- Novel imidazo[4,5-b]pyridine derived acrylonitriles: A combined experimental and computational study of their antioxidative potential
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We describe the synthesis of novel unsubstituted and N-substituted imidazo[4,5-b]pyridine derived acrylonitriles, which were prepared by classical and microwave assisted organic synthesis. Their antioxidative potential was studied using spectroscopic DPPH
- Bo?ek, Ida,Star?evi?, Kristina,Novak Jovanovi?, Ivana,Vianello, Robert,Hranjec, Marijana
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- Cu-Catalyzed C-H Allylation of Benzimidazoles with Allenes
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CuH-catalyzed intramolecular cyclization and intermolecular allylation of benzimidazoles with allenes have been described. The reaction proceeded smoothly with the catalytic system of Cu(OAc)2/Xantphos and catalytic amount of (MeO)2MeSiH. This protocol features mild reaction conditions and a good tolerance of substrates bearing electron-withdrawing, electron-donating, or electron-neutral groups. A new catalytic mechanism was proposed for this copper hydride catalytic system.
- Dong, Yaxi,Breit, Bernhard
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supporting information
p. 6765 - 6769
(2021/09/11)
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- Discovery of iminobenzimidazole derivatives as novel cytotoxic agents
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In our quest to identify inhibitors of the eukaryotic translation initiation factor 4F (eIF4F), we serendipitously discovered a novel cytotoxic agent. Even though this compound did not inhibit translation, we explored the structural requirements for its cytotoxicity due to its structural originality. A series of 1,3-disubstituted iminobenzimidazoles was synthesized and evaluated for their in vitro cytotoxicity. The structure-activity relationship studies demonstrate that hydrophobic substituent is essential for activity. The most active compounds displayed a cytotoxicity in KB, HL60 and HCT116 human cancer cells with an IC50 of about 1μM. These first-in-class series of low molecular weight synthetic molecules may provide the basis for the development of new anticancer drugs.
- Chouha, Nora,Hammoud, Hassan,Brogi, Simone,Campiani, Giuseppe,Welsch, Caroline,Robert, Caroline,Vagner, Stéphan,Cresteil, Thierry,Bentouhami, Embarek,Désaubry, Laurent
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- 5,10-Dihydropyrido-pyrazolo-triazine compounds and application thereof
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The invention relates to 5,10-dihydropyrido[2',3':5,6]pyrazolo[2,3-e][1,2,4]triazine compounds shown in general formula I, and their optical activators or racemates or their pharmaceutically acceptable salts, hydrates or solvates, wherein substituents R1,
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Paragraph 0097; 0098; 0099
(2017/08/02)
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- The Chameleonic Nature of Platinum(II) Imidazopyridine Complexes
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The synthesis and characterization of cyclometalated C^C* platinum(II) complexes with unique photophysical properties, aggregation induced enhancement of the quantum yields with a simultaneous decrease of phosphorescence lifetimes, is reported. Additional
- Pinter, Piermaria,Pittkowski, Rebecca,Soellner, Johannes,Strassner, Thomas
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supporting information
p. 14173 - 14176
(2017/10/07)
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- Imidoyl dichlorides as new reagents for the rapid formation of 2-aminobenzimidazoles and related azoles
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The development of a reagent for the efficient synthesis of five- and six-membered azoles at room temperature is proposed. A variety of substituted 2-aminobenzimidazoles are synthesized in good to excellent yields. The ability to incorporate various protecting groups makes the imidoyl dichloride reagent amenable to a large number of syntheses. The reagent is applied to the total synthesis of the 2-aminobenzimidazole containing carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), from 2-chloro-3-nitropyridine in >60% yield in 6 steps.
- Pollock, Julie A.,Kim, Sung Hoon,Katzenellenbogen, John A.
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supporting information
p. 6097 - 6099
(2015/10/28)
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- PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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Organometallic compounds comprising an imidazole carbene ligand having a N- containing ring fused to the imidazole ring are provided. In particular, the N-containing ring fused to the imidazole ring may contain one nitrogen atom or more than one nitrogen
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Page/Page column 93
(2012/09/22)
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- PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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Organometallic compounds comprising an imidazole carbene ligand having a N-containing ring fused to the imidazole ring are provided. In particular, the N-containing ring fused to the imidazole ring may contain one nitrogen atom or more than one nitrogen a
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- A simple synthesis of aminopyridines: Use of amides as amine source
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A transition metal/microwave irradiation (or base) free synthesis of aminopyridines has been accomplished via C-N bond forming reaction between chloropyridine and a variety of simple amides under refuxing conditions.
- Kodimuthali, Arumugam,Mungara, Anitha,Prasunamba, Padala Lakshmi,Pal, Manojit
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experimental part
p. 1439 - 1445
(2010/11/04)
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- Efficient and selective method for the synthesis of dihydrodipyridopyrazines based on the pd-catalysed animation of halopyridines
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A novel methodology for the efficient: and selective synthesis of isomers A and B of N-substituted dihydrodipyridopyrazines was developed. The key step is the intermolecular coupling of aminopyridines and halonitropyridines/dihalopyr- idines in the presen
- Patriciu, Oana-Irina,Finaru, Adriana-Luminita,Massip, Stephane,Leger, Jean-Michel,Jarry, Christian,Guillaumet, Gerald
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experimental part
p. 3753 - 3764
(2009/12/05)
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- AZABENZIMIDAZOLYL COMPOUNDS
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Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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Page/Page column 57
(2008/06/13)
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- Imidazopyridines: A novel class of hNav1.7 channel blockers
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A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNav1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4 h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10 mg/kg.
- London, Clare,Hoyt, Scott B.,Parsons, William H.,Williams, Brande S.,Warren, Vivien A.,Tschirret-Guth, Richard,Smith, McHardy M.,Priest, Birgit T.,McGowan, Erin,Martin, William J.,Lyons, Kathryn A.,Li, Xiaohua,Karanam, Bindhu V.,Jochnowitz, Nina,Garcia, Maria L.,Felix, John P.,Dean, Brian,Abbadie, Catherine,Kaczorowski, Gregory J.,Duffy, Joseph L.
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p. 1696 - 1701
(2008/12/23)
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- 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators
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The synthesis and structure-activity relationship (SAR) of a novel series of 3-(imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers, derived from a high throughput screening (HTS), are described. Subsequent optimization led to identification of potent, metabolically stable and orally available mGluR2 positive allosteric modulators (PAMs).
- Zhang, Lei,Rogers, Bruce N.,Duplantier, Allen J.,McHardy, Stanley F.,Efremov, Ivan,Berke, Helen,Qian, Weimin,Zhang, Andy Q.,Maklad, Noha,Candler, John,Doran, Angela C.,Lazzaro Jr., John T.,Ganong, Alan H.
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scheme or table
p. 5493 - 5496
(2009/06/18)
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- Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors
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A series of 3-anilino-quinoxalinones has been identified as a new class of glycogen phosphorylase inhibitors. The lead compound 1 was identified through high throughput screening as well as through pharmacophore-based electronic screening. Modifications were made to the scaffold of 1 to produce novel analogues, some of which are 25 times more potent than the lead compound.
- Dudash Jr., Joseph,Zhang, Yongzheng,Moore, John B.,Look, Richard,Liang, Yin,Beavers, Mary Pat,Conway, Bruce R.,Rybczynski, Philip J.,Demarest, Keith T.
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p. 4790 - 4793
(2007/10/03)
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- Oxidative Methylamination of Some Nitropyridines
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2-, 3-, 4-Nitropyridine (1a, i, j) and some simple derivatives of 3-nitropyridine (1b-h) undergo dehydromethylamination in a solution of potassium permanganate in liquid methylamine. In the case of 2- and 6-chloro and 6-methoxy derivatives of 3-nitropyridine (1b-d) dechloro- or demethoxy-methylamination occurs as well.
- Szpakiewicz, Barbara,Wozniak, Marian
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- Heterocyclic compounds having anti-diabetic activity and their use
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Compounds of formula (I): STR1 [wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an integer of from 1 to 5] have hypoglycemic and anti-diabetic activities.
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- Synthetic Routes to Nitroamino Precursors of the Food Carcinogen 2-Amino-1-methyl-6-phenyl-1H-imidazopyridine and its 3-Methyl Isomer via Pd(0)-Catalysed Arylation
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The synthesis of the novel key intermediates 3-methylamino-2-nitro- and 2-methylamino-3-nitro-5-phenylpyridine, and some of their derivatives substituted in the benzene ring, from 5-bromonicotinic acid, 3-bromo-5-methoxypyridine, 2-chloro-3-nitropyridine, 2-amino-5-bromopyridine or 5-bromo-2-methoxypyridine is described.Palladium(0)-mediated arylation of bromopyridines with areneboronic acids was an essential step in the syntheses.
- Linstroem, Stefan,Eriksson, Mikael,Grivas, Spiros
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p. 805 - 812
(2007/10/02)
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- α-Mercaptophenylacetic acid derivatives of imidazole-containing compounds and analogues thereof
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α-Mercaptobenzylacetic acid derivatives of imidazole-containing compounds and analogues thereof, and their use as immunomodulating agents are disclosed.
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