Category: 1008506-24-8

Montgomery, Justin I. published the artcileDiscovery and characterization of a novel class of pyrazolopyrimidinedione tRNA synthesis inhibitors, Name: 3-Methoxypyridine-4-boronic acid, the publication is Journal of Antibiotics (2015), 68(6), 361-367, database is CAplus and MEDLINE.

A high-throughput phenotypic screen for novel antibacterial agents led to the discovery of a novel pyrazolopyrimidinedione, PPD-1, with preferential activity against methicillin-resistant Staphylococcus aureus (MRSA). Resistance mapping revealed the likely target of inhibition to be lysyl tRNA synthetase (LysRS). Preliminary structure-activity relationship (SAR) studies led to an analog, PPD-2, which gained Gram-neg. antibacterial activity at the expense of MRSA activity and resistance to this compound mapped to prolyl tRNA synthetase (ProRS). These targets of inhibition were confirmed in vitro, with PPD-1 showing IC₅₀s of 21.7 and 35 μM in purified LysRS and ProRS enzyme assays, and PPD-2, 151 and 0.04 μM, resp. The highly attractive chem. properties of these compounds combined with intriguing preliminary SAR suggest that further exploration of this compelling novel series is warranted.

Journal of Antibiotics published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Name: 3-Methoxypyridine-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Luecking, Ulrich published the artcileIdentification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer, Formula: C6H8BNO3, the publication is ChemMedChem (2017), 12(21), 1776-1793, database is CAplus and MEDLINE.

Selective inhibition of exclusively transcription-regulating PTEFb/CDK9 is a promising new approach in cancer therapy. Starting from lead compound BAY-958, lead optimization efforts strictly focusing on kinase selectivity, physicochem. and DMPK properties finally led to the identification of the orally available clin. candidate atuveciclib (BAY 1143572). Structurally characterized by an unusual benzyl sulfoximine group, BAY 1143572 exhibited the best overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats. BAY 1143572 is the first potent and highly selective PTEFb/CDK9 inhibitor to enter clin. trials for the treatment of cancer.

ChemMedChem published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Formula: C6H8BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Joseph, Jayan T. published the artcileAryl/heteroaryl pentafluorobenzenesulfonates (ArOPFBs): new electrophilic coupling partners for room temperature Suzuki-Miyaura cross-coupling reactions, HPLC of Formula: 1008506-24-8, the publication is Tetrahedron Letters (2015), 56(36), 5106-5111, database is CAplus.

The first Suzuki-Miyaura cross-coupling reaction between aryl pentafluorobenzenesulfonates e.g., I, and aryl boronic acids under mild conditions was described. High chemoselectivity of these bench stable aryl pentafluorobenzenesulfonates over tosylates, triflates, mesylates, and chlorides for the successful synthesis of highly ortho substituted biaryls was also discussed. Addnl., the generality of this protocol was further extended to other boron containing nucleophiles (boronates, trifluoroborates) and alkyl boronic acids. This process had several advantages which include use of mild catalyst, rapid reaction conditions, wide substrate scope, facile synthesis and high chemoselectivity with good yields.

Tetrahedron Letters published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, HPLC of Formula: 1008506-24-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ohmura, Toshimichi published the artcileOrganocatalytic Diboration Involving “Reductive Addition” of a Boron-Boron σ-Bond to 4,4′-Bipyridine, Related Products of pyridine-derivatives, the publication is Journal of the American Chemical Society (2015), 137(8), 2852-2855, database is CAplus and MEDLINE.

A 4,4′-bipyridine-based catalyst system for diboration of pyrazine derivatives was established. The catalyst cycle consists of the following two steps: (1) reductive addition of the boron-boron bond of bis(pinacolato)diboron to 4,4′-bipyridine to form N,N’-diboryl-4,4′-bipyridinylidene and (2) oxidative boryl transfer from the intermediate to pyrazine to give N,N’-diboryl-1,4-dihydropyrazine with regeneration of 4,4′-bipyridine.

Journal of the American Chemical Society published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Culp, Jeffrey T. published the artcileScreening Hofmann Compounds as CO₂ Sorbents: Nontraditional Synthetic Route to Over 40 Different Pore-Functionalized and Flexible Pillared Cyanonickelates, SDS of cas: 1008506-24-8, the publication is Inorganic Chemistry (2013), 52(8), 4205-4216, database is CAplus and MEDLINE.

A simple reaction scheme based on the heterogeneous intercalation of pillaring ligands (HIPLs) provides a convenient method for systematically tuning pore size, pore functionality, and network flexibility in an extended series of pillared cyanonickelates (PICNICs), commonly named Hofmann compounds The versatility of the approach is demonstrated through the preparation of over 40 different PICNICs containing pillar ligands ranging from âˆ? to âˆ?5 Å in length and modified with a wide range of functional groups, including fluoro, aldehyde, alkylamine, alkyl, aryl, trifluoromethyl, ester, nitro, ether, and non-metalated 4,4′-bipyrimidine. The HIPL method involves reaction of a suspension of preformed polymeric sheets of powd. anhydrous Ni cyanide with an appropriate pillar ligand in refluxing organic solvent, converting the planar [Ni₂(CN)₄]_n networks into polycrystalline three-dimensional porous frameworks containing the organic pillar ligand. Preliminary studies indicate that the HIPL reaction is also amenable to forming Co(L)Ni(CN)₄, Fe(L)Ni(CN)₄, and Fe(L)Pd(CN)₄ networks. The materials show variable adsorption behavior for CO₂ depending on the pillar length and pillar functionalization. Several compounds show structurally flexible behavior during the adsorption and desorption of CO₂. The newly discovered flexible compounds include two flexible Fe(L)Ni(CN)₄ derivatives that are structurally related to previously reported porous spin-crossover compounds The preparations of 20 pillar ligands based on ring-functionalized 4,4′-dipyridyls, 1,4-bis(4-pyridyl)benzenes, and N-(4-pyridyl)isonicotinamides are also described.

Inorganic Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, SDS of cas: 1008506-24-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wilson, Jonathan E. published the artcileDiscovery and development of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists for the treatment of diabetes, SDS of cas: 1008506-24-8, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(12), 2947-2951, database is CAplus and MEDLINE.

A novel series of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists are described. The series was designed to address the suboptimal PK (pharmacokinetic) and off-target profile of a class of N-aryl-benzo-[1,4]-oxazepine-4-carboxamides that were identified from a high-throughput screen of the Merck compound collection for GPR142 agonists. This work led to the discovery of 3-phenoxy-benzo-[1,2,4]-triazolo-[1,4]-oxazepine I, a potent GPR142 agonist with an off-target and PK profile suitable for in vivo studies. This compound and a related analog II were shown to be active in mouse oral glucose tolerance tests (OGTTs). Furthermore, a GPR142 knock-out mouse OGTT study with compound II provides evidence that its glucose-lowering effect is mediated by GPR142.

Bioorganic & Medicinal Chemistry Letters published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C9H13NO2, SDS of cas: 1008506-24-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Hong, Seunghee published the artcileDiscovery of New Benzothiazole-Based Inhibitors of Breakpoint Cluster Region-Abelson Kinase Including the T315I Mutant, COA of Formula: C6H8BNO3, the publication is Journal of Medicinal Chemistry (2013), 56(9), 3531-3545, database is CAplus and MEDLINE.

The existence of drug resistance caused by mutations in the break-point cluster region-Abelson tyrosine kinase (Bcr-Abl) kinase domain remains a clin. challenge due to limited effective treatment options for chronic myeloid leukemia. Herein the authors report a novel series of benzothiazole-based inhibitors that are effective against wild-type and T315I mutant Bcr-Abl kinases. The original hit compound, nocodazole, was extensively modified through a structure-based drug design strategy, especially by varying the groups at the C2 and C6 positions of the scaffold. In addition, the introduction of water-solubilizing groups at the terminal Et group resulted in enhanced physicochem. properties and potency in cellular inhibition. Several compounds inhibited the kinase activity of both wild-type Bcr-Abl and the T315I mutant with IC₅₀ values in the picomolar range and exhibited good antiproliferative effects on Ba/F3 cell lines transformed with either wild-type or T315I mutant Bcr-Abl.

Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, COA of Formula: C6H8BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Niu, Nana published the artcileDesign and Synthesis of Tetrandrine Derivatives as Potential Anti-tumor Agents Against A549 Cell Lines, Category: pyridine-derivatives, the publication is ChemistrySelect (2019), 4(1), 196-201, database is CAplus.

Tetrandrine was converted to 5-bromotetrandrine using a mild oxidative system (DMSO/HBr). Suzuki-Miyaura and Sonogashira cross-coupling reactions were then employed to yield a set of 5-substituted tetrandrine derivatives I (R = 5-formylfuran-2-yl, pyrimidin-5-yl, 2-cyclopropylethynyl, etc.). Their antiproliferative activities against A549 cell lines in vitro were evaluated using the MTT assay. Most of the compounds were found to possess significant inhibitory activities and compound I (R = 2-methoxypyrimidin-5-yl) (A) had the highest (IC₅₀ = 3.04 μM). Further studies on the mechanism demonstrated by (A) showed that it promotes apoptosis of A549 cells in a dose-dependent manner and reduces the mitochondrial membrane potential. Western blot results showed that the compound up-regulated the levels of Bax protein and down-regulated the level of Bcl-2 protein. Compared to the control group, the expression of cleaved-caspase 3 and cleaved-PARP in cells was significantly increased.

ChemistrySelect published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Li, Jian-Yuan published the artcileDevelopment of DNA-Compatible Suzuki-Miyaura Reaction in Aqueous Media, Computed Properties of 1008506-24-8, the publication is Bioconjugate Chemistry (2018), 29(11), 3841-3846, database is CAplus and MEDLINE.

DNA-encoded chem. libraries (DELs) are a cost-effective technol. for the discovery of novel chem. probes and drug candidates. A major limiting factor in assembling productive DELs is the availability of DNA-compatible chem. reactions in aqueous media. In an effort to increase the chem. accessibility and structural diversity of small mols. displayed by DELs, the authors developed a robust Suzuki-Miyaura reaction protocol that is compatible with the DNA structures. By employing a water-soluble Pd-precatalyst, the authors developed conditions that allow efficient coupling of DNA-linked aryl halides with a wide variety of boronic acids/esters including heteroaryl boronates.

Bioconjugate Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, Computed Properties of 1008506-24-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zhang, Han published the artcileDesign, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists, Product Details of C6H8BNO3, the publication is European Journal of Medicinal Chemistry (2020), 112774, database is CAplus and MEDLINE.

7 Nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems was suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761-0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC₅₀ values ranging from 3.3μM to 13.7μM. Compound 3-(4-Bromophenyl)-8-methyl-1-oxa-2,4,8-triazaspiro[4.5]dec-2-ene exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The anal. of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.

European Journal of Medicinal Chemistry published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C13H10F2, Product Details of C6H8BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem