Day: December 8, 2022

Ravasenga, Tiziana published the artcileSpatial regulation of coordinated excitatory and inhibitory synaptic plasticity at dendritic synapses, SDS of cas: 21829-25-4, the publication is Cell Reports (2022), 38(6), 110347, database is CAplus and MEDLINE.

The induction of synaptic plasticity at an individual dendritic glutamatergic spine can affect neighboring spines. This local modulation generates dendritic plasticity microdomains believed to expand the neuronal computational capacity. Here, we investigate whether local modulation of plasticity can also occur between glutamatergic synapses and adjacent GABAergic synapses. We find that the induction of long-term potentiation at an individual glutamatergic spine causes the depression of nearby GABAergic inhibitory synapses (within 3 μm), whereas more distant ones are potentiated. Notably, L-type calcium channels and calpain are required for this plasticity spreading. Overall, our data support a model whereby input-specific glutamatergic postsynaptic potentiation induces a spatially regulated rearrangement of inhibitory synaptic strength in the surrounding area through short-range heterosynaptic interactions. Such local coordination of excitatory and inhibitory synaptic plasticity is expected to influence dendritic information processing and integration.

Cell Reports 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, SDS of cas: 21829-25-4.

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

Aharon, Cheryl published the artcileUsing fluoroform for constructing aromatic and heterocyclic trifluoromethylselenyl compounds, Recommanded Product: 2-Pyridinylboronic acid, the publication is Journal of Fluorine Chemistry (2021), 109866, database is CAplus.

Fluoroform is used to prepare CuCF₃ according to literature procedures. This nucleophilic trifluoromethyl moiety was reacted with aromatic and heterocyclic selenium cyanide derivatives 3-R-4-N(R₁)(R₂)-5-R³C₆H₂SeCN (R = H, Me, Br; R¹ = H, Et, Ac; R² = H, Et, Ac; R³ = H, Me), 3-R⁴-4-R⁵-C₆H₃SeCN (R⁴ = H, Me; R⁵ = Me, t-Bu, Cl, etc.), I (R⁶ = H, Br; R⁷ = H, SeCN; R⁸ = H, SeCN) and II (X = O, S) resp. to form the corresponding trifluoromethylselenium compounds 3-R-4-N(R₁)(R₂)-5-R³C₆H₂SeCF₃, 3-R⁴-4-R⁵-C₆H₃SeCF₃, III (R⁹ = H, SeCF₃; R¹⁰ = H, SeCF₃) and IV. Selenium cyanides were made with 1,3-dicyanotriselenide prepared in situ from malononitrile and selenium dioxide. The electrophilicity of the reagent (^δ+SeCN) was enough to attack aniline derivatives 3-R-4-N(R₁)(R₂)-5-R³C₆H₃ at the para position, but with other aromatics it was advantageous to use the corresponding boronic acids 3-R⁴-4-R⁵-C₆H₃B(OH)₂, V (R¹¹ = H, B(OH)₂; R¹² = H, B(OH)₂) and VI as the moiety was easily displaced by the selenium cyanate moiety.

Journal of Fluorine Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

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

Das, Rudra Narayan published the artcilePredictive in silico Modeling of Ionic Liquids toward Inhibition of the Acetyl Cholinesterase Enzyme of Electrophorus electricus: A Predictive Toxicology Approach, Synthetic Route of 17281-59-3, the publication is Industrial & Engineering Chemistry Research (2014), 53(2), 1020-1032, database is CAplus.

Chems. are the essential components of the industry for maneuvering the required need of the living ecosystem. Ionic liquids are a group of promising novel chems. with potential usefulness toward various industrial applications, although they are not entirely devoid of hazardous outcomes. The present study is an attempt to investigate the chem. attributes of a wide variety of 292 ionic liquids toward their inhibitory potential of acetyl cholinesterase enzyme of elec. eel through the development of predictive regression and classification-based quant. math. models in the light of the OECD guidelines. Mol. docking studies have addnl. corroborated the results. Hydrophilicity, hydrophobicity, branching, and pos. charged N-species were observed to be the major chem. contributors to such toxicity. The docking studies chiefly portrayed the π-cationic type interaction of the cationic N⁺ atom with the Phe 288, Phe 290, and Trp 23 residues of the acyl binding pocket to be responsible for enzyme inhibition.

Industrial & Engineering Chemistry Research published new progress about 17281-59-3. 17281-59-3 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitrile,Salt, name is 1-(Cyanomethyl)pyridin-1-ium chloride, and the molecular formula is C7H7ClN2, Synthetic Route of 17281-59-3.

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

Sarkar, Abhijit published the artcileDendritic polymer networks: a new class of nano-domained environmentally benign antifouling coatings, Category: pyridine-derivatives, the publication is ACS Symposium Series (2009), 165-186, database is CAplus.

A new type of antifouling coatings for application in both fresh water and marine environments has been developed utilizing dendritic polymer nanotechnol. The resulting coatings are capable of encapsulating and strongly binding electrophilic biocides in their dendritic nano-cells, where biocides retain their antifouling activity while being prevented from leaching and polluting the aquatic environment. These coatings for the first time successfully combine the best properties of non-stick and biocide-containing coatings and provide an environment-ally benign solution for the protection of man-made objects.

ACS Symposium Series 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, Category: pyridine-derivatives.

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

Ali, Hasrat published the artcileSynthesis of A-ring fluorinated derivatives of iodine-125-labeled (17α,20E/Z)-iodovinylestradiols: effect on receptor binding and receptor-mediated target tissue uptake, Synthetic Route of 107263-95-6, the publication is Journal of Medicinal Chemistry (1993), 36(21), 3061-72, database is CAplus and MEDLINE.

Title iodovinylestradiols (IVE₂) I, II, III and IV (X = H, Y = H, Me; X = OMe, Y = H) were prepared and in vitro and in vivo properties were their evaluated. Electrophilic substitution of the estrone derivatives and N-fluoropyridinium salt gave the 2- and 4-fluoro analogs which were subsequently converted to the 17α-ethynyl derivatives The tributylstannyl intermediates were obtained from the corresponding 17α-ethynyl analogs using azobisisobutyronitrile or triethylborane as catalyst. All 12 products were also prepared as their no-carrier-added [¹²⁵I]iodovinyl analogs via destannylation of the tributylstannyl precursors. Binding affinity for the estrogen receptor (ER) was in general higher for the 4-F derivatives as compared to the 2-F derivatives, while 20Z isomers of the same compounds showed somewhat higher ER binding affinity as compared to the 20E isomers. The combination of an A-ring fluoro and 7α- or 11β-substituent decreased ER binding affinity. Substitution of a fluoro atom at C-4 on either the 17α-ethynylestradiol or isomeric 17α-IVE₂ enhanced the affinity of the parent mol. for the ER. A-ring fluorination of all other analogs tested had no effect or depressed ER binding affinity. Varying incubation conditions showed substantial differences in ER binding kinetics between the 20E and 20Z isomers. Tissue distribution in immature female rats showed that the highest uterus uptake and uterus to blood/nontarget ratios in the IVE₂ series were obtained with the 4-F-(17α,20Z)IVE₂ isomer. The combination of A-ring fluoro and 7α- or 11β-substitution decreased uterus uptake but had little or no effect on uterus to blood/nontarget ratios. The highest uterus to blood ratios were observed for the 4-F-(17α,20E)11β-OMe-IVE₂ (75 at 6 h and 125 at 12 h pi) reflecting rapids blood clearance and in vivo stability, as confirmed by the low levels of thyroid radioactivity. The lack of correlation between ER binding affinities and uterus uptake,and/or uptake ratios, suggests that other factors, including nonspecific binding and metabolic processes, also are involved in the tissue localization process. The authors’ data suggest that 4-F substitution onto (17α,20Z)IVE₂ and (17α,20E)11β-OMe-IVE₂ enhances the potential of these compounds to function as SPECT imaging agents of ER-rich tissues.

Journal of Medicinal 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 C6H5F4NO3S, Synthetic Route of 107263-95-6.

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

Malarski, Z. published the artcileDielectric and spectroscopic studies of pentachlorophenol-amine complexes, Recommanded Product: 4-Amino-2-picoline, the publication is Journal of Physical Chemistry (1982), 86(3), 401-6, database is CAplus.

Dipole moments in CCl₄, IR absorption spectra under various conditions, and UV spectra of a number of pentachlorophenol (PCP) complexes with N bases were measured over a broad ΔpK_a range. From the dipole moment measurements an inversion region of ΔpK_a was found for which a 50% proton transfer can be expected. The complexes from this region exhibit certain anomalies in their IR spectra, in particular a broad continuous absorption, a strong temperature effect on the absorption in the far-IR, and particular sensitivity to changes in solvent polarity. The UV spectra revealed proton-transfer equilibrium for a number of complexes, both in solutions and in the solid state.

Journal of Physical 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 C6H8N2, Recommanded Product: 4-Amino-2-picoline.

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

Saraf, Isha published the artcileForced Solid-State Oxidation Studies of Nifedipine-PVP Amorphous Solid Dispersion, Computed Properties of 21829-25-4, the publication is Molecular Pharmaceutics (2022), 19(2), 568-583, database is CAplus and MEDLINE.

In the present study, the oxidative degradation behavior of nifedipine (NIF) in amorphous solid dispersions (ASDs) prepared with poly(vinyl pyrrolidone) (PVP) with a short (K30) and a long (K90) chain length was investigated. The ASDs were prepared via dry ball-milling and analyzed using Fourier transform IR (IR) spectroscopy, X-ray scattering, and differential scanning calorimetry. The ASDs were exposed to accelerated thermal-oxidative conditions using a pressurized oxygen headspace (120 °C for 1 day) and high temperatures at atm. pressure (60-120 °C for a period of 42 days). Addnl., solution-state oxidative degradation studies showed that pure NIF degrades to a greater extent than in the presence of PVP. Electronic structure calculations were performed to understand the impact of drug-polymer intermol. interactions on the autoxidation of drugs. While no drug degradation was observed in freshly prepared ASD samples, alkyl free radicals were detected via ESR (EPR) spectroscopy. The free radicals were found to be consumed to a greater extent by PVP K30- than PVP K90-based ASDs upon exposure to high oxygen pressures. This was consistent with the greater solid-state oxidative degradation of NIF observed in ASDs with PVP K30 than with PVP K90. As no drug recrystallization occurred during this study period, the lower glass-transition temperature and presumed greater mol. mobility of PVP K30 and its ASD as compared to the PVP K90 system appear to contribute to the greater drug degradation in PVP-K30-based ASDs. The extent and the rate of oxidative degradation were higher in the case of PVP-K30-based ASD as compared to that in PVP-K90-based ASD, and the overall degradation increased with an increase in temperature IR spectral anal. of drug-polymer interactions supports the electronic calculations of the oxidation process. We infer that, apart from the initial free radical content, the difference in the extent of drug-polymer intermol. interactions in ASDs and amorphous stabilization during the forced oxidation experiments contribute to the observed differences in the autoxidative reactivity of the drug in ASDs with different PVP chain lengths. Overall, the chem. degradation of NIF in ASDs with two PVP chain lengths obtained from accelerated solid-state oxidation studies was in qual. agreement with that obtained from long-term (3 years) storage under ambient conditions. The study highlights the ability of accelerated processes to determine the oxidative degradation behavior of polymeric ASDs and suggests that the polymer chain length could factor into chem. as well as phys. stability considerations.

Molecular Pharmaceutics 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, Computed Properties of 21829-25-4.

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

Zeng, Qingbei published the artcileSynthesis and SAR studies of benzimidazolone derivatives as histamine H₃-receptor antagonists, Related Products of pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(21), 6001-6003, database is CAplus and MEDLINE.

A novel series of benzimidazolone-containing histamine H₃-receptor antagonists were prepared and their structure-activity relationship was explored. These benzimidazolone analogs demonstrate potent H₃-receptor binding affinities, no P 450 enzyme inhibition, and strong H₃ functional activity. Compound I exhibits the best overall profile with H₃K_i = 0.95 nM and rat AUC = 12.9 μM h.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C19H21N3O3S, Related Products of pyridine-derivatives.

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

Bell, Colin Frank published the artcileComplexes between pyridine-2-carboxaldehyde 2′-pyridylhydrazone and the platinum metals. II. Iridium, Synthetic Route of 2215-33-0, the publication is Inorganic Chemistry (1969), 8(1), 161-3, database is CAplus.

Aqueous (NH4)3(IrCl6) was refluxed with pyridine-2-carboxaldehyde 2′-pyridylhydrazone (HL) in CHCl3 to form [Ir(HL)3]. Also prepared were [IrCl2(HL)]ClO4.2H2O, [IrCl2pyL], and [IrCl3py(HL)] (I), where I is the 1,2,6-isomer. The complexes were characterized by absorption spectra, ir. spectra, and conductance measurements. HL appears to behave as a bidentate ligand in the complexes except in the case of [IrCl2pyL] where it is tridentate.

Inorganic Chemistry 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, Synthetic Route of 2215-33-0.

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

Bell, Colin Frank published the artcileComplexes between pyridine-2-aldehyde-2′-pyridylhydrazone and the platinum metals. I. Rhodium, Formula: C11H10N4, the publication is Inorganic Chemistry (1968), 7(2), 325-9, database is CAplus.

Mono, bis, and tris complexes of Rh(III) and pyridine-2-aldehyde-2′-pyridylhydrazone have been prepared and studied. In all three, the H atom of the imino group of the ligand shows marked acidity associated with coordination to a tripos. metal. The ligand is tridentate in the mono and bis complexes but bidentate in the tris complex. Possible geometrical isomers of this are discussed and its probable structure is described. 17 references.

Inorganic Chemistry 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, Formula: C11H10N4.

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