Category: 29682-15-3

Recommanded Product: 29682-15-3In 2016 ,《Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors》 was published in Bioorganic & Medicinal Chemistry. The article was written by Ohno, Hiroaki; Minamiguchi, Daiki; Nakamura, Shinya; Shu, Keito; Okazaki, Shiho; Honda, Maho; Misu, Ryosuke; Moriwaki, Hirotomo; Nakanishi, Shinsuke; Oishi, Shinya; Kinoshita, Takayoshi; Nakanishi, Isao; Fujii, Nobutaka. The article contains the following contents:

Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α) = 0.014-0.017 μM; IC50 (CK2α’) = 0.0046-0.010 μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintained the potent CK2 inhibitory activities [IC50 (CK2α) = 0.014-0.016 μM; IC50 (CK2α’) = 0.0088-0.014 μM] and led to antiproliferative activities [CC50 (A549) = 1.5-3.3 μM] three to six times higher than those of the parent compound In addition to this study using Methyl 5-bromopicolinate, there are many other studies that have used Methyl 5-bromopicolinate(cas: 29682-15-3Recommanded Product: 29682-15-3) was used in this study.

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. Recommanded Product: 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2016,Cross, Jason B.; Zhang, Jing; Yang, Qingyi; Mesleh, Michael F.; Romero, Jan Antoinette C.; Wang, Bin; Bevan, Doug; Poutsiaka, Katherine M.; Epie, Felix; Moy, Terence; Daniel, Anu; Shotwell, Joseph; Chamberlain, Brian; Carter, Nicole; Andersen, Ole; Barker, John; Ryan, M. Dominic; Metcalf, Chester A. III; Silverman, Jared; Nguyen, Kien; Lippa, Blaise; Dolle, Roland E. published 《Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design》.ACS Medicinal Chemistry Letters published the findings.SDS of cas: 29682-15-3 The information in the text is summarized as follows:

The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA replication. A novel class of pyrazolopyridone inhibitors was discovered by optimizing a fragment screening hit scaffold using structure guided design. These inhibitors show potent Gram-pos. antibacterial activity and low resistance incidence against clin. important pathogens. After reading the article, we found that the author used Methyl 5-bromopicolinate(cas: 29682-15-3SDS of cas: 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. SDS of cas: 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

HPLC of Formula: 29682-15-3In 2019 ,《New pyridine based liquid crystalline esters with different terminal chains》 appeared in Journal of Molecular Structure. The author of the article were Karanlik, Gurkan; Ocak, Hale; Bilgin Eran, Belkiz. The article conveys some information:

The synthesis, structural and mesomorphic characterization of new pyridine-based Me esters carrying a n-alkoxy chain or 3,7-dimethyloctyloxy branched group at terminal I [R = C8H17, C10H21, C12H25, (4S)-4,8-dimethylnonyl, 4,8-dimethylnonyl] have been presented. The liquid crystalline properties of the new pyridine-based calamitic mols. have been investigated by polarized optical microscopy and differential scanning calorimetry. New compounds exhibit enantiotropic smectic A mesophase at a variable mesomorphic range depending on alkoxy chain length and branching at terminal. The presence of a branched terminal group in chiral or racemic form gives rise to a sharply increase in mesomorphic range as well as decrease in crystallization points by preserving mesophase type. The experimental process involved the reaction of Methyl 5-bromopicolinate(cas: 29682-15-3HPLC of Formula: 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.HPLC of Formula: 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

SDS of cas: 29682-15-3In 2013 ,《Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 Inhibitor》 was published in Journal of Medicinal Chemistry. The article was written by Voronkov, Andrew; Holsworth, Daniel D.; Waaler, Jo; Wilson, Steven R.; Ekblad, Bie; Perdreau-Dahl, Harmonie; Dinh, Huyen; Drewes, Gerard; Hopf, Carsten; Morth, Jens P.; Krauss, Stefan. The article contains the following contents:

Tankyrases 1 and 2 (TNKS1/2) are promising pharmacol. biotargets with possible applications for the development of novel anticancer therapeutics. A focused structure-activity relationship study was conducted based on the tankyrase inhibitor JW74 (1). Chem. analoging of 1 improved the 1,2,4-triazole based core and led to 4-{5-[(E)-2-{4-(2-chlorophenyl)-5-[5-(methylsulfonyl)pyridin-2-yl]-4H-1,2,4-triazol-3-yl}ethenyl]-1,3,4-oxadiazol-2-yl}benzonitrile (G007-LK), a potent, “”rule of 5″” compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK (66) displayed high selectivity toward tankyrases 1 and 2 with biochem. IC50 values of 46 nM and 25 nM, resp., and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice. The PARP domain of TNKS2 was cocrystd. with 66, and the X-ray structure was determined at 2.8 Å resolution in the space group P3221. The structure revealed that 66 binds to unique structural features in the extended adenosine binding pocket which forms the structural basis for the compound’s high target selectivity and specificity. Our study provides a significantly optimized compound for targeting TNKS1/2 in vitro and in vivo. After reading the article, we found that the author used Methyl 5-bromopicolinate(cas: 29682-15-3SDS of cas: 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. SDS of cas: 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2008,Kimball, F. Scott; Romero, F. Anthony; Ezzili, Cyrine; Garfunkle, Joie; Rayl, Thomas J.; Hochstatter, Dustin G.; Hwang, Inkyu; Boger, Dale L. published 《Optimization of α-Ketooxazole Inhibitors of Fatty Acid Amide Hydrolase》.Journal of Medicinal Chemistry published the findings.Recommanded Product: 29682-15-3 The information in the text is summarized as follows:

A series of α-ketooxazoles, e.g., I, containing conformational constraints in the flexible C2 acyl side chain of II (OL-135) and representative oxazole C5 substituents were prepared and examined as inhibitors of fatty acid amide hydrolase (FAAH). Exceptionally potent and selective FAAH inhibitors emerged from the series (e.g., 6, Ki = 200 and 260 pM for rat and rhFAAH). With simple and small C5 oxazole substituents, each series bearing a biphenylethyl, phenoxyphenethyl, or (phenoxymethyl)phenethyl C2 side chain was found to follow a well-defined linear relationship between -log Ki and Hammett σp of a magnitude (ρ = 2.7-3.0) that indicates that the substituent electronic effect dominates, confirming its fundamental importance to the series and further establishing its predictive value. Just as significantly, the nature of the C5 oxazole substituent substantially impacts the selectivity of the inhibitors whereas the effect of the C2 acyl chain was more subtle but still significant even in the small series examined Combination of these independent features, which display generalized trends across a range of inhibitor series, simultaneously improves FAAH potency and selectivity and can provide exquisitely selective and potent FAAH inhibitors. In the experiment, the researchers used Methyl 5-bromopicolinate(cas: 29682-15-3Recommanded Product: 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is a relatively complex molecule and exhibits a number of different bands in IR spectra. Among others, the bands characterizing the ν8a and ν19b modes have been found to be sensitive to the coordination or protonation of the molecule. Note that the band that is diagnostic for the PyH+ ion at about 1545 cm− 1 (ν19b mode) does not overlap with any of the other bands.Recommanded Product: 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2018,Richardson, Jeffery; Mutton, Simon P. published 《Improved Substrate Scope in the Potassium Hexacyanoferrate(II)-Based Cyanation for the Synthesis of Benzonitriles and Their Heterocyclic Analogues》.Journal of Organic Chemistry published the findings.Category: pyridine-derivatives The information in the text is summarized as follows:

The use of Pd(DPEPhos)Cl2 (P26) as a catalyst for the formation of benzonitriles and their heterocyclic analogs provides excellent complementarity to existing catalysts, allowing highly electron-deficient heterocyclic aryl halides to be efficiently converted to the corresponding nitriles using K4[Fe(CN)6] as cyanide source. This catalyst significantly enhances the scope of this reaction to include a number of substrates that are highly relevant for pharmaceutical and agrochem. applications. Importantly, not only does this cyanation method employ a nontoxic cyanide source, simple semiquant. testing suggests that, unlike many other methods, no free cyanide is present in the reaction mixture or during a variety of potential workups, thus improving the safety aspects of this method from initial setup through to product isolation. Finally, developing and testing a series of convenient cyanation kits has allowed facile application and broader adoption of this method in our laboratories In the part of experimental materials, we found many familiar compounds, such as Methyl 5-bromopicolinate(cas: 29682-15-3Category: pyridine-derivatives)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Electric Literature of C7H6BrNO2In 2015 ,《Dosage delivery of sensitive reagents enables glove-box-free synthesis》 appeared in Nature (London, United Kingdom). The author of the article were Sather, Aaron C.; Lee, Hong Geun; Colombe, James R.; Zhang, Anni; Buchwald, Stephen L.. The article conveys some information:

Contemporary organic chemists employ a broad range of catalytic and stoichiometric methods to construct mols. for applications in the material sciences, and as pharmaceuticals, agrochems., and sensors. The utility of a synthetic method may be greatly reduced if it relies on a glove box to enable the use of air- and moisture-sensitive reagents or catalysts. Furthermore, many synthetic chem. laboratories have numerous containers of partially used reagents that have been spoiled by exposure to the ambient atm. This is exceptionally wasteful from both an environmental and a cost perspective. Here we report an encapsulation method for stabilizing and storing air- and moisture-sensitive compounds We demonstrate this approach in three contexts, by describing single-use capsules that contain all of the reagents (catalysts, ligands, and bases) necessary for the glove-box-free palladium-catalyzed carbon-fluorine, carbon-nitrogen, and carbon-carbon bond-forming reactions. This strategy should reduce the number of error-prone, tedious and time-consuming weighing procedures required for such syntheses and should be applicable to a wide range of reagents, catalysts, and substrate combinations. In the experiment, the researchers used many compounds, for example, Methyl 5-bromopicolinate(cas: 29682-15-3Electric Literature of C7H6BrNO2)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Electric Literature of C7H6BrNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2010,Yu, Ming; Lizarzaburu, Mike; Beckmann, Holger; Connors, Richard; Dai, Kang; Haller, Katrin; Li, Cong; Liang, Lingming; Lindstrom, Michelle; Ma, Ji; Motani, Alykhan; Wanska, Malgorzata; Zhang, Alex; Li, Leping; Medina, Julio C. published 《Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 29682-15-3 The information in the text is summarized as follows:

Piperazine-bisamide analogs I (X = 1,4-phenylene, 2-fluoro-1,4-phenylene, pyridine-2,5-diyl, thiazole-2,4-diyl, etc.; R1 = Ph, 6-indolyl, 8-quinolinyl, etc.; R2, R3 = H, Me; R4 = Ph, 3-MeOC6H4, 2-ClC6H4, 4-pyridyl, etc.) were synthesized and studied for their binding to human growth hormone secretagogue receptor (GHSR). Compounds I [X = 1,4-phenylene; R4 = (un)substituted phenyl] were shown to be partial agonists of GHSR in a high throughput screening. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts led to the identification of potent antagonist I [X = 3-fluoro-1,4-phenylene; R1 = 6-indolyl; R2 = (S)-Me; R3 = H; R4 = 4-pyridyl] with favorable PK profile suitable as a tool compound for in vivo studies.Methyl 5-bromopicolinate(cas: 29682-15-3Application of 29682-15-3) was used in this study.

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. Application of 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The author of 《Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model》 were Heng, Hao; Wang, Zhijie; Li, Hongmei; Huang, Yatian; Lan, Qingyuan; Guo, Xiaoxing; Zhang, Liang; Zhi, Yanle; Cai, Jiongheng; Qin, Tianren; Xiang, Li; Wang, Shuxian; Chen, Yadong; Lu, Tao; Lu, Shuai. And the article was published in European Journal of Medicinal Chemistry in 2019. COA of Formula: C7H6BrNO2 The author mentioned the following in the article:

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD. Compound 46, possessing the most promising cellular activity, blocked the autophosphorylation of FLT3 pathway in MV4-11 cell line. Furthermore, the apoptosis and down regulation of P-STAT5 were also observed in tumor cells extracted from the MV4-11 cell xenografts model upon compound 46 treatment. Compound 46 was also metabolically stable in vitro and suppressed tumor growth significantly in MV4-11 xenografts model in vivo. Compound 46 showed no toxicity to the viscera of mice and caused no decrease in body weight of mice. In conclusion, the results of this study could provide valuable insights into discovery of new FLT3 inhibitors, and compound 46 was worthy of further development as potential drug candidate to treat AML.Methyl 5-bromopicolinate(cas: 29682-15-3COA of Formula: C7H6BrNO2) was used in this study.

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. COA of Formula: C7H6BrNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Discovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active γ-secretase modulators》 was published in Bioorganic & Medicinal Chemistry in 2020. These research results belong to Sekioka, Ryuichi; Honda, Shugo; Honjo, Eriko; Suzuki, Takayuki; Akashiba, Hiroki; Mitani, Yasuyuki; Yamasaki, Shingo. Formula: C7H6BrNO2 The article mentions the following:

Gamma-secretase modulators (GSMs) are promising disease-modifying drugs for Alzheimer’s disease because they can selectively decrease pathogenic amyloid-β42 (Aβ42) levels. Here we report the discovery of orally active N-ethylpyridine-2-carboxamide derivatives as GSMs. The isoindolinone moiety of 5-[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]-2-ethyl-2,3-dihydro-1H-isoindol-1-one hydrogen chloride (1a) was replaced with a picolinamide moiety. Optimization of the benzyl group significantly improved GSM activity and mouse microsomal stability. 5-{8-[([1,1′-Biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-ethylpyridine-2-carboxamide hydrogen chloride (1v) potently reduced Aβ42 levels with an IC50 value of 0.091μM in cultured cells without inhibiting CYP3A4. Moreover, 1v demonstrated a sustained pharmacokinetic profile and significantly reduced brain Aβ42 levels in mice.Methyl 5-bromopicolinate(cas: 29682-15-3Formula: C7H6BrNO2) was used in this study.

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is widely used in the precursor to agrochemicals and pharmaceuticals. Also, it is used as an important reagent and organic solvent.Formula: C7H6BrNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem