- Synthesis and Structure of 2-(1Н-Indol-1-yl)-6-ferrocenyl-4-(2-chloroimidazo[1,2-a]pyridin-3-yl)pyrimidine
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A 2,4,6-trisubstituted pyrimidine including a 2-(1H-indol-1-yl) substituent was synthesized by the reaction of 1-ferrocenyl-3-(2-chloroimidazo[1,2-a]pyridin-3-yl)propanone with 2,5-dimethoxytetrahydrofuran. The structure of the synthesized compound was confirmed by IR and 1Н NMR spectroscopy, and X-ray diffraction analysis. It has been shown that the ferrocene-containing compounds synthesized in the present work all demonstrate intramolecular charge transfer which is evidenced by the observation of the corresponding absorption bands with λmaxabs > 480 nm. The oxidation potential of ferrocene (EoxFc) in all the compounds is higher than 700 mV.
- Antuf’eva,Akhmatzyanova,Dmitriev,Shklyaeva,Abashev
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- Insights into selenylation of imidazo[1,2-a]pyridine: synthesis, structural and antimicrobial evaluation
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An efficient methodology was developed to synthesize novel organoselenium derivatives of formyl-substituted imidazo[1,2-a]pyridine by nucleophilic aromatic substitution with aryl selenolate anions generated in situ through the reduction of different disel
- Kumar, Sanjeev,Sharma, Nidhi,Maurya, Indresh K.,Verma, Ajay,Kumar, Sangit,Bhasin,Sharma, Rohit K.
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- Facile synthesis, structural evaluation, antimicrobial activity and synergistic effects of novel imidazo[1,2-a]pyridine based organoselenium compounds
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A simple and efficient method has been described to synthesize the hitherto unknown imidazo[1,2-a]pyridine selenides (5a-l) by reaction of 2-chloroimidazo [1,2-a]pyridines with aryl/heteroaryl selenols, generated in situ by reduction of various diselenide
- Kumar, Sanjeev,Sharma, Nidhi,Maurya, Indresh K.,Bhasin, Aman K.K.,Wangoo, Nishima,Brand?o, Paula,Félix, Vítor,Bhasin,Sharma, Rohit K.
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- Synthesis and antibacterial activity in?vitro of 2-benzylthioimidazo[1,2-a]pyridine derivatives against pathogenic bacterial
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To explore the antibacterial activity, a set of new 2-thiobenzyl-3-nitro-imidazo[1,2-a]pyridine derivatives were synthesized (9a–h) and characterized by NMR 1H, 13C and high-resolution mass (HRMS). These compounds were obtained by interaction between the 3-nitro-imidazo[1,2-a]pyridine isothiouronium salt (7) with benzyl chloride or bromide (8) in the presence of sodium hydroxide (NaOH). Eight (9a–h) of them were evaluated in?vitro on the positive gram bacterium (S. aureus ATCC 29213) and two others negative gram bacteria (P. aeruginosa ATCC 27853 and P. aeruginosa 933 C/21) by methods diffusion in solid medium and liquid macrodilution. Five among the eight compounds (9a, 9d, 9h, 9f and 9g) showed significant antibacterial activity on P. aeruginosa ATCC 27853 and P. aeruginosa 933 C/21with MIC between 7.81 and 250 μg/mL. All compounds were inactive on S. aureus. The compounds 9a and 9g were more potent on the two strains of P. aeruginosa ATCC 27853.
- Ablo, Evrard,Coulibali, Siomenan,Touré, Daouda,Coulibaly, Souleymane,Kablan, Ahmont Landry Claude,Konan Kouadio, Fernique,Sissouma, Drissa,Guessend Kouadio, Nathalie,Ané, Adjou
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supporting information
p. 462 - 469
(2022/02/25)
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- Synthesis and Physicochemical Properties of New Chalcones Containing a 2-Chloroimidazo[1,2-a]pyridine Fragment
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Abstract: New chalcones containing a 2-chloroimidazo[1,2-a]pyridine fragment have been synthesized, and their optical properties have been studied. The Stokes shifts, forbidden band gap widths, molar absorption coefficients, and fluorescence quantum yields have been determined on the basis of their absorption and emission spectra. Introduction of an additional thiophene fragment into the chalcone molecules produced an increase of the Stokes shift, red shift of the emission maximum, and sharp increase of the quantum yield (up to 22%). The synthesized chalcones showed high thermal stability and good film-forming properties, and films obtained therefrom exhibited an ordered structure.
- Abashev, G. G.,Chukhlantseva, A. N.,Ermolov, D. A.,Lunegov, I. V.,Mokrushin, I. G.,Shklyaeva, E. V.
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p. 1940 - 1947
(2022/01/24)
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- Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
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Despite the therapeutic relevance of δ-containing γ-aminobutyric acid type A receptors (GABAARs) and the need for δ-selective compounds, the structural determinants for the mode and molecular site of action of δ-selective positive allosteric modulator imi
- Rostrup, Frederik,Falk-Petersen, Christina B.,Harpsoe, Kasper,Buchleithner, Stine,Conforti, Irene,Jung, Sascha,Gloriam, David E.,Schirmeister, Tanja,Wellendorph, Petrine,Frolund, Bente
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p. 4730 - 4743
(2021/05/06)
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- FUSED HETEROCYCLIC COMPOUNDS AND THEIR USE AS PEST CONTROL AGENTS
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The present invention discloses a fused heterocyclic compound of formula (I), wherein, R1, Y, Q, A, G,m and E are as defined in the detailed description. The present invention further discloses methods for their preparation and use of the compounds of formula (I) as a pest control agent.
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Page/Page column 91
(2020/12/30)
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- Double (amino-sulfur generation of formic acid ) - 1,3-propane diester compound and its synthetic method, pharmaceutical composition and use thereof
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The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.
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Paragraph 0330-0333
(2016/10/08)
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- HETERO-CYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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The present specification relates to a novel heterocyclic compound and an organic light-emitting device using the same. According to one embodiment of the present specification, provided is a compound in chemical formula 1. The compound of the present specification can be used as an organic matter layer material of an organic light-emitting device.COPYRIGHT KIPO 2016
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Paragraph 0140-0143
(2016/10/08)
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- Exploration of versatile reactions on 2-chloro-3-nitroimidazo[1,2-a] pyridine: Expanding structural diversity of C2- and C3-functionalized imidazo[1,2-a]pyridines
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Alternative strategies for functionalizing 2-chloro-3-nitroimidazo[1,2-a] pyridine have been developed. Suzuki-Miyaura cross-coupling reaction provided easily the corresponding 2-arylated compounds, and herefrom the nitro group was reduced into amine which afforded amides, anilines, and ureas in the 3-position. The amination of the key compound using a metal-catalyzed reaction was reported. This study highlighted the importance of the nitro group to facilitate the chlorine displacement. Other nucleophilic aromatic substitutions open a route to various products derived from imidazo[1,2-a]pyridine.
- Bazin, Marc-Antoine,Marhadour, Sophie,Tonnerre, Alain,Marchand, Pascal
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p. 5378 - 5382
(2013/09/12)
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- An efficient access to 2,3-diarylimidazo[1,2-a]pyridines via imidazo[1,2-a]pyridin-2-yl triflate through a Suzuki cross-coupling reaction-direct arylation sequence
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An efficient method to prepare 2,3-diarylimidazo[1,2-a]pyridines is described. The procedure involves a Suzuki cross-coupling reaction followed by a direct arylation at position 3. Imidazo[1,2-a]pyridin-2-yl triflate was identified as a suitable coupling partner, permitting access to a variety of highly functionalized 2,3-diarylimidazo[1,2-a]pyridines.
- Marhadour, Sophie,Bazin, Marc-Antoine,Marchand, Pascal
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scheme or table
p. 297 - 300
(2012/01/31)
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- Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors
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mTOR is a critical regulator of cellular signaling downstream of multiple growth factors. The mTOR/PI3K/AKT pathway is frequently mutated in human cancers and is thus an important oncology target. Herein we report the evolution of our program to discover ATP-competitive mTOR inhibitors that demonstrate improved pharmacokinetic properties and selectivity compared to our previous leads. Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine scaffolds were identified that demonstrated superior inhibition of mTOR in cellular assays, selectivity over the closely related PIKK family and improved in vivo clearance over our previously reported benzimidazole series.
- Peterson, Emily A.,Boezio, Alessandro A.,Andrews, Paul S.,Boezio, Christiane M.,Bush, Tammy L.,Cheng, Alan C.,Choquette, Deborah,Coats, James R.,Colletti, Adria E.,Copeland, Katrina W.,Dupont, Michelle,Graceffa, Russell,Grubinska, Barbara,Kim, Joseph L.,Lewis, Richard T.,Liu, Jingzhou,Mullady, Erin L.,Potashman, Michele H.,Romero, Karina,Shaffer, Paul L.,Stanton, Mary K.,Stellwagen, John C.,Teffera, Yohannes,Yi, Shuyan,Cai, Ti,La, Daniel S.
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scheme or table
p. 4967 - 4974
(2012/09/07)
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- PYRIMIDINE INHIBITORS OF KINASE ACTIVITY
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Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, L1, R2, R3, n, p, Ar1, and Ar2 are defined in the description. Methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR are also disclosed.
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Page/Page column 55
(2010/12/26)
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- PYRIMIDINE INHIBITORS OF KINASE ACTIVITY
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR.
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Page/Page column 59-60
(2010/12/26)
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