Tag: M.W=100-150

Ranjbar, Hoda; Soti, Monavareh; Janahmadi, Mahyar; Kohlmeier, Kristi A.; Sheibani, Vahid; Ahmadi-Zeidabadi, Meysam; Shabani, Mohammad published the artcile< Modulation of the CB1 cannabinoid receptor has potential therapeutic utility in the 3-acetylpyridine cerebellar ataxia rat model>, Formula: C7H7NO, the main research area is cannabinoid receptor acetylpyridine cerebellar ataxia therapeutic potential; CB1 receptor; Cannabinoid; Cerebellar ataxia; Purkinje cell.

Cerebellar ataxia is a neurodegenerative disorder leading to severe motor incoordination. Recently, it has been suggested that cannabinoids play a role in modulating ataxic symptoms. To understand the possible therapeutic effect of cannabinoids for the management of cerebellar ataxia, we used cannabinoid agonist/antagonists to target the cannabinoid type 1 receptor (CB1R) in the 3 acetyl pyridine (3AP) rat model of ataxia. The role of the CB1R was examined using three different doses of the CB1R agonist, WIN-55,212-2 (WIN; 0.1, 0.5, 1 mg/kg) administrated 30 min prior to 3AP (55 mg/kg, i.p.) which leads to motor impairment through destruction of the inferior olive. In some groups, the CB1R antagonist AM251 (1 mg/kg) was given in combination with WIN. Locomotor activity and motor coordination were impaired by 3AP, and the application of WIN did not ameliorate this effect. However, the abnormal gait, rearing and grooming caused by 3AP were prevented by co-administration of AM251 with WIN. While the addition of the CB1R antagonist improved some ataxic symptoms, there was no effect of AM251 on balance or locomotor activity when co-administrated with WIN. Behavioral testing indicated that not only did WIN fail to exert any protective effect on ataxic symptoms; it exacerbated ataxic symptoms, suggesting that CB1R agonists may not be the ideal therapeutic drug in this disorder. When taken together, the findings from the present study indicate that cannabinoid modulation of ataxia symptoms may not act solely through CB1Rs and other cannabinoid receptors should be considered in future studies.

Experimental Brain Research published new progress about Cannabinoid receptor 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Formula: C7H7NO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mikle, Gabor; Bede, Fanni; Kollar, Laszlo published the artcile< Synthesis of N-picolylcarboxamides in aminocarbonylation>, Quality Control of 3731-53-1, the main research area is picolylcarboxamide preparation; iodocamphene steroidal iodoalkene picolylamine aminocarbonylation palladium catalyst.

Palladium-catalyzed aminocarbonylation of iodocamphene and steroidal iodoalkenes was carried out in the presence of 2-, 3- and 4-picolylamine, as well as secondary amines possessing 1-picolyl substituent. In general, primary picolylamines require less than 2 h to achieve practically complete conversion. The secondary amines proved to be less reactive, requiring 6-24 h depending on the substrate structure. The corresponding carboxamides were isolated in moderate to excellent yields. The synthesis of α,β-unsaturated carboxamides is based on the synthesis of iodoalkene substrates from enolizable ketones.

Tetrahedron published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Xiaotong; Ke, Weijun; Traore, Boubacar; Guo, Peijun; Hadar, Ido; Kepenekian, Mikael; Even, Jacky; Katan, Claudine; Stoumpos, Constantinos C.; Schaller, Richard D.; Kanatzidis, Mercouri G. published the artcile< Two-Dimensional Dion-Jacobson Hybrid Lead Iodide Perovskites with Aromatic Diammonium Cations>, Reference of 3731-53-1, the main research area is aminomethylpyridinium methylammonium lead iodide perovskite luminescence crystal structure.

Two-dimensional (2D) halide perovskites have extraordinary optoelectronic properties and structural tunability. Among them, the Dion-Jacobson phases with the inorganic layers stacking exactly on top of each other are less explored. Two-dimensional (2D) Dion-Jacobson halide perovskites are presented, which adopt the general formula of A’An-1PbnI3n+1 (A’ = 4-(aminomethyl)pyridinium (4AMPY), A = methylammonium (MA), n = 1-4). By modifying the position of the CH2NH3+ group from 4AMPY to 3AMPY (3AMPY = 3-(aminomethyl)pyridinium), the stacking of the inorganic layers changes from exactly eclipsed to slightly offset. The perovskite octahedra tilts are also different between the 2 series, with the 3AMPY series exhibiting smaller bandgaps than the 4AMPY series. Compared to the aliphatic cation of the same size (AMP = (aminomethyl)piperidinium), the aromatic spacers increase the rigidity of the cation, reduce the interlayer spacing, and decrease the dielec. mismatch between inorganic layer and the organic spacer, showing the indirect but powerful influence of the organic cations on the structure and consequently on the optical properties of the perovskite materials. All A’An-1PbnI3n+1 compounds exhibit strong luminescence (PL) at room temperature Preliminary solar cell devices based on the n = 4 perovskites as absorbers of both series exhibit promising performances, with a champion power conversion efficiency (PCE) of 9.20% for (3AMPY)(MA)3Pb4I13-based devices, which is higher than the (4AMPY)(MA)3Pb4I13 and the corresponding aliphatic analog (3AMP)(MA)3Pb4I13-based ones.

Journal of the American Chemical Society published new progress about Band gap. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Reference of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dabaghian, Farid; Khanavi, Mahnaz; Zarshenas, Mohammad M. published the artcile< Bioactive compounds with possible inhibitory activity of Angiotensin-Converting Enzyme-II; a gate to manage and prevent COVID-19>, Synthetic Route of 3731-53-1, the main research area is covid19 virus angiotensin converting enzyme II review.

A review. This letter to the editor looks at bioactive compounds with possible inhibitory activity of Angiotensin-Converting Enzyme-II.

Medical Hypotheses published new progress about COVID-19. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Synthetic Route of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Spinner, E.; White, J. C. B. published the artcile< The spectra and structures of the cations and anions of substituted 2-hydroxypyridines (1,2-dihydro-2-oxopyridines)>, COA of Formula: C6H6ClNO, the main research area is .

The ir spectra of the hydrochlorides and hexachloroantimonates of 2-hydroxy- and 2-methoxypyridines containing substituents (3-, 4-, 5-, and 6-Me; 3- and 5-halo, and 3,5-dihalo; 6-OH) and the uv spectra of the cations have been determined The former cations are 2-hydroxypyridinium ions. H-bonding by the 2-OH proton seems to be responsible for the abnormally high ir intensity of the skeletal stretching band near 1640 cm.-1, which, in the past, caused it to be mistaken for a carbonyl stretching band. The ir, uv, and, where possible, Raman spectra of the Na salts of the above substituted 2-hydroxy-pyridines have also been determined The anions seem to have normal pyridoxide structures, with the neg. charge mainly on the O atom. 24 references

Journal of the Chemical Society [Section] B: Physical Organic published new progress about IR spectra. 13472-84-9 belongs to class pyridine-derivatives, and the molecular formula is C6H6ClNO, COA of Formula: C6H6ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhao, Zean; Liu, Jin; Kuang, Peihua; Luo, Jian; Surineni, Goverdhan; Cen, Xiaolin; Wu, Ting; Cao, Ying; Zhou, Pingzheng; Pang, Jianxin; Zhang, Qun; Chen, Jianjun published the artcile< Discovery of novel verinurad analogs as dual inhibitors of URAT1 and GLUT9 with improved Druggability for the treatment of hyperuricemia>, Recommanded Product: 4-Chloro-3-hydroxypyridine, the main research area is hyperuricemia URAT1 GLUT9 verinurad druggability pharmacokinetics oral bioavailability; Dual inhibitors; GLUT9; URAT1; Verinurad; anti-hyperuricemic.

Verinurad (RDEA3170) is a selective URAT1 inhibitor under investigation for the treatment of gout and hyperuricemia. In an effort to further improve the pharmacodynamics/pharmacokinetics of verinurad and to increase the structural diversity, we designed novel verinurad analogs by introducing a linker (e.g. aminomethyl, amino or oxygen) between the naphthalene and the pyridine ring to increase the flexibility. These compounds were synthesized and tested for their in vitro URAT1-inhibitory activity. Most compounds exhibited potent inhibitory activities against URAT1 with IC50 values ranging from 0.24 μM to 16.35 μM. Among them, compound KPH2f exhibited the highest URAT1-inhibitory activity with IC50 of 0.24 μM, comparable to that of verinurad (IC50 = 0.17 μM). KPH2f also inhibited GLUT9 with an IC50 value of 9.37 ± 7.10 μM, indicating the dual URAT1/GLUT9 targeting capability. In addition, KPH2f showed little effects on OAT1 and ABCG2, and thus was unlikely to cause OAT1/ABCG2-mediated drug-drug interactions and/or to neutralize the uricosuric effects of URAT1/GLUT9 inhibitors. Importantly, KPH2f (10 mg/kg) was equally effective in reducing serum uric acid levels and exhibited higher uricosuric effects in a mice hyperuricemia model, as compared to verinurad (10 mg/kg). Furthermore, KPH2f demonstrated favorable pharmacokinetic properties with an oral bioavailability of 30.13%, clearly better than that of verinurad (21.47%). Moreover, KPH2f presented benign safety profiles without causing hERG toxicity, cytotoxicity in vitro (lower than verinurad), and renal damage in vivo. Collectively, these results suggest that KPH2f represents a novel, safe and effective dual URAT1/GLUT9 inhibitor with improved druggabilities and is worthy of further investigation as an anti-hyperuricemic drug candidate.

European Journal of Medicinal Chemistry published new progress about ATP-binding cassette transporter ABCG2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Recommanded Product: 4-Chloro-3-hydroxypyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Heusler, Arne; Fliege, Julian; Wagener, Tobias; Glorius, Frank published the artcile< Substituted Dihydropyridine Synthesis by Dearomatization of Pyridines>, Synthetic Route of 93-60-7, the main research area is dihydropyridine preparation regioselective; pyridine triflic anhydride dearomatization trimethylamine borane; phenyl chloroformate pyridine dearomatization trimethylamine borane; boranes; chemoselectivity; nitrogen heterocycles; reduction; synthetic methods.

The synthesis of a broad variety of N-substituted 1,4-dihydropyridines I [R = H, 3-Me, 3,5-di-Br, etc.; R1 = Tf, CO2Ph] and 1,2-dihydropyridines II [R2 = F, Cl, CF3, Ph, SPh; R3 = H, F, trimethylsilyl] by very mild and selective reduction with amine borane was reported for the first time.

Angewandte Chemie, International Edition published new progress about Dearomatization. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Synthetic Route of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mowat, Jeffrey; Ehrmann, Alexander H. M.; Christian, Sven; Sperl, Carolyn; Menz, Stephan; Guenther, Judith; Hillig, Roman C.; Bauser, Marcus; Schwede, Wolfgang published the artcile< Identification of the Highly Active, Species Cross-Reactive Complex I Inhibitor BAY-179>, Recommanded Product: 5-Fluoropyridine-2,3-diamine, the main research area is BAY179 complex I inhibitor anticancer amide isostere.

Mitochondria are key regulators of energy supply and cell death. Generation of ATP within mitochondria occurs through oxidative phosphorylation (OXPHOS), a process which utilizes the four complexes (complex I-IV) of the electron transport chain and ATP synthase. Certain oncogenic mutations (e.g., LKB1 or mIDH) can further enhance the reliance of cancer cells on OXPHOS for their energetic requirements, rendering cells sensitive to complex I inhibition and highlighting the potential value of complex I as a therapeutic target. Herein, we describe the discovery of a potent, selective, and species cross-reactive complex I inhibitor. A high-throughput screen of the Bayer compound library followed by hit triaging and initial hit-to-lead activities led to a lead structure which was further optimized in a comprehensive lead optimization campaign. Focusing on balancing potency and metabolic stability, this program resulted in the identification of BAY-179, an excellent in vivo suitable tool with which to probe the biol. relevance of complex I inhibition in cancer indications.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Recommanded Product: 5-Fluoropyridine-2,3-diamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Beak, Peter; Covington, Johnny B.; White, J. Matthew published the artcile< Quantitative model of solvent effects on hydroxypyridine-pyridone and mercaptopyridine-thiopyridone equilibriums: correlation with reaction-field and hydrogen-bonding effects>, Quality Control of 73018-09-4, the main research area is tautomerism pyridone hydroxypyridine; mercaptopyridone thiopyridone tautomerism; solvent effect tautomerization.

A model for the effect of reaction field and H bonding on the relative energies of protomers is applied to the equilibrium between 6-chloro-2-hydroxypyridine and 6-chloro-2-pyridone, 2-mercaptopyridine and 2-thiopyridone, 6-chloro-2-mercaptopyridine and 6-chloro-2-thiopyridone, and 4-mercaptopyridine and 4-thiopyridone in a wide range of solvents. Quant. correlation is obtained by a multivariable anal. In addition to satisfactory statistical tests of the correlation, estimates of the difference in free energies between the isomers in the vapor phase and of the dipole moment component of the reaction-field term are obtained which compare well with the available independent values. These criteria are shown to signal an unacceptable correlation for the case of 2-chloro-4-hydroxypyridine and 2-chloro-4-pyridone. The advantage of this model, which provides an understanding of the effect of mol. environment on protomeric equilibrium in terms of reasonable phys. interactions, over empirical approaches is noted.

Journal of Organic Chemistry published new progress about Free energy. 73018-09-4 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Quality Control of 73018-09-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sepehri, Nima; Khoshneviszadeh, Mehdi; Farid, Sara Moghadam; Moayedi, Seyedeh Sara; Asgari, Mohammad Sadegh; Moazzam, Ali; Hosseini, Samanesadat; Adibi, Hossein; Larijani, Bagher; Pirhadi, Somayeh; Attarroshan, Mahshid; Sakhteman, AmirHossein; Kabiri, Maryam; Hamedifar, Haleh; Iraji, Aida; Mahdavi, Mohammad published the artcile< Design, synthesis, biological evaluation, and molecular docking study of thioxo-2,3-dihydroquinazolinone derivative as tyrosinase inhibitors>, Related Products of 3731-53-1, the main research area is thioxo dihydroquinazolinone preparation antioxidant docking tyrosinase inhibitor.

In this study, a series of thioxo-dihydroquinazolinone compounds I (R1 = i-Pr, Ph, pyridin-3-ylmethyl, cyclopentyl, etc.) were designed and synthesized as tyrosinase inhibitors. Among the investigated compounds, I (R1 = i-Pr (III)) demonstrated the best inhibitory activity with an IC50 value of 15.48μM compared to kojic acid as a pos. control with IC50 value of 9.30μM. In kinetic evaluation against tyrosinase, (III) depicted a mixed inhibition pattern. Addnl., antioxidant evaluations exhibited moderate to weak potency in 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The detailed interactions and binding mode toward tyrosinase of the most potent derivative were explicated by mol. docking study. Moreover, the computer-aided drug-likeness and pharmacokinetic studies were also carried out.

Journal of Molecular Structure published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Related Products of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem