activity in Sertoli cells, thus prompting us to investigate the Ca+2 flux induced by L-selectin ligand in ASC-17D cells. Using fluorescent real-time image, we first demonstrated the increase of intracellular Ca+2 level following L-selectin ligand stimulation. This Ca+2 increase was inhibited in ASC-17D cells pretreated with nifedipine, the L-type voltage-operated Ca+2 channel (VOCC) blocker, but not mibefradil, the T-type VOCC blocker. We then demonstrated the up-regulation of Rho and Rac1 in ASC-17D cells following the administration of L-selectin ligand, and the pre-treatment with nifedipine, but not mibefradil, prior to L-selectin ligand-binding abolished the activation of both Rho and Rac1. Together, we conclude that the activation of L-selectin induces Ca+2 influx through the L-type VOCC, which up-regulates Rho and Rac1 proteins, in ASC-17D cells.

Biochemical and Biophysical Research Communications published new progress about Blood-testis barrier. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lee, Chin-Mei published the artcileGIGANTEA recruits the UBP12 and UBP13 deubiquitylases to regulate accumulation of the ZTL photoreceptor complex, Category: pyridine-derivatives, the main research area is Arabidopsis seed UBP12 UBP13 GIGANTEA ZTL photoreceptor complex.

ZEITLUPE (ZTL), a photoreceptor with E3 ubiquitin ligase activity, communicates end-of-day light conditions to the plant circadian clock. It still remains unclear how ZTL protein accumulates in the light but does not destabilize target proteins before dusk. Two deubiquitylating enzymes, UBIQUITIN-SPECIFIC PROTEASE 12 and 13 (UBP12 and UBP13), which regulate clock period and protein ubiquitylation in a manner opposite to ZTL, associate with the ZTL protein complex. Here we demonstrate that the ZTL interacting partner, GIGANTEA (GI), recruits UBP12 and UBP13 to the ZTL photoreceptor complex. We show that loss of UBP12 and UBP13 reduces ZTL and GI protein levels through a post-transcriptional mechanism. Furthermore, a ZTL target protein is unable to accumulate to normal levels in ubp mutants. This demonstrates that the ZTL photoreceptor complex contains both ubiquitin-conjugating and -deconjugating enzymes, and that these two opposing enzyme types are necessary for circadian clock pacing. This shows that deubiquitylating enzymes are a core element of circadian clocks, conserved from plants to animals.

Nature Communications published new progress about Arabidopsis thaliana. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Grenier, Melissa C. published the artcileThe antibacterial activity of 4,4′-bipyridinium amphiphiles with conventional, bicephalic and gemini architectures, Quality Control of 36437-30-6, the main research area is antibacterial bipyridinium amphiphile.

Dialkyl 4,4′-bipyridinium compounds are widely employed for their useful redox properties, and are commonly known as viologens due to their intense coloration upon reduction Despite their prevalence and amphiphilic nature, the antibacterial activity of these compounds remains largely unreported. The authors have prepared a series of mono- and bis-alkylated analogs of 4,4′-bipyridine to investigate structure-activity relationships in their inhibition of a battery of Gram-pos. and Gram-neg. bacteria. The prepared cationic compounds were conventional (one cationic head, one non-polar tail), bicephalic (two heads, one tail), or gemini (two heads, two tails) in their amphiphilic structure. Addnl., an isomeric series of six bis-alkylated compounds ranging from sym. (PQ-11,11) to highly asym. (PQ-20,2) were prepared Four themes of bioactivity emerged: (1) the most bioactive compounds were gemini in structure; (2) 22 carbons in the alkyl chains, with little to modest asymmetry, led to optimal activity; (3) bicephalic compounds were generally comparable to conventional amphiphiles, though only about 12 carbons in the alkyl chains were solubilized in water by each cationic nitrogen; (4) the effects of counterion identity were not evident between chlorides and bromides; however, the presence of the iodide counterion inhibited dissolution in all compounds tested. Three isomeric compounds with little to no asymmetry in tail length, PQ-11,11, PQ-12,10, and PQ-14,8, prepared as the bromide salts, showed comparable and highly potent activity, with MIC levels around 2 μM against 3 of 4 bacteria tested. The simple (one- to two-step) syntheses of potent antimicrobials portend well for future optimization.

Bioorganic & Medicinal Chemistry Letters published new progress about Antibacterial agents. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Quality Control of 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kulathooran, S. published the artcileSynthesis and biological activities of novel heterocyclic chalcone derivatives by two different methods using anhydrous potassium carbonate as an efficient catalyst, SDS of cas: 71255-09-9, the main research area is acetyl dimethylfuran aryl aldehyde potassium carbonate catalyst microwave irradiation; chalcone preparation diastereoselective green chem antibacterial antifungal activity SAR.

A series of twenty 3-(aryl)-1-(2,5-dimethylfuran-3-yl)prop-2-en-1-one I [R = 2,5-(F)2-C6H3, 2-naphthyl, 2-biphenyl, etc.] were synthesized by using conventional and microwave irradiation methods in the presence of anhydrous potassium carbonate as an safe, inexpensive and efficient basic catalyst. Synthesized compounds were evaluated for their in-vitro antimicrobial activity against variety of microbial strains and it was characterized by IR, NMR (1H & 13C) and mass spectral anal. The biol. screening results indicated that some of the compounds showed significant antibacterial and antifungal activities. Compound I [R = 3-methyl-2-thiophenyl] displayed excellent antimicrobial activity against various microbial strains. The newly synthesized high potent compound I [R = 3-methyl-2-thiophenyl] was subjected to thermogravimetric anal. (TGA), differential scanning calorimetric (DSC) and single crystal XRD.

Pharma Chemica published new progress about Antibacterial agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, SDS of cas: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fontaine, Fanny published the artcileFirst identification of boronic species as novel potential inhibitors of the Staphylococcus aureus NorA efflux pump, COA of Formula: C6H8BNO2S, the main research area is boron compound transport protein NorA Staphylococcus.

Overexpression of efflux pumps is an important mechanism of bacterial resistance that results in the extrusion of antimicrobial agents outside the bacterial cell. Inhibition of such pumps appears to be a promising strategy that could restore the potency of existing antibiotics. The NorA efflux pump of Staphylococcus aureus confers resistance to a wide range of unrelated substrates, such as hydrophilic fluoroquinolones, leading to a multidrug-resistance phenotype. Here, 150 heterocyclic boronic species were evaluated for their activity against susceptible and resistant strains of S. aureus. Twenty-four hit compounds, although inactive when tested alone, were found to potentiate ciprofloxacin activity by a 4-fold increase at concentrations ranging from 0.5 to 8 μg/mL against S. aureus 1199B, which overexpresses NorA. Boron-free analogs showed no biol. activity, thus revealing that the boron atom is crucial for biol. activity. This work describes the first reported efflux pump inhibitory activity of boronic acid derivatives

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, COA of Formula: C6H8BNO2S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Empel, Anna published the artcileTowards Property Profiling: SYNTHESIS and SAR Probing of New Tetracyclic Diazaphenothiazine Analogues, Recommanded Product: 2-Chloro-4-methylpyridin-3-amine, the main research area is lung breast cancer SAR anticancer tertiary phenothiazine quinoline; antibacterial activity; antiproliferative activity; azaphenothiazines; lipophilicity; pharmacophore mapping; phenothiazine; similarity-activity landscape index.

A series of new tertiary phenothiazine derivatives containing a quinoline and a pyridine fragment was synthesized by the reaction of 1-methyl-3-benzoylthio-4-butylthioquinolinium chloride with 3-aminopyridine derivatives bearing various substituents on the pyridine ring. The direction and mechanism of the cyclization reaction of intermediates with the structure of 1-methyl-4-(3-pyridyl)aminoquinolinium-3-thiolate was related to the substituents in the 2- and 4-pyridine position. The structures of the compounds were analyzed using 1H, 13C NMR (COSY, HSQC, HMBC) and X-ray anal., resp. Moreover, the antiproliferative activity against tumor cells (A549, T47D, SNB-19) and a normal cell line (NHDF) was tested. The antibacterial screening of all the compounds was conducted against the reference and quality control strain Staphylococcus aureus ATCC 29213, three clin. isolates of methicillin-resistant S. aureus (MRSA). In silico computation of the intermol. similarity was performed using principal component anal. (PCA) and hierarchical clustering anal. (HCA) on the pool of structure/property-related descriptors calculated for the novel tetracyclic diazaphenothiazine derivatives The distance-oriented property evaluation was correlated with the exptl. anticancer activities and empirical lipophilicity as well. The quant. shape-based comparison was conducted using the CoMSA method in order to indicate the potentially valid steric, electronic and lipophilic properties. Finally, the numerical sampling of similarity-related activity landscape (SALI) provided a subtle picture of the SAR trends.

International Journal of Molecular Sciences published new progress about Antibacterial agents. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Recommanded Product: 2-Chloro-4-methylpyridin-3-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jin, Bo published the artcileSynthesis and biological evaluation of 3-(pyridine-3-yl)-2-oxazolidinone derivatives as antibacterial agents, Synthetic Route of 1079179-12-6, the main research area is pyridinyl oxazolidinone preparation mol docking antibiofilm antibacterial activity; 3-(pyridine-3-yl)-2-oxazolidinone; antibacterial activity; biofilm formation inhibitory activity; drug resistance development; molecular docking.

In this research, a series of 3-(pyridine-3-yl)-2-oxazolidinone derivatives I [R = (pyridin-3-yl)carbonyl, Me, N-cyclohexylcarbamoyl, etc.], II (X = F, H) was designed, synthesized, and evaluated for in vitro antibacterial activity, which included bacteriostatic, morphol., kinetic studies, and mol. docking. The results demonstrated that compounds II [R = cyclohexanecarbonyl, (2E)-3-(furan-2-yl)prop-2-enoyl (III), (2E)-3-(pyridin-3-yl)prop-2-enoyl, N-(4-chlorophenyl)carbamoyl; X = F] exhibited strong antibacterial activity similar to that of linezolid toward five Gram-pos. bacteria. After observing the effect of the drug on the morphol. and growth dynamics of the bacteria, the possible modes of action were predicted by mol. docking. Furthermore, the antibiofilm activity and the potential drug resistance assay were proceeded. These compounds exhibited universal antibiofilm activity and compound III showed significant concentration-dependent inhibition of biofilm formation. Compound III also showed a stable effect on S. pneumoniae (ATCC 49619) with less drug resistance growth for 15 days, which is much longer than that of linezolid. Overall, these results can be used to guide further exploration of novel antimicrobial agents.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Antibacterial agents. 1079179-12-6 belongs to class pyridine-derivatives, name is 2-Chloro-3-fluoro-5-nitropyridine, and the molecular formula is C5H2ClFN2O2, Synthetic Route of 1079179-12-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jin, Bo published the artcileSynthesis and biological evaluation of 3-(pyridine-3-yl)-2-oxazolidinone derivatives as antibacterial agents, SDS of cas: 26820-62-2, the main research area is pyridinyl oxazolidinone preparation mol docking antibiofilm antibacterial activity; 3-(pyridine-3-yl)-2-oxazolidinone; antibacterial activity; biofilm formation inhibitory activity; drug resistance development; molecular docking.

In this research, a series of 3-(pyridine-3-yl)-2-oxazolidinone derivatives I [R = (pyridin-3-yl)carbonyl, Me, N-cyclohexylcarbamoyl, etc.], II (X = F, H) was designed, synthesized, and evaluated for in vitro antibacterial activity, which included bacteriostatic, morphol., kinetic studies, and mol. docking. The results demonstrated that compounds II [R = cyclohexanecarbonyl, (2E)-3-(furan-2-yl)prop-2-enoyl (III), (2E)-3-(pyridin-3-yl)prop-2-enoyl, N-(4-chlorophenyl)carbamoyl; X = F] exhibited strong antibacterial activity similar to that of linezolid toward five Gram-pos. bacteria. After observing the effect of the drug on the morphol. and growth dynamics of the bacteria, the possible modes of action were predicted by mol. docking. Furthermore, the antibiofilm activity and the potential drug resistance assay were proceeded. These compounds exhibited universal antibiofilm activity and compound III showed significant concentration-dependent inhibition of biofilm formation. Compound III also showed a stable effect on S. pneumoniae (ATCC 49619) with less drug resistance growth for 15 days, which is much longer than that of linezolid. Overall, these results can be used to guide further exploration of novel antimicrobial agents.

Frontiers in Chemistry (Lausanne, Switzerland) published new progress about Antibacterial agents. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, SDS of cas: 26820-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Oikonomou, Katerina D. published the artcileCalcium dysregulation and compensation in cortical pyramidal neurons of the R6/2 mouse model of Huntington′s disease, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Huntington disease calcium dysregulation cortical pyramidal neuron; Huntington’s disease; R6/2 mice; calcium imaging; cortical pyramidal neurons; dantrolene; two-photon laser scanning microscopy.

Huntington′s disease (HD) is a fatal, hereditary neurodegenerative disorder that predominantly affects striatal medium-sized spiny neurons and cortical pyramidal neurons (CPNs). It has been proposed that perturbations in Ca2+ homeostasis could play a role in CPN alterations. To test this hypothesis, we used the R6/2 mouse model of juvenile HD at different stages of disease progression; presymptomatic, early symptomatic, and late symptomatic. We combined whole-cell patch-clamp recordings of layer 2/3 CPNs with two-photon laser scanning microscopy to image somatic and dendritic Ca2+ transients associated with evoked action potentials (APs). We found that the amplitude of AP-induced Ca2+ transients recorded at the somata of CPNs was significantly reduced in presymptomatic and late symptomatic R6/2 mice compared with wild-type (WT) littermates. However, reduced amplitudes were compensated by increases in decay times, so that Ca2+ transient areas were similar between genotypes. AP-induced Ca2+ transients in CPN proximal dendrites were variable and differences did not reach statistical significance, except for reduced areas in the late symptomatic group. In late symptomatic mice, a specific store-operated Ca2+ channel antagonist, EVP4593, reduced somatic Ca2+ transient amplitude similarly in WT and R6/2 CPNs. In contrast, dantrolene, a ryanodine receptor (RyR) antagonist, and nifedipine, an L-type Ca2+ channel blocker, significantly reduced both somatic Ca2+ transient amplitude and area in R6/2 but not WT CPNs. These findings demonstrate that perturbations of Ca2+ homeostasis and compensation occur in CPNs before and after the onset of overt symptoms, and suggest RyRs and L-type Ca2+ channels as potential targets for therapeutic intervention. NEW & NOTEWORTHY We used two-photon microscopy to examine calcium influx induced by action potentials in cortical pyramidal neurons from a mouse model of Huntington′s disease (HD), the R6/2. The amplitude of somatic calcium transients was reduced in R6/2 mice compared with controls. This reduction was compensated by increased decay times, which could lead to reduced calcium buffering capacity. L-type calcium channel and ryanodine receptor blockers reduced calcium transient area in HD neurons, suggesting new therapeutic avenues.

Journal of Neurophysiology published new progress about Animal cell, somatic. 21829-25-4 belongs to class pyridine-derivatives, 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:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem