Category: pyridine-derivatives

On September 5, 2013, Musdal, Yaman; Hegazy, Usama M.; Aksoy, Yasemin; Mannervik, Bengt published an article.Reference of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate The title of the article was FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1. And the article contained the following:

Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compounds used for other indications would be a shortcut to clin. applications and a search for GST P1-1 inhibitors among approved drugs and other compounds was therefore conducted. We tested 1040 FDA-approved compounds as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC50 values in the low micromolar range. For comparison, these compounds were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione saturation of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compounds investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Reference of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

The Article related to recombinant glutathione transferase p11 inhibitor adjuvant chemotherapy, adjuvant chemotherapeutics, enzyme inhibition, ethacrynic acid, fda-approved drugs, glutathione transferase p1-1 and other aspects.Reference of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 9, 2003, Rist, Oystein; Hogberg, Thomas; Holst Lange, Birgitte; Schwartz, Thue W.; Elling, Christian E. published a patent.Computed Properties of 75449-26-2 The title of the patent was Use of metal ion chelates in validating biological molecules as drug targets in test animal models. And the patent contained the following:

The invention discloses the use of chem. compounds or selections of chem. compounds (libraries) of the general Formula R1XFY(R1)GZR1 [F, G = N, O, S, Se, P; X, Y, Z = (un)branched C1-12 alkyl, aryl, heteroaryl, etc.; R1 = ABC; A = coupling or connecting moiety; B = spacer moiety; C = functional group] for in vivo methods for testing or validating the physiol. importance and/or the therapeutic or pharmacol. potential of biol. target mols., notably proteins such as, e.g., receptors and especially 7TM receptors in test animals expressing the biol. target mol. with, notably, a silent, engineered metal ion site. Use of specific metal ion binding sites of a generic nature in specific biol. target mols. such as, e.g. transmembrane proteins wherein the metal ion binding site is capable of forming a complex with a metal ion is also described. Also disclosed are chem. compounds or libraries suitable for use in methods for improving the in vivo pharmacokinetic behavior of metal ion chelates (e.g. the absorption pattern, the plasma half-life, the distribution, the metabolism and/or the elimination of the metal ion chelates). In order to improve the efficacy of the impact of the metal ion chelate on the biol. target mol. after administration of the metal ion chelate in vivo to a test animal, it is advantageous e.g. to increase the period during which the metal ion chelate is in the circulatory system and/or localized at the target. Further disclosed are metal ion-chelating compounds designed to be suitable for use in a target validation process according to the invention, as well as libraries of at least two or more of such metal ion-chelating compounds The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Computed Properties of 75449-26-2

The Article related to metal chelate drug screening target validation, protein target drug screening metal chelate, receptor target drug screening metal chelate, pharmacokinetics metal chelate drug screening and other aspects.Computed Properties of 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Padivitage, Nilusha L.; Smuts, Jonathan P.; Breitbach, Zachary S.; Armstrong, Daniel W.; Berthod, Alain published an article in 2015, the title of the article was Preparation and Evaluation of HPLC Chiral Stationary Phases Based on Cationic/Basic Derivatives of Cyclofructan 6.Category: pyridine-derivatives And the article contains the following content:

The cyclofructan 6 (CF6) macrocyclic-oligosaccharide was derivatized with five different substituents able to bear pos. charges: Pr imidazole, Me benzimidazole, di-Me aminopropyl, pyridine, and di-Me aminophenyl. The derivatized cyclofructans were reacted with triethoxysilyl-propylisocyanate as a linker to bond them to 5μm spherical silica gel particles and then used to prepare liquid chromatog. columns. The bonded silica particles were analyzed to establish the bonding densities. A set of 34 chiral compounds including acids, neutral compounds, and bases was tested with nine different mobile phase compositions including two reverse phase (RP) acetonitrile/pH 4 buffer, three polar organic (PO) acetonitrile/methanol, and four normal phase (NP) heptane/ethanol mobile phases. No compounds could be separated in the RP mode. Eight compounds only could be enantiosepd. in the PO mode and 21 compounds in the NP mode. The most effective chiral stationary phase was the Pr imidazole derivatized CF6 phase, provided no more than six imidazole substituents and two linkers are attached per CF6 unit. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Category: pyridine-derivatives

The Article related to cyclofructan cationic derivative hplc chiral stationary phase enantiomer separation, liquid chromatography, cationic derivatives, chiral separation, cyclofructan, enantiomer separation and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 30, 2019, Silverblatt, Joshua A.; Ziff, Oliver J.; Dancy, Luke; Daniel, Allen; Carter, Ben; Scott, Paul; Sado, Daniel M.; Shah, Ajay; Bromage, Daniel I. published an article.Synthetic Route of 132-20-7 The title of the article was Therapies to limit myocardial injury in animal models of myocarditis: a systematic review and meta-analysis. And the article contained the following:

Meta-anal. of current myocarditis guidelines do not advocate treatment to prevent myocardial injury and scar deposition in patients with myocarditis and normal left ventricular ejection fraction. We aimed to ascertain the utility of beta blockers, calcium channel blockers and antagonists of the renin-angiotensin system in ameliorating myocardial injury, scar formation and calcification in animal in vivo models of myocarditis. The project was prospectively registered with the PROSPERO database of systematic reviews (CRD42018089336). Primary outcomes (necrosis, fibrosis and calcification) were meta-analyzed with random-effects modeling. 52 Studies were systematically reviewed. Meta-anal. was performed compared with untreated controls. In each study, we identified all independent comparisons of treatment vs. control groups. The pooled weighted mean difference (WMD) indicated treatment reduced necrosis by 16.9% (71 controlled analyses, 95% CI 13.2-20.7%; P < 0.001), however there was less evidence of an effect after accounting for publication bias. Treatment led to a 12.8% reduction in fibrosis (73 controlled analyses, 95% CI 7.6-18.0%; P < 0.001). After accounting for publication bias this was attenuated to 7.8% but remained significant. Treatment reduced calcification by 4.1% (28 controlled analyses, 95% CI 0.2-8.0%; P < 0.0395). We observed significant heterogeneity in effect size in all primary endpoints, which was predominantly driven by differences between drug categories. Beta blockers and angiotensin-converting enzyme (ACE) inhibitors were the only agents that were effective for both necrosis and fibrosis, while only ACE inhibitors had a significant effect on calcification. This study provides evidence for a role for ACE inhibitors and beta blockers to prevent myocardial injury and scar deposition in in vivo models of myocarditis. There is a need for further well-designed studies to assess the translational application of these treatments. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Synthetic Route of 132-20-7

The Article related to meta analysis myocardial injury myocarditis beta calcium channel blocker, calcification, drug treatment, fibrosis, meta-analysis, myocarditis, necrosis, remodelling, systematic review and other aspects.Synthetic Route of 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 31, 2021, Sun, Ji-yun; Kumata, Katsushi; Chen, Zhen; Zhang, Yi-ding; Chen, Jia-hui; Hatori, Akiko; Fu, Hua-long; Rong, Jian; Deng, Xiao-yun; Yamasaki, Tomoteru; Xie, Lin; Hu, Kuan; Fujinaga, Masayuki; Yu, Qing-zhen; Shao, Tuo; Collier, Thomas Lee; Josephson, Lee; Shao, Yi-han; Du, Yun-fei; Wang, Lu; Xu, Hao; Zhang, Ming-rong; Liang, Steven H. published an article.Electric Literature of 1820711-82-7 The title of the article was Synthesis and preliminary evaluation of novel 11C-labeled GluN2B-selective NMDA receptor negative allosteric modulators. And the article contained the following:

Abstract: N-methyl-D-aspartate receptors (NMDARs) play critical roles in the physiol. function of the mammalian central nervous system (CNS), including learning, memory, and synaptic plasticity, through modulating excitatory neurotransmission. Attributed to etiopathol. of various CNS disorders and neurodegenerative diseases, GluN2B is one of the most well-studied subtypes in preclin. and clin. studies on NMDARs. Herein, we report the synthesis and preclin. evaluation of two 11C-labeled GluN2B-selective neg. allosteric modulators (NAMs) containing N,N-dimethyl-2-(1H-pyrrolo[3,2-b]pyridin-1-yl)acetamides for positron emission tomog. (PET) imaging. Two PET ligands, namely [11C]31 and [11C]37 (also called N2B-1810 and N2B-1903, resp.) were labeled with [11C]CH3I in good radiochem. yields (decay-corrected 28% and 32% relative to starting [11C]CO2, resp.), high radiochem. purity (>99%) and high molar activity (>74 GBq/μmol). In particular, PET ligand [11C]31 demonstrated moderate specific binding to GluN2B subtype by in vitro autoradiog. studies. However, because in vivo PET imaging studies showed limited brain uptake of [11C]31 (up to 0.5 SUV), further medicinal chem. and ADME optimization are necessary for this chemotype attributed to low binding specificity and rapid metabolism in vivo. The experimental process involved the reaction of tert-Butyl 6-bromo-1H-pyrrolo[3,2-b]pyridine-1-carboxylate(cas: 1820711-82-7).Electric Literature of 1820711-82-7

The Article related to glun2b receptor neg allosteric modulator pet imaging radiotracer brain, glun2b subunit, nmdars, carbon-11, ionotropic glutamate receptors (iglurs), positron emission tomography (pet) and other aspects.Electric Literature of 1820711-82-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 27, 2003, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradel, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine The title of the patent was Preparation of triazinyl and other carboxamides as inhibitors of histone deacetylase. And the patent contained the following:

The invention relates to triazines (shown as I; variables defined below; e.g. 4-[[4-amino-6-(2-indanylamino)-[1,3,5]triazin-2-ylamino]methyl]-N-(2-aminophenyl)benzamide) and Cy3-X1-Ar2-(C(R5):C(R6))qC(O)NH-Ay2 (II; variables defined below; e.g. ), many of which are N-(o-aminophenyl)carboxamides, as inhibitors of histone deacetylase (data included for many I and II). The invention provides compounds and methods for inhibiting histone deacetylase enzymic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I and II are illustrated for colorectal, pulmonary and pancreatic neoplasms; also the combined antineoplastic effect of histone deacetylase inhibitors and histone deacetylase antisense oligonucleotides on tumor cells in vivo was demonstrated. For I: R3 and R4 = H, L1, Cy1 and -L1-Cy1 (L1 = C1-C6 alkyl, C2-C6 heteroalkyl, or C3-C6 alkenyl; Cy1 = cycloalkyl, aryl, heteroaryl, or heterocyclyl) or R3 and R4 are taken together with the adjacent N atom to form a 5-, 6-, or 7-membered ring, wherein the ring atoms = C, O, S, and N, and wherein the ring is optionally substituted, and optionally forms part of a bicyclic ring system, or is optionally fused to one or two aryl or heteroaryl rings, or to one or two saturated or partially unsaturated cycloalkyl or heterocyclic rings, each of which rings and ring systems is optionally substituted. Y1 = -N(R1)(R2), -CH2-C(O)-N(R1)(R2), halogen, and H (R1 and R2 = H, L1, Cy1, and -L1-Cy1). Y2 = chem. bond or N(R0) (R0 = H, alkyl, aryl, aralkyl, and acyl); Ak1 = C1-C6 alkylene, C1-C6-heteroalkylene (preferably, in which one -CH2- is replaced with -NH-, and more preferably -NH-CH2), C2-C6 alkenylene or C2-C6 alkynylene; Ar1 = arylene or heteroarylene, either of which is optionally substituted; and Z1 = C(O)NH-Ay1 and CH:CHC(O)NH-Ay1 (Ay1 = aryl or heteroaryl, each of which is optionally substituted). For II: Cy2 = cycloalkyl, aryl, heteroaryl, or heterocyclyl; X1 = covalent bond, M1-L2-M1, and L2-M2-L2 (L2 = chem. bond, C1-C4 alkylene, C2-C4 alkenylene, and C2-C4 alkynylene, provided that L2 is not a chem. bond when X1 is M1-L2-M1; M1 = -O-, -N(R7)-, -S-, -S(O)-, S(O)2-, -S(O)2N(R7)-, -N(R7)S(O)2-, -C(O)-, -C(O)NH-, -NHC(O)-, -NHC(O)-O- and -OC(O)NH- (R7 = H, alkyl, aryl, aralkyl, acyl, heterocyclyl, and heteroaryl); and M2 = M1, heteroarylene, and heterocyclylene, either of which rings is optionally substituted). Ar2 = arylene or heteroarylene, each of which is optionally substituted; R5 and R6 = H, alkyl, aryl, and aralkyl; q is 0 or 1; and Ay2 is a 5-6 membered cycloalkyl, heterocyclyl, or heteroaryl substituted with an amino or hydroxy moiety (preferably these groups are ortho to the amide N to which Ay2 is attached) and further optionally substituted; provided that when Cy2 is naphthyl, X1 is -CH2-, Ar2 is Ph, R5 and R6 are H, and q is 0 or 1, Ay2 is not Ph or o-hydroxyphenyl. Although the methods of preparation are not claimed, hundreds of example preparations are included. The experimental process involved the reaction of N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine(cas: 199522-66-2).Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

The Article related to carboxamide preparation inhibitor histone deacetylase proliferative disease treatment, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease treatment and other aspects.Name: N1-(5-Bromopyrid-2-yl)ethane-1,2-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gumbau-Brisa, R.; Hayward, J. J.; Wallis, J. D.; Rawson, J. M.; Pilkington, M. published an article in 2016, the title of the article was Structural insights into the coordination chemistry and reactivity of a 3,3′-bis-imine-2,2′-bipyridine ligand.Recommanded Product: [2,2′-Bipyridine]-3,3′-diamine And the article contains the following content:

The coordination chem. of ligand L8 Schiff-base derived from 6,6′-diamine-2,2′-bipyridine and salicylaldehyde, with Lewis acidic metal ions affords mononuclear [Sn(L9)Cl4] (1) and two paramagnetic dimers [Cu(L9)(sal)]2(ClO4)2, (2) and [Mn(L9)Cl2(EtOH)]2 (3). The x-ray crystal structures of 1-3 reveal a propensity for L8 to undergo metal catalyzed hydrolysis and cyclization to the diazepine ligand L9. Theor. calculations on L8 and a model Sn(IV) complex reveal that coordination to a metal ion weakens the imine bonds, rendering them more susceptible to hydrolysis reactions and/or attack by nucleophiles. In contrast, reaction of L8 with FeCl3 in the presence of base affords the partial hydrolysis product [Fe(L10)2]Cl·CH3CN (4). Tuning the reaction conditions via the addition of a 2nd base slows down the hydrolysis of the ligand sufficiently to afford a few crystals of the μ2-oxo diferric complex (μ-O)[Fe(L8)]2·2CH3CN (5) in which intact L8 coordinates to the Fe(III) in a bis-bidentate manner through a deprotonated salicyl oxygen and a bis-imine nitrogen lone pair, with the nitrogen atoms of its 2,2′-bipyridine remaining uncoordinated. 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 tin transition metal schiff diaminebipyridine salicylaldehyde diazepine complex preparation, crystal structure tin transition metal schiff diaminebipyridine salicylaldehyde diazepine and other aspects.Recommanded Product: [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On September 30, 2009, Li, Hong Liang published an article.Computed Properties of 75449-26-2 The title of the article was 2,2′-[(2,2′-Bipyridine-3,3′-diyl)bis(nitrilomethylidyne)]diphenol. And the article contained the following:

The title mol., C24H18N4O2, lies on a 2-fold rotation axis with a dihedral angle of 73.7(1)° between the mean planes of the symmetry-related pyridine rings. The dihedral angle between unique benzene and pyridine rings is 8.0(1)°. An intramol. O-H…N H bond may influence the mol. conformation. In the crystal structure, there are weak π-π stacking interactions with a centroid-centroid distance of 3.7838(15) Å. Crystallog. data and at. coordinates are given. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Computed Properties of 75449-26-2

The Article related to mol structure bipyridinediyl nitrilomethylidyne phenol, crystal structure bipyridinediyl nitrilomethylidyne phenol, hydrogen bond bipyridinediylnitrilomethylidynediphenol, pi stacking interaction bipyridinediylnitrilomethylidynediphenol and other aspects.Computed Properties of 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 27, 2005, Toele, P.; Glasbeek, M. published an article.Electric Literature of 75449-26-2 The title of the article was Ultrafast excited-state intramolecular double proton transfer dynamics of [2,2′-bipyridyl]-3,3′-diamine. And the article contained the following:

A femtosecond fluorescence upconversion study of [2,2′-bipyridyl]-3,3′-diamine (BP(NH2)2), in liquid solution, is reported. It is concluded that photoexcited BP(NH2)2 undergoes a branched intramol. double proton transfer reaction comprising two trajectories: (a) ultrafast double proton transfer (<100 fs) followed by twisting (∼250 fs); (b) a combined process of double proton transfer and twisting, with an overall reaction time of ∼250 fs. Picosecond transient fluorescence is attributed to vibrational cooling in the excited product state. The lifetime of ∼10 ps of the tautomer product state is indicative of conical intersection of the product- and ground-state potential energy surfaces. The experimental process involved the reaction of [2,2'-Bipyridine]-3,3'-diamine(cas: 75449-26-2).Electric Literature of 75449-26-2

The Article related to fluorescence upconversion study bipyridyldiamine photoinduced intramol double proton transfer, excited state intramol double proton transfer dynamics bipyridyldiamine, photoinduced tautomerization photophys photochem bipyridyldiamine and other aspects.Electric Literature of 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 14, 2005, Munoz, M. Paz; Adrio, Javier; Carretero, Juan Carlos; Echavarren, Antonio M. published an article.Recommanded Product: 109660-12-0 The title of the article was Ligand Effects in Gold- and Platinum-Catalyzed Cyclization of Enynes: Chiral Gold Complexes for Enantioselective Alkoxycyclization. And the article contained the following:

Phosphine and bidentate N-N ligands inhibit the Alder-ene-type cycloisomerization of enynes catalyzed by Pt(II) and favor the alkoxycyclization process. The enantioselective Pt(II)-catalyzed alkoxycyclization has been studied in the presence of chiral mono- and bidentate phosphines, as well as chiral bidentate N-N ligands. Modest levels of enantioselection (up to 50% ee) have been obtained with Tol-BINAP as ligand. The alkoxycyclizations with a catalyst formed from [Au(L)Cl]/AgX proceed more readily, and up to 94% ee’s have been obtained using [(AuCl)2(Tol-BINAP)] (1) as the precatalyst. X-ray crystal structures of Au(I) complexes 1 and chloro-(R)-2-(tert-butylsulfenyl)-1-(diphenylphosphino)ferrocene gold(I) show the AuCl fragments monocoordinated with the P centers of the chiral phosphine ligands. The experimental process involved the reaction of 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine(cas: 109660-12-0).Recommanded Product: 109660-12-0

The Article related to enyne phosphine platinum gold complex catalyzed stereoselective alkoxycyclization alc, platinum chiral phosphine complex preparation methoxycyclization catalyst, gold chiral phosphine complex preparation alkoxycyclization catalyst and other aspects.Recommanded Product: 109660-12-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem