Day: November 7, 2022

Frosini, Maria; Sesti, Casilde; Saponara, Simona; Donati, Alessandro; Palmi, Mitri; Valoti, Massimo; Machetti, Fabrizio; Sgaragli, Gimpietro published an article in 2000, the title of the article was Effects of taurine and some structurally related analogues on the central mechanism of thermoregulation: A structure-activity relationship study.Category: pyridine-derivatives And the article contains the following content:

There is large body of evidences on the role of taurine in the central mechanisms of thermoregulation in mammals, but it is not clear, whether the hypothermic effect of taurine depends on its interaction with GABA receptors or with a specific receptor. In order to answer this question, the authors have performed a structure-activity relationship study by using both in vitro and in vivo preparations μM amounts of taurine or each of 20 analogs were injected intracerebroventricularly in conscious, restrained rabbits while rectal temperature was recorded. Receptor-binding studies, with synaptic membrane preparations from rabbit brain were used to determine the affinities of these compounds for GABAA and GABAB receptors. Furthermore, the interaction with presynaptic GABA and taurine uptake systems was studied using crude synaptosomal preparations from rabbit brain. Among the compounds tested, (±)-cis-2-aminocyclohexane sulfonic acid, induced hypothermia, but did not interact with GABAA and GABAB receptors neither did it affect GABA and taurine uptake, thus suggesting that its effect on body temperature is not mediated by the central GABA-ergic system. Interestingly, the trans-isomer was devoid of effects either in vivo or in vitro. In order to explain (±)-cis-2-aminocyclohexane sulfonic acid-induced hypothermia, a stereoscopic model was produced showing its possible interactions with a putative taurine brain receptor. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Category: pyridine-derivatives

The Article related to taurine structure activity thermoregulation brain, gaba taurine receptor thermoregulation brain, Pharmacology: Structure-Activity and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Balzarini, J.; De Clercq, E. published an article in 1982, the title of the article was Structure-function relationship of the antitumor cell activity of pyrimidine and pyridine derivatives.Recommanded Product: 73591-69-2 And the article contains the following content:

Fifty-two 2′-deoxyuridines, 10 2′-deoxycytidines, uracil arabinoside  [3083-77-0] and 7 analogs, cytosine arabinoside  [147-94-4] and 7 analogs, 5 nicotinic acid analogs, and 4 nicotinamide analogs were compared for their inhibitory effects on murine leukemia (L1210) cell growth. The most dramatic antitumor activity was demonstrated by the deoxyuridine analogs containing a small C5-substituent with high electron-withdrawing potency, i.e., F-, CF3-, ethynyl, or formyl. The deoxycytidine analogs were generally less active, with the 5-nitro- [69100-02-3] and 5-ethynyl [69075-47-4] analogs having the greatest effect. Of the 5-substituted uracil arabinosides, only the 5-Me analog [605-23-2] significantly inhibited L1210 growth. Cytosine arabinoside and its 5-fluoro analog [4298-10-6] were highly effective inhibitors. Of the nicotinic acid derivatives, only the m-propyl- [73591-68-1] and m-isopropyl [73591-69-2] derivatives showed weak antitumor activity. The meta- and para-alkylated nicotinamide derivatives also had weak activity. The experimental process involved the reaction of 5-Isopropylnicotinic acid(cas: 73591-69-2).Recommanded Product: 73591-69-2

The Article related to antitumor pyridine pyrimidine derivative structure, structure activity pyridine pyrimidine derivative, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 73591-69-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 19, 1998, Liu, Shenquan; Tang, Cheng; Ho, Bin; Ankersen, Michael; Stidsen, Carsten E.; Crider, A. Michael published an article.Synthetic Route of 199522-66-2 The title of the article was Nonpeptide Somatostatin Agonists with sst4 Selectivity: Synthesis and Structure-Activity Relationships of Thioureas. And the article contained the following:

Utilizing NNC 26-9100 as a structural lead, a variety of nonpeptide derivatives of somatostatin were synthesized and evaluated for sst2 and sst4 receptor binding affinity. A novel thiourea scaffold was utilized to attach (1) a heteroaromatic nucleus to mimic the Trp8 residue, (2) a nonheteroarom. nucleus to mimic Phe7, and (3) a primary amine or other basic group to mimic the Lys9 residue of somatostatin. Displacement studies were carried out using membranes from cell lines expressing ssts [BHK cells (sst4) and HEK 293 cells (sst2)] utilizing [125I]Tyr11-SRIF as the radioligand. Several thioureas and an urea derivative exhibited Ki values of less than 100 nM. Two thioureas and the urea derivative are believed to be the most potent nonpeptide sst4 agonists known with Ki of 6, 16, and 14 nM, resp. Since the thiourea and the urea derivatives exhibit high sst4 selectivity, these novel nonpeptide derivatives may be useful tools for studying the sst4 receptor. Studies are currently in progress to evaluate the therapeutic potential of NNC 26-9100 in the treatment of glaucoma. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Synthetic Route of 199522-66-2

The Article related to thiourea preparation structure somatostatin agonist, nnc26910 derivative somatostatin sst4 receptor agonist, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 199522-66-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 11, 2017, Gunaga, Prashantha; Lloyd, John; Mummadi, Somanadham; Banerjee, Abhisek; Dhondi, Naveen Kumar; Hennan, James; Subray, Veena; Jayaram, Ramya; Rajugowda, Nagendra; Umamaheshwar Reddy, Kommuri; Kumaraguru, Duraimurugan; Mandal, Umasankar; Beldona, Dasthagiri; Adisechen, Ashok Kumar; Yadav, Navnath; Warrier, Jayakumar; Johnson, James A.; Sale, Harinath; Putlur, Siva Prasad; Saxena, Ajay; Chimalakonda, Anjaneya; Mandlekar, Sandhya; Conder, MaryLee; Xing, Dezhi; Gupta, Arun Kumar; Gupta, Anuradha; Rampulla, Richard; Mathur, Arvind; Levesque, Paul; Wexler, Ruth R.; Finlay, Heather J. published an article.Name: Pyridine-3-sulfonic acid The title of the article was Selective IKur 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. And the article contained the following:

We have recently disclosed 5-phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (I) as a potent IKur 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. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Name: Pyridine-3-sulfonic acid

The Article related to ph quinazoline sulfonamide synthesis pharmacokinetics brain potassium channel herg, pyridine sulfonamide antiarrhythmic atrial fibrillation, Pharmacology: Structure-Activity and other aspects.Name: Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kawata, Tsutomu; Yamamoto, Motokazu; Yamana, Masao; Tajima, Moritaka; Nakano, Tomoyasu published an article in 1975, the title of the article was Characteristics of viologen derivatives for electrochromic display.Recommanded Product: 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide And the article contains the following content:

The polarog. half-wave potentials (E1/2, in aqueous solutions with pH 3.29 at 25°) and the absorption spectra (at λ = 250-700 nm) in various media (aqueous solution, MeOH, glycerin) were determined to characterize the electrochromic behavior of the viologen derivatives X-RN+C5H4-C5H4N+RX- [= Viol] (R = Pr, C6H13, or C7H15 for X = Br; X = Cl, Br, or I for R = PhCH2). Two polarog. waves were observed for each derivative: the 1st E1/2 [= 0.568-0.710 V vs. SCE] was attributed to the reduction, dication of Viol (I, colorless) + e- ⇄ radical cation (II, colored); and the 2nd E1/2 [= 0.775-0.965 V] was attributed to II + e- ⇄ biradical (III, colored). The E1/2 values were smaller for the PhCH2 derivatives than for the alkyl derivatives For R = PhCH2, the observed absorption maximum were at λ (in nm) ≈ 260 for I, ≈ 260, 400, and 630 for II, and ≈ 380 for III. With a viologen derivative in an electrochromic display device (having a transparent SnO2 cathode and a Pt anode), the writing time decreased with increasing applied voltage, and was ∼0.4-0.8 sec for obtaining a transmittance of 80%. An applied voltage greater than the 2nd E1/2 caused the color to change from purple to yellow; on open circuit, the color changed back to purple. The experimental process involved the reaction of 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide(cas: 52243-87-5).Recommanded Product: 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide

The Article related to viologen derivative polarog optical absorption, electrochromic display viologen derivative, Electric Phenomena: Other Devices and other aspects.Recommanded Product: 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Madura, J. D.; Lombardini, J. B.; Briggs, J. M.; Minor, D. L.; Wierzbicki, A. published an article in 1997, the title of the article was Physical and structural properties of taurine and taurine analogs.Formula: C5H5NO3S And the article contains the following content:

The inhibition of the phosphorylation of an ∼20kDa protein present in the mitochondrial fraction of the rat retina by taurine and taurine analogs was investigated using computational methods. Correlations between mol. weight, mol. volume, and calculated pKa values vs. IC50 values are reported. These data appear to support the hypotheses according to Lombardini and Props that the inhibition of the phosphorylation of an ∼20 kDa protein by taurine and taurine analogs dependent on (i) the critical distance between the N and S atoms in the taurine moiety (S-C-C-N) of the analog, (ii) the environment of the N atom in the taurine analog (saturated ring vs. unsaturated ring), and (iii) the placement of both the S and N atoms not being present simultaneously in the ring structure. Using computational methods results supporting hypotheses (i) and (ii) are presented. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Formula: C5H5NO3S

The Article related to taurine qsar protein phosphorylation inhibition retina, Mammalian Biochemistry: Metabolism and other aspects.Formula: C5H5NO3S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kelani, Khadiga M.; Hegazy, Maha A.; Hassan, Amal M.; Tantawy, Mahmoud A. published an article in 2021, the title of the article was Determination of naphazoline HCl, pheniramine maleate and their official impurities in eye drops and biological fluid rabbit aqueous humor by a validated LC-DAD method.COA of Formula: C20H24N2O4 And the article contains the following content:

A simple RP-HPLC-DAD method was developed and validated, as per the ICH guidelines, for simultaneous determination of naphazoline HCl (NPZ) & pheniramine maleate (PHN) along with three of their official impurities. Chromatog. separation was performed on a hypersil ODS column (5 mm, 250-4.6 mm i.d.) with isocratic elution using phosphate buffer pH 6.0: acetonitrile (70 : 30, volume/volume) as mobile phase, at a flow rate of 1.0 mL min-1 and UV detection at 260.0 nm. The developed method was found to be linear over the concentration ranges of 5.00-45.00 Μg mL-1 for NPZ and NPZ impurity B and 10.00-110.00 Μg mL-1, 10-70 Μg mL-1 and 10-120 Μg mL-1 for PHN, and PHN impurity A and B, resp., with correlation coefficient values <0.999 for the five cited compounds The method was confirmed to be accurate, robust and precise with RSD >2.0%. LOD and LOQ values for the five cited compounds were calculated Moreover, the method was also validated in rabbit aqueous humor as per the US food and drug administration (FDA) bioanal. validation guidelines. Finally, the proposed method was applied for the anal. of the two drugs along with their impurities in dosage form and spiked aqueous humor samples. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).COA of Formula: C20H24N2O4

The Article related to naphazoline hcl pheniramine maleate eye drop biol fluid, Biochemical Methods: Immunological and other aspects.COA of Formula: C20H24N2O4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 1, 2018, Le, Chip; Chen, Tiffany Q.; Liang, Tao; Zhang, Patricia; MacMillan, David W. C. published an article.Synthetic Route of 2229858-27-7 The title of the article was A radical approach to the copper oxidative addition problem: Trifluoromethylation of bromoarenes. And the article contained the following:

Transition metal-catalyzed arene functionalization was widely used for mol. synthesis over the past century. In this arena, copper catalysis has long been considered a privileged platform due to the propensity of high-valent copper to undergo reductive elimination with a wide variety of coupling fragments. However, the sluggish nature of oxidative addition has limited copper’s capacity to broadly facilitate haloarene coupling protocols. Here, this copper oxidative addition problem can be overcome with an aryl radical-capture mechanism, wherein the aryl radical was generated through a silyl radical halogen abstraction. This strategy was applied to a general trifluoromethylation of aryl bromides through dual copper-photoredox catalysis. Mechanistic studies support the formation of an open-shell aryl species. The experimental process involved the reaction of 4,4′-Bis(trifluoromethyl)-2,2′-bipyridinebis[3,5-difluoro-2-[5-methyl-2-pyridinyl)phenyl] iridium(III) hexafluorophosphate(cas: 2229858-27-7).Synthetic Route of 2229858-27-7

The Article related to copper oxidative addition trifluoromethylation bromoarene, Physical Organic Chemistry: General and other aspects.Synthetic Route of 2229858-27-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 18, 2020, Xia, Yanzhi; Long, Xiaojing; Jiang, Zhenjie; Li, Daohao; Ji, Quan; Quan, Fengyu; Wang, Bingbing published a patent.Recommanded Product: [2,2′-Bipyridine]-3,3′-diamine The title of the patent was Marine organism polysaccharide grafted pyridine organic micromolecule multicolor adjustable aggregation induced luminescent material and preparation method thereof. And the patent contained the following:

The invention relates to polysaccharide grafted pyridine organic micromol., the pyridine mols. are chem. cross-linked through Schiff base reactions to prepare multicolor tunable marine biopolysaccharide materials with aggregation-induced luminescence properties. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Recommanded Product: [2,2′-Bipyridine]-3,3′-diamine

The Article related to polysaccharide grafted pyridine organic luminescent material, Industrial Carbohydrates: Nonsugars and other aspects.Recommanded Product: [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 31, 1979, Nicholson, S. H.; Suckling, C. J.; Iversen, L. L. published an article.HPLC of Formula: 636-73-7 The title of the article was GABA analogs: conformational analysis of effects on [3H]GABA binding to postsynaptic receptors in human cerebellum. And the article contained the following:

A study of the inhibition of Na-independent 3H-labeled GABA [56-12-2] binding to synaptic membranes of human brain cortex by synthesized simple substituted GABA mols. and some related aromatic and heterocyclic amino acids showed that C-alkyl or -aryl substitution of the GABA mol. markedly reduced its ability to bind to the receptor. Rigid mols. were also unable to interact strongly with the receptor. The larger and more numerous the substituents, the weaker was the receptor binding of the GABA analog. For binding to the GABA receptor, the substituent blocked the approach of the charged atom of the ligand to its complementary site on the receptor, and also raised the energy of that conformation required for binding to the receptor. A planar, eclipsed, partially folded conformation must be adopted by GABA when it binds to its receptor. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).HPLC of Formula: 636-73-7

The Article related to gaba receptor structure activity, Pharmacodynamics: Structure-Activity and other aspects.HPLC of Formula: 636-73-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem