Category: pyridine-derivatives

Yang, Yilei published the artcileCYP3A5 genotype-dependent drug-drug interaction between tacrolimus and nifedipine in Chinese renal transplant patients, Category: pyridine-derivatives, the main research area is tacrolimus nifedipine human renal transplant CYP3A5 genotype drug interaction; CYP3A5; drug-drug interaction; nifedipine; renal transplantation; tacrolimus.

The drug-drug interactions (DDIs) of tacrolimus greatly contributed to pharmacokinetic variability. Nifedipine, frequently prescribed for hypertension, is a competitive CYP3A5 inhibitor which can inhibit tacrolimus metabolism The objective of this study was to investigate whether CYP3A5 genotype could influence tacrolimusnifedipine DDI in Chinese renal transplant patients. All renal transplant patients were divided into CYP3A5*3/*3 homozygotes (group I) and CYP3A5*1 allele carriers (CYP3A5*1/*1 + CYP3A5*1/*3) (group II). Each group was subdivided into patients taking tacrolimus co-administered with nifedipine (CONF) and that administrated with tacrolimus alone (Controls). Tacrolimus trough concentrations (C0) were measured using high performance liquid chromatog. A retrospective anal. compared tacrolimus dose (D)-corrected trough concentrations (C0) (C0/D) between CONF and Controls in group I and II, resp. At the same time, a multivariate line regression anal. was made to evaluate the effect of variates on C0/D. In this study, a significant DDI between tacrolimus and nifedipine with respect to the CYP3A5*3 polymorphism was confirmed. In group I (n = 43), the C0/D of CONF was significantly higher than in Controls [225.2 ± 66.3 vs. 155.1 ± 34.6 ng/mL/(mg/kg); p = 0.002]. However, this difference was not detected in group II (n = 27) (p = 0.216). The coadministrated nifedipine and CYP3A5*3/*3 homozygotes significantly increased tacrolimus concentrations in multivariate line regression anal. A CYP3A5 genotype-dependent DDI was found between tacrolimus and nifedipine. Therefore, personalized therapy accounting for CYP3A5 genotype detection as well as therapeutic drug monitoring are necessary for renal transplant patients when treating with tacrolimus and nifedipine.

Frontiers in Pharmacology published new progress about Allele frequency. 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

Yuan, Yu-Chang published the artcileMetal-Free Catalyzed Synthesis of Fluorescent Indolizine Derivatives, Computed Properties of 91-02-1, the publication is Journal of Organic Chemistry (2021), 86(18), 12737-12744, database is CAplus and MEDLINE.

A mild and high efficient method to prepare indolizines such as I [R = H, Me; R¹ = Me, Ph, CH₂CH₂CO₂Et; R² = H, Me, OEt; R³ = Me, Ph, 4-ClC₆H₄; R¹R² = (CH₂)₃] by two-component reaction with the acid as the catalyst was developed. In this reaction, a new ring efficiently formed in one-step reaction. A wide range of substrates could be applied and the desired products were obtained in 8-95% yields under metal-free conditions. Different indolizine derivatives I were synthesized by general conditions and microwave irradiation conditions, and compound I [R = H, R¹ = Me, R² = H, R³ = Ph] gave the best results with an isolated yield of 95% and 82%, resp. The structures of synthesized compounds I were characterized by spectral anal., and compound I [R = H, R¹R² = (CH₂)₃, R³ = 4-ClC₆H₄] was confirmed by single crystal X-ray anal. UV-vis absorption and fluorescence properties of these compounds I were correlated with substituent groups on indolizine rings.

Journal of Organic 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 C8H14O2, Computed Properties of 91-02-1.

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

Wei, Feng published the artcileStructural and photophysical study of copper iodide complex with PN̂ or PN̂P̂ ligand, Application of 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, the publication is CrystEngComm (2014), 16(24), 5338-5344, database is CAplus.

Two PN̂-type ligands, 8-(diphenylphosphino)quinoline (L₁) and 2-[2-(diphenylphosphino)ethyl]pyridine (L₂), and two PN̂P̂-type ligands, 2,6-bis((diphenylphosphino)methyl)pyridine (L₃) and 2,6-bis((di-tert-butylphosphino)methyl)pyridine (L₄), were synthesized to coordinate with copper iodide (CuI). As a result, CuI complexes with rich structures, such as discrete complexes with formulas of [Cu₂I₂(L₁)₂] (5), [Cu₃I₃(L₂)₂] (6), and [CuI(L₃)] (7), and polymeric complexes with repeating units of [Cu₂I₂(L₄)] (8), and [Cu₃I₃(L₄)] (9) were synthesized and characterized by single crystal X-ray diffraction. Besides the intriguing structures, these complexes showed rich photoluminescent properties, with emission color that varied from blue to red and a photoluminescence quantum yield (PLQY) from 1.6 to 29.9% in the solid state. MO calculation and exptl. study showed that the emissions involve halide to ligand charge transfer (XLCT), metal to ligand charge transfer (MLCT), and/or cluster-centered (CC) excited states.

CrystEngComm published new progress about 338800-13-8. 338800-13-8 belongs to pyridine-derivatives, auxiliary class Bis-phosphine Ligands, name is 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, and the molecular formula is C8H6ClF3, Application of 2,6-Bis((di-tert-butylphosphino)methyl)pyridine.

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

Zhu, Shan-Shan published the artcilePolymerization-Enhanced Photocatalysis for the Functionalization of C(sp³)-H Bonds, Safety of Phenyl(pyridin-2-yl)methanone, the publication is ACS Catalysis (2022), 12(1), 126-134, database is CAplus.

A series of conjugated polymeric photocatalysts (CPPs) based on 1,2,3,5-tetrakis(carbazol-9-yl)4,6-dicyanobenzene (4CzIPN) were synthesized via nucleophilic substitution reaction and Sonogashira-Hagihara coupling. Among the as-prepared CPPs (CPP1-CPP6), CPP3 [the copolymer of a tetrakis(dibromocarbazolyl)isophthalonitrile with 1,3,5-triethynylbenzene] was selected as the optimized heterogeneous photocatalyst for visible-light-driven functionalization of C(sp³)-H bonds to synthesize 87 final products with yields up to 99%. The heterogeneous photocatalyst CPP3 is easily recovered from the reaction with excellent retention of photocatalytic activity, which can be reused at least for five times. Time-dependent d. functional theory (TD-DFT) calculations demonstrate that the photocatalysis performance of CPP3 is superior to the corresponding monomer 4CzIPN because of the enhanced intersystem crossing (ISC) process. Spin-orbit coupling calculations prove that the rate constant of ISC outcompetes that of reverse intersystem crossing (RISC). The rapidly generated and long-lived triplet state T₁ is considered to be a more accessible excited state than the singlet-state S₁ generated from either direct excitation or RISC. The successful application of this polymerization-enhanced photocatalysis strategy should guide a metal-free approach to the rational design of CPP-type heterogeneous photocatalysts to address the dilemma of homogeneous photocatalysts in sustainability, stability, and recyclability.

ACS Catalysis 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 C19H34ClN, Safety of Phenyl(pyridin-2-yl)methanone.

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

Fang, Zhen published the artcileDiscovery of a potent and selective inhibitor of histone lysine demethylase KDM4D, Quality Control of 197958-29-5, the publication is European Journal of Medicinal Chemistry (2021), 113662, database is CAplus and MEDLINE.

Histone lysine demethylase 4D (KDM4D) plays an important role in the regulation of tumorigenesis, progression and drug resistance and has been considered a potential target for cancer treatment. However, there is still a lack of potent and selective KDM4D inhibitors. In this investigation, we report a new class of KDM4D inhibitors containing the 2-(aryl(pyrrolidine-1-yl)methyl)phenol scaffold, identified through AlphaLisa-based screening, structural optimization, and structure-activity relationship analyses. Among these inhibitors, 24s (I) was the most potent, with an IC₅₀ value of 0.023 ± 0.004μM. This compound exhibited more than 1500-fold selectivity towards KDM4D vs. KDM4A as well as other JMJD subfamily members, indicating good selectivity for KDM4D. Kinetic anal. indicated that 24s did not occupy the 2-oxoglutarate binding pocket. In an in vitro assay, 24s significantly suppressed the proliferation and migration of colorectal cancer (CRC) cells. Overall, this study has identified a good tool compound to explore the biol. function of KDM4D and a good lead compound for drug discovery targeting KDM4D.

European Journal of Medicinal 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, Quality Control of 197958-29-5.

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

Wang, Chao-Yu published the artcilePalladium(II) complexes containing a bulky pyridinyl N-heterocyclic carbene ligand: Preparation and reactivity, HPLC of Formula: 89076-64-2, the publication is Journal of Organometallic Chemistry (2007), 692(18), 3976-3983, database is CAplus.

Coordination chem. of a pyridine imidazole-2-ylidene ligand (pyN-C) with sterically hindered substituents toward Pd(II) metal ions was studied. The Pd carbene complex [(C-pyN-C)Pd(η³-allyl)Cl] (3) was prepared via transmetalation from the corresponding Ag carbene complexes with [ClPd(η³-allyl)]₂. Upon the abstraction of chloride, coordination of pyridinyl N becomes feasible to form [C,N-(pyN-C)Pd(η³-allyl)](BF₄) (4). Ligand substitution reaction of 4 with PPh₃ gave [(C-pyN-C)Pd(PPh₃)(η³-allyl)](BF₄), in which the pyridinyl N donor is substituted by the phosphine. This Pd complex appears to be base sensitive. Treatment of 4 with KOCMe₃ causes decomposition to yield metal nanoparticles. Also, decomplexation of 4 takes place under H atm. to generate the carbene precursor, 1-(6-mesityl-2-picolyl)-3-mesitylimidazolium salt. Nevertheless, the Pd complex 4 shows good catalytic activity on the Suzuki-Miyaura and Mizoroki-Heck reactions.

Journal of Organometallic Chemistry published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C7H4ClIO2, HPLC of Formula: 89076-64-2.

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

Tang, Luning published the artcileSelective single C-F bond arylation of trifluoromethylalkene derivatives, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Chemical Science (2019), 10(37), 8701-8705, database is CAplus and MEDLINE.

A strategically novel single C-F bond functionalization of CF₃-derived mols., which shows a prominent advantage for the expedient construction of difluoromethylene-bridged organic scaffolds, is disclosed. The reported protocol consists of S_N2′ amination, N-alkylation and palladium-catalyzed allylic substitution reactions, which enables straightforward arylation and alkenylation of vinyltrifluoromethane derivatives Furthermore, this strategy is characterized by its broad substrate scope with respect to both CF₃-alkene and arylboronic acid derivatives

Chemical Science 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 C12H9N3O4, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

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

Gunaga, Prashantha published the artcileSelective I_Kur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide, HPLC of Formula: 636-73-7, the publication is Journal of Medicinal Chemistry (2017), 60(9), 3795-3803, database is CAplus and MEDLINE.

We have recently disclosed 5-phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (I) as a potent I_Kur current blocker with selectivity vs. hERG, Na and Ca channels and an acceptable preclin. PK profile. On further characterization in vivo, Compound I demonstrated an unacceptable level of brain penetration. In an effort to reduce the level of brain penetration while maintaining the overall profile, SAR was developed at the C2′ position for a series of close analogs by employing hydrogen bond donors. As a result, 5-(5-phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl)pyridine-3-sulfonamide (II) was identified as the lead compound in this series. Compound II showed robust effects in rabbit and canine pharmacodynamic models and an acceptable cross-species pharmacokinetic profile and was advanced as the clin. candidate. Further optimization of II to mitigate pH dependent absorption resulted in identification of the corresponding phosphoramide prodrug (29) with an improved solubility and pharmacokinetic profile.

Journal of Medicinal 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 C5H5NO3S, HPLC of Formula: 636-73-7.

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

Qiu, Zhi-Hui published the artcilecatena-Poly[[diaquamanganese(II)]-di-μ-pyridine-3-sulfonato-κ²N:O;κ²O:N], Quality Control of 636-73-7, the publication is Acta Crystallographica, Section E: Structure Reports Online (2008), 64(6), m765, m765/1-m765/7, database is CAplus and MEDLINE.

In the title polymeric complex, [Mn(C₅H₄NO₃S)₂(H₂O)₂]_n, the Mn atom is located on a center of inversion and is coordinated by two O atoms and two N atoms derived from four different pyridine-3-sulfonate (pySO₃) ligands, and two O atoms derived from two H₂O mols. in a distorted trans-N₂O₄ octahedral geometry. The metal atoms are bridged by the pySO₃ ligands to form a 1-dimensional chain. The chains are further connected into a three-dimensional architecture via H bonds. Crystallog. data and at. coordinates are given.

Acta Crystallographica, Section E: Structure Reports Online 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

Jiang, Lin published the artcileCRISPR activation of endogenous genes reprograms fibroblasts into cardiovascular progenitor cells for myocardial infarction therapy, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Molecular Therapy (2022), 30(1), 54-74, database is CAplus and MEDLINE.

Fibroblasts can be reprogrammed into cardiovascular progenitor cells (CPCs) using transgenic approaches, although the underlying mechanism remains unclear. We determined whether activation of endogenous genes such as Gata4, Nkx2.5, and Tbx5 can rapidly establish autoregulatory loops and initiate CPC generation in adult extracardiac fibroblasts using a CRISPR activation system. The induced fibroblasts (>80%) showed phenotypic changes as indicated by an Nkx2.5 cardiac enhancer reporter. The progenitor characteristics were confirmed by colony formation and expression of cardiovascular genes. Cardiac sphere induction segregated the early and late reprogrammed cells that can generate functional cardiomyocytes and vascular cells in vitro. Therefore, they were termed CRISPR-induced CPCs (ciCPCs). Transcriptomic anal. showed that cell cycle and heart development pathways were important to accelerate CPC formation during the early reprogramming stage. The CRISPR system opened the silenced chromatin locus, thereby allowing transcriptional factors to access their own promoters and eventually forming a pos. feedback loop. The regenerative potential of ciCPCs was assessed after implantation in mouse myocardial infarction models. The engrafted ciCPCs differentiated into cardiovascular cells in vivo but also significantly improved contractile function and scar formation. In conclusion, multiplex gene activation was sufficient to drive CPC reprogramming, providing a new cell source for regenerative therapeutics.

Molecular Therapy 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, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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