Month: November 2022

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

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

Tan, Qing-Hua; Wang, Yan-Qin; Guo, Xiao-Yu; Liu, Hou-Ting; Liu, Zhi-Liang published an article in 2016, the title of the article was A gadolinium MOF acting as a multi-responsive and highly selective luminescent sensor for detecting o-, m-, and p-nitrophenol and Fe3+ ions in the aqueous phase.Application In Synthesis of 5,5′-(Pyridine-2,5-diyl)diisophthalic acid And the article contains the following content:

A microporous Gd-MOF, [Gd6(L)3(HL)2(H2O)10]·18H2O·x(solvent) (1), was successfully synthesized by a solvothermal reaction between Gd(NO3)3·6H2O and the multidentate π-conjugated ligand, H4L, which has a Lewis basic pyridyl site (H4L = 5,5′-(pyridine-2,5-diyl)isophthalic acid). The crystal structure shows that compound 1 consists of Gd3 units, which are further interlinked by multicarboxylate ligands to form a 2-dimensional network. A solid sample of 1 emits bright blue light, which can be assigned to H4L ligand-centered emission. The luminescence of finely ground particles of 1 dispersed in H2O shows high sensitivity and selectivity towards trace amounts of o-, m-, and p-nitrophenol (NP) and Fe3+ ions with good linearity, which indicates that 1 can be used as a multi-responsive luminescence sensor for the detection of o-, m-, and p-NP and Fe3+ ions in an aqueous system. The experimental process involved the reaction of 5,5′-(Pyridine-2,5-diyl)diisophthalic acid(cas: 1431292-15-7).Application In Synthesis of 5,5′-(Pyridine-2,5-diyl)diisophthalic acid

The Article related to gadolinium mof preparation structure luminescence indicator nitrophenol iron ion, crystal structure gadolinium pyridinediylisophthalate mof preparation luminescent indicator nitrophenol and other aspects.Application In Synthesis of 5,5′-(Pyridine-2,5-diyl)diisophthalic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 30, 2015, Le Tiran, Arnaud; Le Diguarher, Thierry; Starck, Jerome-Benoit; Henlin, Jean-Michel; De Nanteuil, Guillaume; Geneste, Olivier; Davidson, James Edward Paul; Murray, James Brooke; Chen, I-Jen published a patent.HPLC of Formula: 908267-63-0 The title of the patent was New indolizine carboxamide derivatives, their preparation as pro-apoptotic and antitumor agents and their pharmaceutical compositions containing them. And the patent contained the following:

Indolizine and indolizine derivatives, especially 5,6,7,8-tetrahydroindolizine optionally substituted with an NH2 group, 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine optionally substituted with a Me group and pyrrolo[1,2-a]pyrimidine derivatives, e.g., I•HCl, were prepared as inducers of caspase activity and apoptosis for treating neoplasm. Thus, I•HCl was prepared by a multi-step procedure starting from II (preparation given) and (3R)-3-methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride (preparation given). I•HCl was evaluated for its ability to induce caspase activity and therefore apoptosis in vitro and in vivo and for its ability to inhibit the Bcl-2 protein. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).HPLC of Formula: 908267-63-0

The Article related to indolizine preparation antitumor proapoptotic agent inducer caspase activity apoptosis, pyrrolopyrazine pyrrolopyrimidine indolizine carboxamide preparation antitumor proapoptotic agent and other aspects.HPLC of Formula: 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On January 29, 2015, Le Tiran, Arnaud; Le Diguarher, Thierry; Starck, Jerome-Benoit; Henlin, Jean-Michel; De Nanteuil, Guillaume; Geneste, Olivier; Davidson, James Edward Paul; Murray, James Brooke; Chen, I-Jen published a patent.Synthetic Route of 908267-63-0 The title of the patent was New indolizine carboxamide derivatives, their preparation as pro-apoptotic and antitumor agents and their pharmaceutical compositions containing them. And the patent contained the following:

Indolizine and indolizine derivatives, especially 5,6,7,8-tetrahydroindolizine optionally substituted with an NH2 group, 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine optionally substituted with a Me group and pyrrolo[1,2-a]pyrimidine derivatives, e.g., I•HCl, were prepared as inducers of caspase activity and apoptosis for treating neoplasm. Thus, I•HCl was prepared by a multi-step procedure starting from II (preparation given) and (3R)-3-methyl-1,2,3,4-tetrahydroisoquinoline hydrochloride (preparation given). I•HCl was evaluated for its ability to induce caspase activity and therefore apoptosis in vitro and in vivo and for its ability to inhibit the Bcl-2 protein. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Synthetic Route of 908267-63-0

The Article related to indolizine preparation antitumor proapoptotic agent inducer caspase activity apoptosis, pyrrolopyrazine pyrrolopyrimidine indolizine carboxamide preparation antitumor proapoptotic agent and other aspects.Synthetic Route of 908267-63-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 31, 2010, Nirmalram, Jeyaraman Selvaraj; Muthiah, Packianathan Thomas published an article.Formula: C5H5NO3S The title of the article was Hydrogen-bonding patterns in pyrimethaminium pyridine-3-sulfonate. And the article contained the following:

In the asym. unit of the title salt [systematic name: 2,4-diamino-5-(4-chlorophenyl)-6-ethylpyrimidin-1-ium pyridine-3-sulfonate], C12H14N4Cl+·C5H4NSO3-, there are two independent pyrimethaminium cations and two 3-pyridine sulfonate anions. Each sulfonate group interacts with the corresponding protonated pyrimidine ring through two N-H…O hydrogen bonds, forming a cyclic hydrogen-bonded bimol. R22(8) motif. Even though the primary mode of association is the same, the next higher level of supramol. architectures are different due to different hydrogen-bonded networks. In one of the independent mols. in the asym. unit, the pyrimethamine cation is paired centrosym. through N-H…N hydrogen bonds, generating an R22(8) ring motif. In the other mol., the pyrimethamine cation does not form any base pairs; instead it forms hydrogen bonds with the 3-pyridine sulfonate anion. The structure is further stabilized by C-H…O, C-H…N and π-π stacking [centroid-centroid distance = 3.9465 (13) Å] interactions. Crystallog. data are given. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Formula: C5H5NO3S

The Article related to pyrimethaminium pyridine sulfonate salt crystal structure, supramol mol structure pyrimethaminium pyridinesulfonate salt, hydrogen bond pi stacking pyrimethaminium pyridinesulfonate salt and other aspects.Formula: C5H5NO3S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 29, 2005, Delorme, Daniel; Woo, Soon Hyung; Vaisburg, Arkadii; Moradei, Oscar; Leit, Silvana; Raeppel, Stephane; Frechette, Sylvie; Bouchain, Giliane published a patent.Category: pyridine-derivatives 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 provides compounds and methods for inhibiting histone deacetylase enzymic activity. Such compounds include carboxamides I [Cy2 = (un)substituted cycloalkyl, aryl, heteroaryl, heterocyclyl (each of which is optionally fused to one or two aryl or heteroaryl rings, or to one or two (un)saturated cycloalkyl or heterocyclic rings); X1 = a bond, M1L2M1, L2M2L2 (wherein L2 = a bond, alkylene, alkenylene, alkynylene; M1 = O, S, SO, NHCO, etc.; M2 = M1, heteroarylene, heterocyclylene); Ar2 = (un)substituted (hetero)arylene; R5, R6 = H, alkyl, aryl, aralkyl; q = 0-1; Ay2 = (un)substituted 5-6 membered cycloalkkyl, heterocyclyl or heteroaryl substituted with an amino or hydroxy moiety; with provisos] which were prepared and claimed. E.g., a multi-step synthesis of II, starting from Me 4-(aminomethyl)benzoate.HCl, was given. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Antineoplastic effects of some I 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. 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).Category: pyridine-derivatives

The Article related to carboxamide preparation inhibitor histone deacetylase hdac proliferative disease antitumor, triazinyl carboxamide preparation inhibitor histone deacetylase proliferative disease antitumor and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 1, 1987, Heinisch, Gottfried; Loetsch, Gerhard published an article.Synthetic Route of 97483-79-9 The title of the article was Homolytic alkoxycarbonylation reactions in two-phase systems. 3. Introduction of a single carboxylic acid ester function into cyano- or (alkoxycarbonyl)-substituted N-heteroaromatics. And the article contained the following:

Radical alkoxycarbonylation of pyridines I (R = cyano, CO2Et, R1-R3 = H; R = R2 = R3 = H, R1 = cyano, CO2Et; R = R1 = R3 = H, R2 = cyano, CO2Et) with MeCOCO2Me or MeCOCO2Et in H2O-CH2Cl2 containing H2O2-FeSO4 gave mainly monosubstitution products. Thus, I (R = cyano, R1-R3 = H) was treated with MeCOCO2Et to give 34% I (R = cyano, R1 = R3 = H, R2 = CO2Et) and 13% I (R = cyano, R1 = R2 = H, R3 = CO2Et). Similarly, I (R = R2 = R3 = H, R1 = CO2Et) reacted with MeCOCO2Me to give 29% I (R = CO2Me, R1 = CO2Et, R2 = R3 = H), 36% I (R = R3 = H, R1 = CO2Et, R2 = CO2Me), and 20% I (R = R2 = H, R1 = CO2Et, R3 = CO2Me). Only the mixed ester I (R = CO2Me, R1 = R3 = H, R2 = CO2Et) was obtained (in 81% yield) by treating I (R = R1 = R3 = H, R2 = CO2Et) with MeCOCO2Me. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Synthetic Route of 97483-79-9

The Article related to pyridine alkoxycarbonyl cyano, cyanopyridinecarboxylate, pyridazinedicarboxylate, homolytic alkoxycarbonylation cyanopyridine pyruvate, radical alkoxycarbonylation pyridinecarboxylate pyruvate and other aspects.Synthetic Route of 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 30, 2013, Zhao, Hongwu; Yue, Yuanyuan; Li, Hailong; Sheng, Zhihui; Yang, Zhao; Meng, Wei published an article.Name: [2,2′-Bipyridine]-3,3′-diamine The title of the article was Asymmetric synthesis of novel axially chiral 2,2′-bipyridine N,N’-dioxides bearing α-amino acid residues and their applications in enantioselective allylation of aromatic aldehydes with allyltrichlorosilane. And the article contained the following:

A series of novel axially chiral 2,2′-bipyridine N,N’-dioxides bearing C1 or C2-symmetry were synthesized by the use of enantiopure α-amino acids as chiral sources. The absolute stereochem. of the axial chirality of these organocatalysts was clearly assigned by CD measurements together with literature protocols. The reactivities and enantioselectivities of these organocatalysts were examined in the reactions of aromatic aldehydes with allyltrichlorosilane, thus providing the desired products with moderate yields and enantioselectivies. 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 amino acid bipyridine oxide asym synthesis allylation catalyst, aromatic aldehyde allylchlorosilane enantioselective allylation bipyridine oxide catalyst, benzylic homoallyl alc asym synthesis and other aspects.Name: [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 30, 1979, Brown, Norman M. D.; Cowley, David J.; Hashmi, Mahoud published an article.Synthetic Route of 52243-87-5 The title of the article was Kinetic studies of the photoreduction of 4,4′-di-n-alkylbipyridylium salts by alkanols in aqueous solution. And the article contained the following:

The photoreduction of ≤10-3 M solutions of I (R = Me, Et, Pr, Bu, pentyl, hexyl, heptyl; X = halide) by RCH(OH)R1 (II; R = H, R1 = Me, Et, Pr, Bu; R = R1 = Me) on irradiation at 254 nm was studied. Triplet excited I react initially with the alc. to give an exciplex which by H atom transfer gives a cation radical. Halide ions exerted a strong quenching effect, and the quantum yield of photoreduction was greatly influenced by the R groups in I and the R and R1 groups in II. The experimental process involved the reaction of 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide(cas: 52243-87-5).Synthetic Route of 52243-87-5

The Article related to alkylbipyridylium photoreduction alc kinetics, bipyridylium alkyl photoreduction alc kinetics, reduction photochem alkylbipyridylium kinetics, substituent effect alkylbipyridylium photoreduction and other aspects.Synthetic Route of 52243-87-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem