Tag: 100-200

Sicho, Vladislav; Kralova, Blanka published an article in 1966, the title of the article was Influence of antivitamins on the microbiological biosynthesis of vitamins. II. Stimulation of nicotinic acid biosynthesis in the microorganism Saccharomyces cerevisiae by pyridine-3-sulfonic acid.Formula: C5H5NO3S And the article contains the following content:

The influence of the antivitamin of nicotinic acid (I), pyridine-3-sulfonic acid (II) on I biosynthesis in S. cerevisiae was investigated. II stimulated I synthesis 3-fold when added at 25 μg./100 g. nutrient media. The increased production of I probably results from the compensating response of the respective controlling systems to the competitive inhibition of the antivitamin. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Formula: C5H5NO3S

The Article related to saccharomyces nicotinic acid, nicotinic acid saccharomyces, pyridinesulfonate nicotinate yeast, yeast pyridinesulfonate nicotinate, antivitamin yeast nicotinate, saccharomyces and other aspects.Formula: C5H5NO3S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 16, 1971, Nicolson, Adrian published a patent.Application of 34968-33-7 The title of the patent was Chlorofluoropyridines. And the patent contained the following:

The title compounds were prepared by fluorination of chloropyridines with KF or NaF in a nonhydroxylic solvent, e.g. tetramethylene sulfone (I) or AcNMe2, in the presence of alcs., acids, or bases, e.g. MeOH, HO(CH2)2OH, glycerol, EtCO2H, or Bu3N. Thus, pentachloropyridine was added to KF (1:5.7 mole %) in I. ClCH2CO2H was added and the mixture refluxed 2 hr to give 79% fluorinated pyridines consisting of 3,5-dichlorotrifluoropyridine 97.5, pentafluoropyridine+3-chlorotetrafluoropyridine 2.2, and 3,5,6-tri-chlorodifluoropyridine 0.4%. Similarly prepared were 4-chloro-2-fluoro-, 2-chloro-4-fluoro-, 2,4-difluoro-, 6-chloro-2,4-difluoro,-and 4-chloro-2,6-difluoropyridine. The experimental process involved the reaction of 4-Chloro-2,6-difluoropyridine(cas: 34968-33-7).Application of 34968-33-7

The Article related to chlorofluoropyridine preparation, fluorochloropyridine preparation, pyridine chlorofluoro preparation, fluorination and other aspects.Application of 34968-33-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bernstein, Jack; Stearns, Barbara; Shaw, Elliott; Lott, W. A. published an article in 1947, the title of the article was Derivatives of 2,6-diaminopyridine.Related Products of 51566-22-4 And the article contains the following content:

Since 2,6-diaminopyridine (I) showed an appreciable antiparasitic activity when tested against Plasmodium lophurae in ducklings, various derivatives of I have been prepared to determine if further substitution in the mol. would increase the antiparasitic activity of the parent compound I (66 g.) in 300 cc. dioxane, treated dropwise with 23.5 g. AcCl in 50 cc. dioxane (0.5 h.) at 25-30° and stirred 2 addnl. hrs., gives 40% of the 2-Ac derivative (II), m. 156-7°; 2-butyryl derivative m. 152-3°, 25%; 2-salicyloyl derivative (prepared from o-AcOC6H4COCl and purified by precipitation from dilute HCl with dilute NaOH) m. 178-9°, 44%; 2-[phenyl(acetoxy)acetyl] derivative (as HCl salt with 1 mol. H2O) m. 151-3°, 23%. N,N’-Bis(6-amino-2-pyridyl)adipamide m. 228-9°, 72%; N,N’-bis(6-amino-2-pyridyl)sebacamide m. 152-5°, 55%. 1,3-Bis(6-amino-2-pyridyl)urea does not melt, 71%. (CH2CO)2O (30 g.) in 200 cc. dioxane, treated slowly with 33 g. I in 200 cc. dioxane and heated 3 h. on the steam bath, gives 57% N-(6-amino-2-pyridyl)succinamic acid, m. 174-5° (decomposition). I (46 g.) and 222 cc. AcCH2CO2Et, heated 15 min. at 160° and the product in EtOH treated with alc. HCl, give 40% 2,6-bis(acetylacetamido)pyridine-HCl, m. 195-8°; the filtrate yields 10% of the 2-acetylacetamido derivative, m. 146-7°. I (22 g.) and 22.6 g. NCCH2CO2Et, heated 2 h. at 165°, give 85% 2-amino-6-cyanoacetamidopyridine, m. 152-3°. 2-Acetamido-6-carbethoxyacetamidopyridine m. 150-1.5°, 41%. I (282 g.) and 290 g. HOCH2CO2H, fused 15 h. at 120° under reduced pressure, give 35% 2,6-bis(glycolylamino)pyridine, m. 220-1°. I (33 g.) in 200 cc. absolute EtOH containing 6.9 g. Na and 43 g. Et2NCH2CO2Et, refluxed 2 h., give 55% 2,6-bis(diethylaminoacetamido)pyridine, m. 109.5-10.5°. I (22 g.) and 27 g. AcNHCOCl, ground in a mortar and 35 cc. C5H5N added, give 19% 2,6-bis(acetamidoacetamido)pyridine, m. 260-1°. MeC(:NH)NH2.HCl (24.6 g.) in 100 cc. absolute EtOH, added to 22 g. I in 150 cc. absolute EtOH, stirred 3 h., and allowed to stand overnight at room temperature, give 38% N-(6-amino-2-pyridyl)acetamidine-HCl, m. 246-7° (decomposition). I (396 g.) in 8 l. H2O, treated dropwise with 195 g. ClCO2Et (3 h.), gives 76% 2-amino-6-carbethoxyaminopyridine (III), m. 109-12°. I (33 g.) in 500 cc. H2O, 200 cc. N HCl, and 300 g. ice, treated dropwise with 33 g. ClCO2Et, stirred 2 h., 200 cc. N HCl added, and the mixture allowed to stand overnight at 10°, gives 55% 2,6-bis(carbethoxyamino)pyridine, m. 132.5-3.5°, and 12 g. III. III (21.6 g.) in 120 cc. 3 N EtOH-NH3, heated 12 h. at 110°, gives 75% 2-amino-6-ureidopyridine, m. 175-6° (decomposition). I (48 g.) and 48 g. CO(NH2)2, heated 36 h. at 130°, give 49% 2,6-diureidopyridine, does not melt below 300° (purified by extraction with 300 cc. 3% HCl and crystallization of the residue from H2O). I (12 g.) in 1500 cc. C6H6, treated dropwise with 17.9 g. p-EtOC6H4NCO in 75 cc. C6H6, gives 86% 2-(p-ethoxyphenylureido)-6-aminopyridine, m. 168-9°; 2-(2-nitro-4-methoxyphenylureido)-6-aminopyridine m. 208-10°, 73%; reduction over Pt oxide gives 50% of the corresponding 2-(2-amino-4-methylphenylureido) derivative, m. 182-4°. I (154 g.) and 200 g. of the HCl salt of I, heated 12 h. at 190°, give 60% bis(6-amino-2-pyridyl)amine, m. 172-3° (the HCl salt does not melt). 2,6-Dibromopyridine (IV) (38 g.) and 160 cc. 25% aqueous MeNH2, heated 8 h. at 190°, give 59% 2,6-bis(methylamino)pyridine, m. 70-1°; this results in 20% yield from 27.6 g. 2-amino-6-bromopyridine (V) and 110 cc. 25% aqueous MeNH2 on heating 30 h. at 190°. V (80 g.) and 200 cc. EtNH2, heated 36 h. at 170-80°, give 81% 2-amino-6-(diethylamino)pyridine (VI), b4.5 122-3°, m. 34-5° (HCl salt, m. 143-4°). IV (45 g.) and 27.8 g. Et2NH in 100 cc. absolute EtOH, heated 8 h. at 170-80°, give 85% 2-bromo-6-(diethylamino)pyridine (VII), b4 97-9°; VII does not react with NH4OH (d. 0.9) at 170-80° (8 h.); 11 g. VII and 35 cc. 5 N EtOH-NH3, heated 25 h. at 170°, also did not react; 18.8 g. VII in 100 cc. NH4OH (d. 0.9) containing 1 g. CuSO4.5H2O, heated 30 h. at 140-5°, gives 44% VI. IV (35.6 g.) and 100 cc. Et2NH containing 4 cc. 25% CuSO4.5H2O, heated 30 h. at 160°, give 76% 2,6-bis(diethylamino)pyridine, b3 120-2° (HCl salt, m. 120-2°). 2-Amino-6-(3-diethylaminopropylamino)pyridine-HCl m. 65-75°, 53%; 2-acetamido-6-(4-diethylamino-1-methylbutylamino)pyridine m. 106-8° (51%). 2-Acetamido-6-(3-keto-1-methylbutylideneamino)-pyridine, 2,6-AcNHC5H3N(N:CMeCH2Ac), m. 146-7.5°, 40%. 2-Acetamido-6-(2,5-dimethyl-1-pyrryl)pyridine m. 147.5-8.5°, 54%. 2-Methoxy-6,9-dichloroacridine (11.2 g.) in 50 g. PhOH, warmed on the steam bath, treated with 11 g. I, and heated 3 h., gives 61% 2-methoxy-6-chloro-9-(6-amino-2-pyridylamino)acridine, yellow, m. 232-3°. II (30.2 g.), added in small portions to 100 cc. HNO3 (d. 1.5) at -5° to -2° and stirred an addnl. 30 min., gives 65% of the Ac derivative, decompose violently at 193°, of 2-nitramino-6-aminopyridine (VIII), darkens at 240-50° (hydrolysis by refluxing 1 h. with N NaOH); reduction of 15.4 g. VIII in 300 cc. 10% NaOH at 0-2° with 31 g. Zn gives 69% 2-hydrazino-6-aminopyridine, pale yellow, m. 93-4°; warmed 2 h. on the steam bath with AcCH2CO2Et (N atm.), there results 44% 1- (6-amino-2-pyridyl)-3-methyl-5-pyrazolone, m. 188-9.5°. 3-Methylpyridine (80 g.), 160 g. PhNMe2, and 144 g. NaNH2, heated 10 h. at 130-50° and 6 h. at 170-200°, give 4% 2,6-diamino-3-methylpyridine, m. 149-50°. 2,6-Dihydroxy-4-methylpyridine (9 g.) and 30 g. PBr3, heated 4.5 h. at 180°, give 36% 2,6-dibromo-4-methylpyridine, m. 74-5°; heated with NH4OH (d. 0.9) 27 h. at 195°, there results 71% 2,6-diamino-4-methylpyridine, m. 87-8°, which on sublimation m. 109-11° but reverts to the lower m.p. on standing. 2,6-Diamino-3-iodopyridine (23.5 g.) in 25 cc. AcOH and 35 cc. Ac2O, heated 1 h. on the steam bath, gives 33% of the di-Ac derivative, m. 210-11°. I (38 g.) in 550 cc. H2O, treated with 93 g. iodine and 93 g. KI in 150 cc. H2O, the mixture stirred 8 h., and allowed to stand overnight at room temperature, gives 36% 2,6-diamino-3,5-diiodopyridine-HCl, m. 160-5°; the free base m. 209-10°. 3-Methoxypyridine (IX) (15.8 g.) in 100 cc. concentrated H2SO4, treated dropwise (with cooling) with 25 cc. HNO3 (d. 1.6) and warmed 6 h. on the steam bath, gives 12.2 g. 3-methoxy-2,6-dinitropyridine (X), m. 114-15°. IX (57 g.), added to 130 cc. concentrated H2SO4 at 5°, the mixture treated with 70 cc. HNO3 (d. 1.6), and heated 1 h. on the steam bath, yields 38 g. 2-nitro-3-methoxypyridine (XI), m. 73-5°; 5 g. XI in 15 cc. concentrated H2SO4, treated with 4 cc. HNO3 (d. 1.6), gives 4.4 g. X. Catalytic reduction (Pt oxide) of 16.8 g. X in 500 cc. AcOH and 250 cc. Ac2O at room temperature (4 h.) gives 60% 3-methoxy-2,6-diacetamidopyridine, m. 173.5-4.5°. 2,3,6-Triaminopyridine-2HCl in 200 cc. H2O and 25 g. Ac2 in 200 cc. H2O, boiled 4 min., yield 98% 2,3-dimethyl-6-aminopyrido[2,3]pyrazine, m. 227-8°; 6-aminopyrido[2,3]pyrazine m. 267°, 62%. 2,3,6-Triaminopyridine oxalate (80 g.) in 150 cc. (CO2Et)2, heated 90 min. at 185°, gives 68% 2,3-dihydroxy-6-aminopyrido[2,3]pyrazine, does not m. below 300°. Addition of 23.8 g. 2,6-diacetamido-3-nitropyridine to 100 g. SnCl2.2H2O in 150 cc. concentrated HCl gives 26% 2-methyl-5-amino-1-imidazo[b]pyridine-HCl; neither the base nor the salt melts. I (55 g.) and 194 g. KCNS in 1 l. 95% AcOH, treated dropwise at -5° to -10° with 26 cc. Br, give 24% 2,5-diaminopyrido[2,3-d]thiazole (XII), m. 138-9°; II likewise gives the 5-Ac derivative of XII, m. 184-5°. I (66 g.) in 2 l. AcOH, treated with 460 g. KCNS in 100 cc. H2O and then at 0-3° with 64 cc. Br, with stirring 1 h. at room temperature, yields 22% 2,6-diaminopyrido[2,3-d,6,5-d’]bisthiazole, does not melt below 300°. I (25 g.), 29 g. I.HCl, and 42 g. benzoin, heated 1 h. at 185°, yield 89% 2,3-diphenyl-6-amino-1-pyrrolo[2,3-b]pyridine, m. 234.5-5.5°. 2-Amino-6-(3-keto-1-methylbutylideneamino)pyridine (16 g.) in 100 cc. 85% H3PO4, warmed 1 h. on the steam bath, gives 84% 2,4-dimethyl-7-amino-1,8-naphthyridine, m. 216-18°; this results in 85% yield from 5 g. I and 5 cc. CH2Ac2 in 25 cc. 85% H3PO4 on warming 30 min. on the steam bath. 2,7-Dihydrazino-4-methyl-1,8-naphthyridine-2HCl-2H2O (23 g.) and 18 g. AcCH2CO2Et in 200 cc. 50% EtOH, heated 5 min. at 70°, give 84% 2,7-bis(3-methyl-5-keto-1-pyrazolyl)-4-methyl-1,8-naphthyridine, m. 260-2°. The most active of these compounds (II, XII, and the di-Ac derivative of I) are only 1/3 as active as quinine as antiparasitic agents for Plasmodium lophurae in ducklings. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).Related Products of 51566-22-4

The Article related to aminopyridines, malaria and other aspects.Related Products of 51566-22-4

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

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

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

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

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

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

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