Gesmundo, Nathan J.’s team published research in Nature (London, United Kingdom) in 2018-05-31 | CAS: 82090-52-6

Nature (London, United Kingdom) published new progress about Chemical library. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Product Details of C8H8N2O.

Gesmundo, Nathan J. published the artcileNanoscale synthesis and affinity ranking, Product Details of C8H8N2O, the main research area is structure drug discovery.

Most drugs are developed through iterative rounds of chem. synthesis and biochem. testing to optimize the affinity of a particular compound for a protein target of therapeutic interest. This process is challenging because candidate mols. must be selected from a chem. space of more than 1060 drug-like possibilities1, and a single reaction used to synthesize each mol. has more than 107 plausible permutations of catalysts, ligands, additives and other parameters2. The merger of a method for high-throughput chem. synthesis with a biochem. assay would facilitate the exploration of this enormous search space and streamline the hunt for new drugs and chem. probes. Miniaturized high-throughput chem. synthesis3-7 has enabled rapid evaluation of reaction space, but so far the merger of such syntheses with bioassays has been achieved with only low-d. reaction arrays, which analyze only a handful of analogs prepared under a single reaction condition8-13. High-d. chem. synthesis approaches that have been coupled to bioassays, including on-bead14, on-surface15, on-DNA16 and mass-encoding technologies17, greatly reduce material requirements, but they require the covalent linkage of substrates to a potentially reactive support, must be performed under high dilution and must operate in a mixture format. These reaction attributes limit the application of transition-metal catalysts, which are easily poisoned by the many functional groups present in a complex mixture, and of transformations for which the kinetics require a high concentration of reactant. Here the authors couple high-throughput nanomole-scale synthesis with a label-free affinity-selection mass spectrometry bioassay. Each reaction is performed at a 0.1-M concentration in a discrete well to enable transition-metal catalysis while consuming less than 0.05 mg of substrate per reaction. The affinity-selection mass spectrometry bioassay is then used to rank the affinity of the reaction products to target proteins, removing the need for time-intensive reaction purification This method enables the primary synthesis and testing steps that are critical to the invention of protein inhibitors to be performed rapidly and with minimal consumption of starting materials.

Nature (London, United Kingdom) published new progress about Chemical library. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Product Details of C8H8N2O.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Feng, Song’s team published research in ACS Medicinal Chemistry Letters in 2015-03-12 | CAS: 82090-52-6

ACS Medicinal Chemistry Letters published new progress about Antiviral agents. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Quality Control of 82090-52-6.

Feng, Song published the artcileDiscovery of Imidazopyridine Derivatives as Highly Potent Respiratory Syncytial Virus Fusion Inhibitors, Quality Control of 82090-52-6, the main research area is imidazopyridine preparation antiviral respiratory syncytial virus fusion inhibitory activity; Respiratory syncytial virus (RSV); antiviral; fusion inhibitors; heterocycle; imidazopyridine; virus.

A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and phys.-chem. properties. Several highly potent compounds such as I (R = CONH2, SO2Me, SO2Et) were identified with single nanomolar activities. The most potent compound I (R = SO2Et) showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of I (R = SO2Et) appeared to be superior to BMS433771, and supported further optimization.

ACS Medicinal Chemistry Letters published new progress about Antiviral agents. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Quality Control of 82090-52-6.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Verhoest, Patrick R.’s team published research in Journal of Medicinal Chemistry in 2009-08-27 | CAS: 82090-52-6

Journal of Medicinal Chemistry published new progress about Molecular modeling. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Category: imidazoles-derivatives.

Verhoest, Patrick R. published the artcileDiscovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920)(I) for the Treatment of Schizophrenia, Category: imidazoles-derivatives, the main research area is schizophrenia phosphodiesterase 10A inhibitor PDE10A pyrazole derivative.

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique “”selectivity pocket”” for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) (I). This PDE10A inhibitor is the first reported clin. entry for this mechanism in the treatment of schizophrenia.

Journal of Medicinal Chemistry published new progress about Molecular modeling. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Oguchi, Minoru’s team published research in Journal of Medicinal Chemistry in 2000-08-10 | CAS: 82090-52-6

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Recommanded Product: Imidazo[1,2-a]pyridin-2-ylmethanol.

Oguchi, Minoru published the artcileMolecular Design, Synthesis, and Hypoglycemic Activity of a Series of Thiazolidine-2,4-diones, Recommanded Product: Imidazo[1,2-a]pyridin-2-ylmethanol, the main research area is thiazolidinedione preparation hypoglycemic insulin resistance structure.

A series of imidazopyridine thiazolidine-2,4-diones were designed and synthesized from their corresponding pyridines. These compounds represent conformationally restricted analogs of the novel hypoglycemic compound rosiglitazone. The series was evaluated for its effect on insulin-induced 3T3-L1 adipocyte differentiation in vitro and its hypoglycemic activity in the genetically diabetic KK mouse in vivo. The structure-activity relationships are discussed. On the basis of the in vivo potency, 5-[4-(5-methoxy-3-methyl-3H-imidazo[4,5-b]pyridin-2-ylmethoxy)benzyl]thiazolidine-2,4-dione was selected as the candidate for further studies in a clin. setting.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Recommanded Product: Imidazo[1,2-a]pyridin-2-ylmethanol.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Desbois, Nicolas’s team published research in Heterocycles in 2005-05-01 | CAS: 82090-52-6

Heterocycles published new progress about Alkaloids Role: BSU (Biological Study, Unclassified), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses) (pyrido[4,3-b]carbazole). 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Name: Imidazo[1,2-a]pyridin-2-ylmethanol.

Desbois, Nicolas published the artcileSynthesis of polyfused heterocycle derivatives containing the dipyridoimidazole core by Friedlaender’s reaction: Access to analogs of ellipticine, Name: Imidazo[1,2-a]pyridin-2-ylmethanol, the main research area is oligodeoxynucleotide intercalation triazacyclopentafluorene triazabenzofluorene dipyridoimidazole triazaindenophenanthrene; tetraazacyclopentafluorene preparation intercalation oligodeoxynucleotide; tetraazabenzofluorene preparation intercalation oligodeoxynucleotide; aminoformylimidazopyridine Friedlander reaction aldehyde ketone; aminoimidazopyridinecarboxaldehyde Friedlander cyclocondensation aldehyde ketone; ellipticine analog preparation intercalation oligodeoxynucleotide.

Reaction of 3-amino-2-formylimidazo[1,2-a]pyridine (I) with various aldehydes and ketones by Friedlaender’s methodol. afforded an entry to dipyridoimidazoles II (R1 = Me, R2 = H; R1 = H, R2 = Me, Ph; R1 = CO2Et, R2 = Me), tri(tetra)azacyclopenta[b]fluorenes III (X3 = Y3 = CH2; X3 = CH2, Y3 = NCO2Et; X3 = NCO2Et, Y3 = CH2), tri(tetra)azabenzo[b]fluorenes IV (X4 = Y4 = CH2; X4 = C:O, Y4 = CH2; X4 = CH2, Y4 = NH·HCl, CHCO2Et) and triazaindeno[2,1-b]phenanthrene V. Intercalation with a synthetic oligodeoxynucleotide, d(CGATCG)2, was examined

Heterocycles published new progress about Alkaloids Role: BSU (Biological Study, Unclassified), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses) (pyrido[4,3-b]carbazole). 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Name: Imidazo[1,2-a]pyridin-2-ylmethanol.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Stock, Nicholas S.’s team published research in Journal of Medicinal Chemistry in 2011-12-08 | CAS: 82090-52-6

Journal of Medicinal Chemistry published new progress about Blood serum albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (human serum albumin – FLAP binding equilibrium). 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Name: Imidazo[1,2-a]pyridin-2-ylmethanol.

Stock, Nicholas S. published the artcile5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor, Name: Imidazo[1,2-a]pyridin-2-ylmethanol, the main research area is lipoxygenase activating protein inhibitor AM803 GSK2190915 antiasthmatic; FLAP inhibitor SAR.

The potent 5-lipoxygenase-activating protein (FLAP) inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid 11cc (I) is described (AM803, now GSK2190915). Building upon AM103, SAR studies centering around the pyridine moiety led to the discovery of compounds that exhibit significantly increased potency in a human whole blood assay measuring LTB4 inhibition with longer drug preincubation times (15 min vs 5 h). Further studies identified 11cc with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood (5 h incubation) and excellent preclin. toxicol. and pharmacokinetics in rat and dog. 11Cc also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. This compound has successfully completed phase 1 clin. studies in healthy volunteers and is currently undergoing phase 2 trials in asthmatic patients.

Journal of Medicinal Chemistry published new progress about Blood serum albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (human serum albumin – FLAP binding equilibrium). 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Name: Imidazo[1,2-a]pyridin-2-ylmethanol.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem