Day: November 7, 2022

On December 1, 1995, Tanaka, Shunitz; Kodama, Kokoro; Kaneta, Takashi; Nakamura, Hiroshi published an article.Application In Synthesis of Pyridine-3-sulfonic acid The title of the article was Migration behavior of niacin derivatives in capillary electrophoresis. And the article contained the following:

The migration behavior of niacin derivatives was investigated by capillary zone electrophoresis (CZE) and micellar electrokinetic chromatog. (MEKC). When the pH of the buffer solution is lower than the pKa of the pyridine ring in the niacin derivatives, they are pos. charged by protonation on the pyridine ring and migrate electrophoretically. The mobilities of niacin derivatives in CZE were controlled by the pH of the migrating buffer. Good separation of 13 niacin derivatives was achieved at pH 2.8. Further, to shorten the anal. time and to achieve a more complete separation, an investigation by MEKC using SDS micelles was performed. All 13 niacin derivatives were eluted within 30 min and a satisfactory separation was achieved. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Application In Synthesis of Pyridine-3-sulfonic acid

The Article related to niacin derivative migration capillary zone electrophoresis, micellar electrokinetic chromatog niacin derivative, Biochemical Methods: Electrical and other aspects.Application In Synthesis of Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 30, 2011, Borkar, Nitin; Sawant, Sakshi published an article.Application of 132-20-7 The title of the article was Review of simultaneous determination of analytes by high performance liquid chromatography (HLPC) in multicomponent cough and cold oral drug products. And the article contained the following:

A review. The objective of this article is to review the methodologies of determination of the most widely used analytes in cough and cold preparations by HPLC. This article studies the effect of all chromatog. parameters so as to provide a fast, reliable and cost effective methodol. of testing. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Application of 132-20-7

The Article related to review cough cold oral drug analysis hplc, Pharmaceutical Analysis: Reviews and other aspects.Application of 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 31, 1991, Kaczmarek, Lukasz; Nantka-Namirski, Pawel; Klodzinska, Aleksandra; Bujak, Barbara; Tatarczynska, Ewa published an article.Name: [2,2′-Bipyridine]-3,3′-diamine The title of the article was Synthesis and pharmacological properties of some dipyrido[1,3]diazepinones. And the article contained the following:

The synthesis of two isomeric dipyrido[1,3]diazepinones (I and II, R = e.g., Bu, 3-dimethylaminopropyl) and N-monosubstituted derivatives of I by cyclocondensation of corresponding bipyridinediamines with urea was described. The alkylation of these compounds with alkyl halides in K2CO3/DMF/TBAB system gave N,N’-disubstituted compounds Dipyrido[1,3]diazepinones and I showed a weak general depressive action on the central nervous system and they were also devoid of antidepressant, anxiolytic, anticonvulsant and serotoninolytic or serotoninomimetic properties. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Name: [2,2′-Bipyridine]-3,3′-diamine

The Article related to dipyridodiazepinone pharmacol preparation, Pharmacology: Structure-Activity and other aspects.Name: [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pandey, Ajay Kumar; Dwivedi, Dharmendra published an article in 2017, the title of the article was A validated titrimetric method for the determination of pheniramine maleate in pure form and in their pharmaceutical formulation.SDS of cas: 132-20-7 And the article contains the following content:

A simple, convenient and accurate visual titrimetric method for the determination of Pheniramine maleate (PM) in pure form and in their pharmaceutical formulations Avil (tablet and injection) using Pyridinium fluoro chromate (PFC) as an oxidant is described. The titrimetric method is based on the oxidation of the drugs in sulfuric acid medium by known excess of Pyridinium fluoro chromate and iodometric determination of the unreacted Pyridinium fluoro chromate (PFC). To examine the accuracy and precision of results percentage error, standard deviation (SD) and coefficient of variation (CV) were also calculated for each sample. Proposed method was validated by recovery anal. by drug addition method of drug. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).SDS of cas: 132-20-7

The Article related to pheniramine maleate avil tablet titrimetry, Pharmaceutical Analysis: General and other aspects.SDS of cas: 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 31, 2004, Crider, A. M.; Liu, S.; Li, T.; Mahajan, S.; Ankersen, M.; Stidsen, C. E. published an article.Category: pyridine-derivatives The title of the article was Somatostatin receptor subtype 4 (sst4) ligands: Synthesis and evaluation of indol-3-yl- and 2-pyridyl-thioureas. And the article contained the following:

Thiourea analogs of NNC 26-9100 (2) were prepared as somatostatin receptor subtype 4 (sst4) ligands. The indole 9 exhibited high affinity (Ki = 23 nM) and about a 100-fold selectivity at sst4 compared to sst2 receptors. The (imidazol-4-yl) Pr group appears to play a major role in the affinity and selectivity of these thioureas at sst4. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Category: pyridine-derivatives

The Article related to somatostatin receptor sst4 thiourea ligand, Pharmacology: Structure-Activity and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 31, 1996, Lombardini, John B. published an article.Safety of Pyridine-3-sulfonic acid The title of the article was Quantitative analysis of the combination dose-effects of taurine and taurine analogs on the phosphorylation of an ∼44-Kd protein present in a mitochondrial subfraction of rat heart. And the article contained the following:

Combinations of taurine and analogs of taurine that partially contain the N-C-C-S moiety within a semirigid saturated ring structure were tested for their effects on the phosphorylation of an ∼44-Kd protein present in the mitochondrial fraction of rat heart. (±)-Piperidine-3-sulfonic acid (PiP), an inhibitor of the phosphorylation of the ∼44-Kd protein with activity approx. similar to that of taurine, was observed to be mutually exclusive with taurine, i.e., to have a similar mode of action. The combination of taurine plus PiP in a fixed ratio mixture of 1:1 was slightly antagonistic at all concentrations (±)-Aminotetrahydrothiopyran-1,1-dioxide (APS), a sulfone derivative of taurine with a net pos. charge, also has approx. the same inhibitory activity as taurine. However, APS was mutually nonexclusive with taurine when tested in combination and thus appears to act independently of taurine. Taurine plus APS in a fixed ratio mixture of 3:1 was highly antagonistic at low concentrations of the mixture, approached an additive relation at 50% saturation, and became synergistic at high concentrations of the mixture Three analogs of taurine, pyridine-3-sulfonic acid (PyS), quinoline-8-sulfonic acid (QS), and 2-aminobenzenesulfonic acid (ABS), that have the basic taurine structure (N-C-C-S) partially in a semirigid unsaturated ring structure stimulate the phosphorylation of the ∼44-Kd protein. Due to the unsaturated ring structure, these analogs of taurine have a net neg. charge at physiol. pH and are not zwitterions. When PyS, QS, or ABS was titrated in the presence of a fixed concentration of taurine (10 mM), there was a competitive relation even through their electronic nature is quite different than that of taurine. The combination of QS plus PyS (1:5) appears to progress through a transition from being synergistic at low concentrations of the fixed ratio mixture, additive at 50% saturation, and finally antagonistic at high concentration of the fixed ratio mixture The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Safety of Pyridine-3-sulfonic acid

The Article related to taurine analog heart protein structure activity, Pharmacology: Structure-Activity and other aspects.Safety of Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 10, 2020, Smil, David; Wong, Jong Fu; Williams, Eleanor P.; Adamson, Roslin J.; Howarth, Alison; McLeod, David A.; Mamai, Ahmed; Kim, Soyoung; Wilson, Brian J.; Kiyota, Taira; Aman, Ahmed; Owen, Julie; Poda, Gennady; Horiuchi, Kurumi Y.; Kuznetsova, Ekaterina; Ma, Haiching; Hamblin, J. Nicole; Cramp, Sue; Roberts, Owen G.; Edwards, Aled M.; Uehling, David; Al-awar, Rima; Bullock, Alex N.; O’Meara, Jeff A.; Isaac, Methvin B. published an article.Recommanded Product: 3,5-Dibromo-4-methoxypyridine The title of the article was Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. And the article contained the following:

There are currently no effective chemotherapeutic drugs approved for the treatment of diffuse intrinsic pontine glioma (DIPG), an aggressive pediatric cancer resident in the pons region of the brainstem. Radiation therapy is beneficial but not curative, with the condition being uniformly fatal. Anal. of the genomic landscape surrounding DIPG has revealed that activin receptor-like kinase-2 (ALK2) constitutes a potential target for therapeutic intervention given its dysregulation in the disease. An open science approach has been adopted to develop a series of potent, selective, orally bioavailable, and brain-penetrant ALK2 inhibitors based on the lead compound LDN-214117. Modest structural changes to the C-3, C-4, and C-5 position substituents of the core pyridine ring afforded compounds M4K2009, M4K2117, and M4K2163, each with a superior potency, selectivity, and/or blood-brain barrier (BBB) penetration profile. Robust in vivo pharmacokinetic (PK) properties and tolerability mark these inhibitors as advanced preclin. compounds suitable for further development and evaluation in orthotopic models of DIPG. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Recommanded Product: 3,5-Dibromo-4-methoxypyridine

The Article related to preparation alk2 inhibitor diffuse intrinsic pontine glioma, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 30, 2018, Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J. L.; Laraia, Luca; Waldmann, Herbert published an article.Name: 3,5-Dibromo-4-methoxypyridine The title of the article was Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors. And the article contained the following:

Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small mol. modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biol. validation experiments indicated that the mode of action was upstream or independent of mTOR. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).Name: 3,5-Dibromo-4-methoxypyridine

The Article related to dimethoxy pyridine derivative preparation autophagy inhibitor structure, Pharmacology: Structure-Activity and other aspects.Name: 3,5-Dibromo-4-methoxypyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Marugan, Juan Jose; Huang, Wenwei; Motabar, Omid; Zheng, Wei; Xiao, Jingbo; Patnaik, Samarjit; Southall, Noel; Westbroek, Wendy; Lea, Wendy A.; Simeonov, Anton; Goldin, Ehud; DeBernardi, Maria A.; Sidransky, Ellen published an article in 2012, the title of the article was Non-iminosugar glucocerebrosidase small molecule chaperones.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine And the article contains the following content:

Small mol. chaperones are a promising therapeutic approach for the Lysosomal Storage Disorders (LSDs). Here, we report the discovery of a new series of non-iminosugar glucocerebrosidase inhibitors with chaperone capacity, and describe their structure-activity relationship (SAR), selectivity, cell activity and pharmacokinetics. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to glucocerebrosidase inhibitor chaperone pharmacokinetics brain ml156 msbar, Pharmacology: Structure-Activity and other aspects.Recommanded Product: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 1, 2018, Shinozuka, Tsuyoshi; Tsukada, Tomoharu; Fujii, Kunihiko; Tokumaru, Eri; Shimada, Kousei; Onishi, Yoshiyuki; Matsui, Yumi; Wakimoto, Satoko; Kuroha, Masanori; Ogata, Tsuneaki; Araki, Kazushi; Ohsumi, Jun; Sawamura, Ryoko; Watanabe, Nobuaki; Yamamoto, Hideki; Fujimoto, Kazunori; Tani, Yoshiro; Mori, Makoto; Tanaka, Jun published an article.Safety of 4-Chloro-2,6-difluoropyridine The title of the article was Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization. And the article contained the following:

Attempts were made to reduce the lipophilicity of previously synthesized compound (II) for the avoidance of hepatotoxicity. The replacement of the left-hand side benzene with 2-pyridine resulted in the substantial loss of potency. Because poor membrane permeability was responsible for poor potency in vitro, the adjustment of lipophilicity was examined, which resulted in the discovery of di-Me pyridine derivative (I, DS-6930). In preclin. studies, DS-6930 demonstrated high PPARγ agonist potency with robust plasma glucose reduction DS-6930 maintained diminished PPARγ-related adverse effects upon toxicol. evaluation in vivo, and demonstrated no hepatotoxicity. Cofactor recruitment assay showed that several cofactors, such as RIP140 and PGC1, were significantly recruited, whereas several canonical factors was not affected. This selective cofactor recruitment was caused due to the distinct binding mode of DS-6930. The calcium salt, DS-6930b, which is expected to be an effective inducer of insulin sensitization without edema, could be evaluated clin. in T2DM patients. The experimental process involved the reaction of 4-Chloro-2,6-difluoropyridine(cas: 34968-33-7).Safety of 4-Chloro-2,6-difluoropyridine

The Article related to ds 6930 preparation ppar modulator diabetes, benzimidazole, ds-6930, pparγ, Pharmacology: Structure-Activity and other aspects.Safety of 4-Chloro-2,6-difluoropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem