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Journal articles on the topic 'Pyrazine Amides'

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1

Allen, Annette D., Andrei V. Fedorov, Nanyan Fu, et al. "Pyrazinyl- and pyrimidinylketenes, bisketenes, and ylides: direct observation and nucleophilic reactivity." Canadian Journal of Chemistry 92, no. 12 (2014): 1119–30. http://dx.doi.org/10.1139/cjc-2014-0208.

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Pyrazinylketene (9) and 4-pyrimidinylketene (11), identified by their IR absorption at 2128 and 2130 cm−1, respectively, are formed in CH3CN as transient intermediates by photolysis of the corresponding diazoketones. The corresponding ylides 10 and 12 are formed concurrently as longer-lived intermediates identified by their distinctive IR and UV absorption. Reactions of 2-pyridylketene and of 9 and 11 with diethylamine form initial amide enol intermediates leading to dihydroheteroarene intermediates and then to amides, whereas amide enols are not observed in reactions with n-butylamine. Reacti
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2

Zitko, Jan, Alžběta Mindlová, Ondřej Valášek, et al. "Design, Synthesis and Evaluation of N-pyrazinylbenzamides as Potential Antimycobacterial Agents." Molecules 23, no. 9 (2018): 2390. http://dx.doi.org/10.3390/molecules23092390.

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Three series of N-(pyrazin-2-yl)benzamides were designed as retro-amide analogues of previously published N-phenylpyrazine-2-carboxamides with in vitro antimycobacterial activity. The synthesized retro-amides were evaluated for in vitro growth inhibiting activity against Mycobacterium tuberculosis H37Rv (Mtb), three non-tuberculous mycobacterial strains (M. avium, M. kansasii, M. smegmatis) and selected bacterial and fungal strains of clinical importance. Regarding activity against Mtb, most N-pyrazinylbenzamides (retro-amides) possessed lower or no activity compared to the corresponding N-phe
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3

Wackerbarth, Ines, Ni Nyoman Agnes Tri Widhyadnyani, Simon Schmitz, et al. "CuII Complexes and Coordination Polymers with Pyridine or Pyrazine Amides and Amino Benzamides—Structures and EPR Patterns." Inorganics 8, no. 12 (2020): 65. http://dx.doi.org/10.3390/inorganics8120065.

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Isonicotine amide, picoline amide, pyrazine 2-amide, 2- and 4-amino benzamides and various CuII salts were used to target CuII complexes of these ligands alongside with 1D and 2D coordination polymers. Under the criterion of obtaining crystalline and single phased materials a number of new compounds were reliably reproduced. Remarkably, for some of these compounds the ideal Cu:ligand ratio of the starting materials turned out to be very different from Cu:ligand ratio in the products. Crystal and molecular structures from single-crystal XRD were obtained for all new compounds; phase purity was
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4

Dolezal, Martin, Miroslav Miletin, Jiri Kunes, and Katarina Kralova. "Substituted Amides of Pyrazine-2-carboxylic acids: Synthesis and Biological Activity." Molecules 7, no. 3 (2002): 363–73. http://dx.doi.org/10.3390/70300363.

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5

Grill, Birgit, Maximilian Glänzer, Helmut Schwab, et al. "Functional Expression and Characterization of a Panel of Cobalt and Iron-Dependent Nitrile Hydratases." Molecules 25, no. 11 (2020): 2521. http://dx.doi.org/10.3390/molecules25112521.

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Nitrile hydratases (NHase) catalyze the hydration of nitriles to the corresponding amides. We report on the heterologous expression of various nitrile hydratases. Some of these enzymes have been investigated by others and us before, but sixteen target proteins represent novel sequences. Of 21 target sequences, 4 iron and 16 cobalt containing proteins were functionally expressed from Escherichia coli BL21 (DE3) Gold. Cell free extracts were used for activity profiling and basic characterization of the NHases using the typical NHase substrate methacrylonitrile. Co-type NHases are more tolerant t
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6

Ghosh, Arun K., Wayne J. Thompson, M. Katharine Holloway, et al. "Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands." Journal of Medicinal Chemistry 36, no. 16 (1993): 2300–2310. http://dx.doi.org/10.1021/jm00068a006.

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7

Tumova, Lenka, Katerina Gallova, Jana Rimakova, Martin Dolezal, and Jiri Tuma. "The effect of substituted amides of pyrazine-2-carboxylic acids on flavonolignan production in Silybum marianum culture in vitro." Acta Physiologiae Plantarum 27, no. 3 (2005): 357–62. http://dx.doi.org/10.1007/s11738-005-0012-8.

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8

Zhou, Yan Mei, Yong Wei, Jin Yang, Hai Hai Li, Miao Deng Liu, and Nian Yu Huang. "Synthesis and In Vitro Anti-Inflammatory Activity of Pyrrolo[1,2-A]pyrazines via Pd-Catalyzed Intermolecular Cyclization Reaction." Advanced Materials Research 830 (October 2013): 115–18. http://dx.doi.org/10.4028/www.scientific.net/amr.830.115.

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Pyrrolo [1,2-a] pyrazine possessed widely bioactivities due to its particular structure. In this work, three pyrrolo [1,2-a] pyrazines derivatives were synthesized from the 2-bromo-5-methoxypyrazine and propargyl amines or ethers through the Pd-catalyzed intermolecular cycloisomerization strategy. Their structures were characterized by NMR, IR, EI-MS and elemental analysis, and all of them exhibited moderatein vitroanti-inflammatory effects with the inhibitions of 43-59% against IL-6 at 50 μM. The compound3crevealed relatively good anti-inflammatory activities. The bioactive pyrrolo [1,2-a] py
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9

GHOSH, A. K., W. J. THOMPSON, M. K. HOLLOWAY, et al. "ChemInform Abstract: Potent HIV Protease Inhibitors: The Development of Tetrahydrofuranylglycines as Novel P2-Ligands and Pyrazine. Amides as P3-Ligands." ChemInform 24, no. 52 (2010): no. http://dx.doi.org/10.1002/chin.199352194.

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10

Mukhopadhyay, Uday, Richard Galian та Ivan Bernal. "Metal induced cleavage of amide bonds. Part 3. Cleavage of aromatic amides and isolation of [cis-α-Co(trien) (salicylamide)](ClO4)2 (I), Co(tren)(pyrazine-2-carboxylato)](ClO4)2·2H2O (II) and [Co(tren)(pyrazine-2,3-dicarboxylatomonoamide)](ClO4)Cl (III)". Inorganica Chimica Acta 362, № 11 (2009): 4237–40. http://dx.doi.org/10.1016/j.ica.2009.05.034.

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11

Bouz, Ghada, Martin Juhás, Lluis Pausas Otero, et al. "Substituted N-(Pyrazin-2-yl)benzenesulfonamides; Synthesis, Anti-Infective Evaluation, Cytotoxicity, and In Silico Studies." Molecules 25, no. 1 (2019): 138. http://dx.doi.org/10.3390/molecules25010138.

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We prepared a series of substituted N-(pyrazin-2-yl)benzenesulfonamides as an attempt to investigate the effect of different linkers connecting pyrazine to benzene cores on antimicrobial activity when compared to our previous compounds of amide or retro-amide linker type. Only two compounds, 4-amino-N-(pyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 25 μM) and 4-amino-N-(6-chloropyrazin-2-yl)benzenesulfonamide (MIC = 6.25 μg/mL, 22 μM) exerted good antitubercular activity against M. tuberculosis H37Rv. However, they were excluded from the comparison as they—unlike the other compounds—posses
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12

Jyothi, Boggavarapu, and Nannapaneni Madhavi. "Green Synthesis and Antimicrobial Activity of Some Novel N-Arylimidazo[1,2-a]pyrazine-2-Carboxamide Derivatives." Asian Journal of Chemistry 32, no. 1 (2019): 84–90. http://dx.doi.org/10.14233/ajchem.2020.22365.

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The article deals with the synthesis of some novel N-arylimidazo[1,2-a]pyrazine-2-carboxamides (7a-l) by condensation reaction of imidazo[1,2-a]pyrazine-2-carboxylic acid (5) with different aliphatic/aromatic amines (6a-l) by using 1-methylimidazole, Mukaiyama’s reagent and 2-chloro-1-methylpyridinium iodide under microwave irradiation conditions. A new series of compounds 7 have been prepared from 2-iodopyrazine (1). Compound 1 on purged with ammonia gas in the presence of Cu2O and K2CO3 furnishes pyrazin-2-amine (2), which is treated with ethyl 3-bromo-2-oxopropanoate (3) to produce ethyl im
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13

Sharma, Shubham, Dharmender Singh, Sunit Kumar, et al. "An efficient metal-free and catalyst-free C–S/C–O bond-formation strategy: synthesis of pyrazole-conjugated thioamides and amides." Beilstein Journal of Organic Chemistry 19 (March 2, 2023): 231–44. http://dx.doi.org/10.3762/bjoc.19.22.

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An operationally simple and metal-free approach is described for the synthesis of pyrazole-tethered thioamide and amide conjugates. The thioamides were generated by employing a three-component reaction of diverse pyrazole C-3/4/5 carbaldehydes, secondary amines, and elemental sulfur in a single synthetic operation. The advantages of this developed protocol refer to the broad substrate scope, metal-free and easy to perform reaction conditions. Moreover, the pyrazole C-3/5-linked amide conjugates were also synthesized via an oxidative amination of pyrazole carbaldehydes and 2-aminopyridines usin
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14

Akbar, Siddiqui, Sagathevan, Iqbal, and Khan. "Gut Bacteria of Water Monitor Lizard (Varanus salvator) Are a Potential Source of Antibacterial Compound(s)." Antibiotics 8, no. 4 (2019): 164. http://dx.doi.org/10.3390/antibiotics8040164.

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For the past few decades, there has been limited progress in the development of novel antibacterials. Previously, we postulated that the gut microbiota of animals residing in polluted environments are a forthcoming supply of antibacterials. Among various species, the water monitor lizard is an interesting species that feeds on organic waste and the carcass of wild animals. Gut microbiota of the water monitor lizard were sequestered, identified and cultivated in RPMI-1640 to produce conditioned medium (CM). Next, the antimicrobial properties of CM were evaluated versus a selection of Gram-negat
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15

Smith, Henry S. T., Ben Giuliani, Kanchana Wijesekera, et al. "Investigations of amination reactions on an antimalarial 1,2,4-triazolo[4,3-a]pyrazine scaffold." Beilstein Journal of Organic Chemistry 21 (June 10, 2025): 1126–34. https://doi.org/10.3762/bjoc.21.90.

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1,2,4-Triazolo[4,3-a]pyrazines have previously been explored by the Open Source Malaria project as potent in vitro and in vivo antimalarial drug leads. With a view to generating a library of unique antimalarial 1,2,4-triazolo[4,3-a]pyrazines and exploring regiochemical preference for nucleophilic amines, we utilised the known synthetic 5-chloro-3-(4-chlorophenyl)-[1,2,4]triazolo[4,3-a]pyrazine (1) as a scaffold for aminations with 14 commercially available primary amines. Reacting scaffold 1 with excess primary amine at room temperature for 16 h generated the desired amine analogues in respect
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16

Morteza, Shiri, and Bozorgpour‑Savadjani Zahra. "Highly selective base-catalyzed ring closing Ugi-adducts from the reaction of 2-formylindole, 2-bromoacetic acid, amines and isocyanides." Journal of the Iranian Chemical Society 12, no. 3 (2014): 389–96. https://doi.org/10.1007/s13738-014-0495-6.

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The intermediate products of the Ugi reaction between indole-2-carboxaldehyde, 2bromoacetic acid, amines and isocyanides were treated with Cs2CO3 in DMF to form a series of novel cyclized 1,2-dihydropyrazino[1,2a]indol-3(4H)-ones (indole –NH cyclization) as major and piperazin-2-ones (amide –NH cyclization) as minor products.
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17

Yu, Xia, Deshang Meng, Qingchun Zhao, Lianting Liang, and Lili Cui. "Analysis and Comparison of Volatile Compounds in Stropharia Rugosoannulata and Tricholoma Lobayense by Headspace Solid-Phase Microextraction-Gas Chromatography-Mass Spectrometry." Current Topics in Nutraceutical Research 22, no. 4 (2024): 1132–38. http://dx.doi.org/10.37290/ctnr2641-452x.22:1132-1138.

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The volatile components of Stropharia rugosoannulata and Tricholoma lobayense were analyzed by mass spectrometry, and the relative contents of each component were determined by the internal standard method. In Stropharia rugosoannulata, 58 volatile components were identified, including 10 alcohols, 14 esters, 9 aldehydes, 5 ketones, 1 phenol, 3 alkanes, 4 amines, 5 acids, 1 furan, 1 pyrazine, 1 olefin, 1 oxime, 1 pyrazole, and 2 other components. Among them, the most abundant volatile component was hexanal (1655.40 ng/g), followed by pentanoic acid (1503.10 ng/g) and phenylethyl alcohol (1215.
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18

Parsonidis, Panagiotis, Mahammad Shaik, Athanasia Panagiota Serafeim, Ioanna Vlachou, Vasiliki Daikopoulou, and Ioannis Papasotiriou. "Design, Synthesis, and In Vitro Activity of Pyrazine Compounds." Molecules 24, no. 23 (2019): 4389. http://dx.doi.org/10.3390/molecules24234389.

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Despite the fact that there are several anticancer drugs available, cancer has evolved using different pathways inside the cell. The protein tyrosine phosphatases pathway is responsible for monitoring cell proliferation, diversity, migration, and metabolism. More specifically, the SHP2 protein, which is a member of the PTPs family, is closely related to cancer. In our efforts, with the aid of a structure-based drug design, we optimized the known inhibitor SHP099 by introducing 1-(methylsulfonyl)-4-prolylpiperazine as a linker. We designed and synthesized three pyrazine-based small molecules. W
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19

Ghoshal, Anirban, Álvaro F. Magalhães, Kesatebrhan Haile Asressu, Mohammad Anwar Hossain, Matthew H. Todd та Timothy M. Willson. "Identification of Dihydropyrazolo[1,5-a]pyrazin-4(5H)-ones as Cyclic Products of β-Amidomethyl Vinyl Sulfone Alphavirus Cysteine Protease Inhibitors". Pharmaceuticals 17, № 7 (2024): 836. http://dx.doi.org/10.3390/ph17070836.

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Optimized syntheses of (E)-5-(2-ethoxyphenyl)-N-(3-(methylsulfonyl)allyl)-1H-pyrazole-3-carboxamide (RA-0002034, 1), a promising antiviral covalent cysteine protease inhibitor lead, were developed. The syntheses avoid the contamination of 1 with the inactive cyclic dihydropyrazolo[1,5-a]pyrazin-4(5H)-one 2, which is formed by the intramolecular aza-Michael reaction of the vinyl sulfone warhead under basic conditions and slowly at pH 7.4 in phosphate buffer. The pure cysteine protease inhibitor 1 could be synthesized using either modified amide coupling conditions or through the introduction of
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20

Ma, Shuchao, Ben Ouyang, Linan Wang, and Lei Yao. "Design and Biological Evaluation of 3-Aryl-4-alkylpyrazol-5-amines Based on the Target Fishing." Current Computer-Aided Drug Design 16, no. 5 (2020): 564–70. http://dx.doi.org/10.2174/1573409915666191003123900.

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Background: Pyrazol-5-amine derivatives are an important class of heterocyclic compounds. However, there are less 4-alkyl substituted pyrazoles reported. Objective: Here reported are the design, synthesis and biological evaluation of 3-aryl-4- alkylpyrazol-5-amines derivatives. Methods: A serials of 3-aryl-4-alkylpyrazol-5-amines were designed and the biological action targets were screened by target fishing function of Discovery Studio software. The synthesis route involved 3-oxo-3-arylpropanenitrile formation, alkylation, pyrazole formation, and amides formation. The antitumor activities of
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21

Blass, Benjamin. "Novel Pyrazine Amide Compounds." ACS Medicinal Chemistry Letters 6, no. 7 (2015): 729–31. http://dx.doi.org/10.1021/acsmedchemlett.5b00186.

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22

Sui, Liqiang, Sugui Wang, Xin Wang, et al. "Analysis of Different Strains Fermented Douchi by GC×GC-TOFMS and UPLC–Q-TOFMS Omics Analysis." Foods 13, no. 21 (2024): 3521. http://dx.doi.org/10.3390/foods13213521.

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Douchi is a kind of soybean-fermented food in China. To explore the common and differential compounds in different Douchi, Douchi was fermented by Aspergillus niger, Rhizopus arrhizus, and Bacillus circulans, respectively, and co-fermented by the three strains in this study. The common and characteristic flavor compounds and common and characteristic non-volatile components of different strains of fermented Douchi were explored through GC×GC-TOFMS and UPLC–Q-TOFMS omics analysis. The result suggested that Pyrazines, ketones, and alkenes such as tetramethyl-pyrazine, 2,5-dimethyl pyrazine, fura
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23

Li, Feng-Cai, Xi-Li Li, Li-Kun Tan, Jin-Tang Wang, and Wei-Zhong Yao. "Evans–Showell-type polyoxometalate-based metal–organic complexes with novel 3D structures constructed from flexible bis-pyrazine–bis-amide ligands and copper metals: syntheses, structures, and fluorescence and catalytic properties." Dalton Transactions 48, no. 6 (2019): 2160–69. http://dx.doi.org/10.1039/c8dt04698k.

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24

Li, Feng-Cai, Li-Kun Tan, Xi-Li Li, et al. "Syntheses, structures and catalytic properties of Evans–Showell-type polyoxometalate-based 3D metal–organic complexes constructed from the semi-rigid bis(pyridylformyl)piperazine ligand and transition metals." Dalton Transactions 48, no. 17 (2019): 5831–41. http://dx.doi.org/10.1039/c9dt00499h.

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25

Wang, Xiu-Li, Dan-Na Liu, Hong-Yan Lin, et al. "Application of flexible bis-pyrazine–bis-amide ligands to construct various polyoxometalate-based metal–organic complexes." RSC Advances 5, no. 70 (2015): 56687–96. http://dx.doi.org/10.1039/c5ra09529h.

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Five novel polyoxometalates-based metal–organic complexes constructed from different types of polyanions and flexible bis-pyrazine–bis-amide ligands with different spacer lengths have been hydrothermally synthesized and structurally characterized.
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26

Cui, Zi-Wei, Jun-Jun Lu, Hong-Yan Lin, et al. "Four Keggin-type polyoxometalate-based complexes derived from bis(pyrazine)–bis(amide) ligands for electrochemical sensing of multiple analytes and adsorbing dye molecules." CrystEngComm 24, no. 4 (2022): 828–36. http://dx.doi.org/10.1039/d1ce01403j.

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Four new Keggin-based complexes derived from bis(pyrazine)–bis(amide) ligands are used to detect multiple analytes (BrO3− NO2−, Cr(vi) and Fe(iii) ions) and adsorb organic dye molecules from aqueous solution.
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27

Genç, Hasan, Volkan Taşdemir, İsrafil Tozlu, and Erdal Ögün. "Synthesis of Novel Tetra-Substituted Pyrazole Derivatives from 2,3- Furandione." Letters in Organic Chemistry 16, no. 11 (2019): 891–97. http://dx.doi.org/10.2174/1570178616666190314150302.

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Synthesis of pyrazole-3-carboxylic acid was progressed via two different protocols, one of which is solid state. Pyrazole-3-carboxylic acid was converted into different derivatives such as ester, urea, amide and nitrile. The amide compound was converted to nitrile using SOCl2 and DMF. Solid state heating of carboxylic acid gave decarboxylated product. Cyclization of tetra-substituted pyrazole with hydrazines resulted in pyrazolopyridazinones. The antimicrobial activities of the synthesized pyrazole derivatives against Bacillus cereus, Escherichia coli, Micrococcus luteus, Staphylococcus aureus
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28

Ferland, Jean-Marie, Christopher A. Demerson, and Leslie G. Humber. "Synthesis of derivatives of isoindole and of pyrazino[2,1-a]isoindole." Canadian Journal of Chemistry 63, no. 2 (1985): 361–65. http://dx.doi.org/10.1139/v85-061.

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Amines were reacted with lactones 7 or with unsaturated nitro derivatives 8 to give isoindole and pyrazino[2,1-a]isoindole derivatives. The mechanisms of formation, proofs of structure, and stereochemistry are presented.
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29

Ashram, Muhammad, Ahmed Al-Mustafa, Wael A. Al-Zereini, Firas F. Awwadi, and Islam Ashram. "A convenient one-pot approach to the synthesis of novel pyrazino[1,2-a]indoles fused to heterocyclic systems and evaluation of their biological activity as acetylcholinesterase inhibitors." Zeitschrift für Naturforschung B 76, no. 5 (2021): 303–12. http://dx.doi.org/10.1515/znb-2020-0205.

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Abstract Pyrazino[1,2-a]indoles fused with various heterocycles, such as oxazolidine, oxazinane, imidazolidine, hexahydropyrimidine and benzimidazole, were synthesized transition metal-free by domino reactions which involved the condensation of 1-(2-bromoethyl)-3-chloro-1H-indole-2-carbaldehydes 28–31 with various nucleophilic amines, resulting in the formation of two new interesting fused heterocycles. The anticholinesterase, antioxidant and antibacterial activities of the compounds were evaluated. Acetylcholinesterase (AChE) inhibitory activities were tested by Ellman’s assay, antioxidant ac
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30

Al-Smaisim, Rafah F., Redha E. Al-Bayati, and Abdul Hussain K. Sharba. "Synthesis of New Heterocyclic compounds derived from Pyrazoline-5-one compound." Al Mustansiriyah Journal of Pharmaceutical Sciences 9, no. 1 (2011): 123–31. http://dx.doi.org/10.32947/ajps.v9i1.278.

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In this work new heterocyclic pyrazolin derivatives have been synthesized from diazonium chloride salt of 4-aminobenzoic acid: firstly, Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, (ethyl acetoacetate)obtain the corresponding hydrazono derivative (1). Secondly, Cyclocondensation reaction of compound (1) with hydrazine hydrate (2) in boiling ethanol affording the corresponding pyrazoline-5-one. Then compound (2) reacted with thionyl chloride to give the corresponding acid chloride derivative(3
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31

Hearne, Neil, Mark M. Turnbull, Christopher P. Landee, Elizabet M. van der Merwe, and Melanie Rademeyer. "Halide-bi-bridged polymers of amide substituted pyridines and -pyrazines: polymorphism, structures, thermal stability and magnetism." CrystEngComm 21, no. 12 (2019): 1910–27. http://dx.doi.org/10.1039/c9ce00071b.

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The structural trends, polymorphic behaviour, magnetic properties and thermal stability of a family of halide-bi-bridged polymers of CuX<sub>2</sub> and amide-substituted pyridines and -pyrazines are reported, and compared with related compounds in the literature.
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32

Saha, Supriyo, Dilipkumar Pal, and Satish B. Nimse. "Recent Advances in the Discovery of GSK-3 Inhibitors from Synthetic Origin in the Treatment of Neurological Disorders." Current Drug Targets 22, no. 12 (2021): 1437–62. http://dx.doi.org/10.2174/1389450122666210120143953.

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Background: Glycogen synthase kinase 3 (GSK-3) is a serine/threonine kinase enzyme that controls neuronal functions such as neurite outgrowth, synapse formation, neurotransmission, and neurogenesis. The enzyme has two subunits as GSK-3α and GSK-3β. 4ACC, 1Q3D, 3AFG, 1UV5, and 1Q5K are the important GSK-3 receptors isolated from Homo sapiens and Mus musculus. This enzyme mainly phosphorylates Tau protein with the increased amount in neuronal fibres together with beta-amyloid plaques that cause neuronal diseases like Alzheimer's, Parkinson’s and many more. Objective: We investigated the developm
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33

Pattan, S. R., P. A. Chavan, R. A. Muluk, et al. "SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME HETEROCYCLES CONTAINING OXADIAZOLE AND PYRAZOLE RING FOR ANTI-BACTERIAL, ANTI-FUNGAL AND ANTI-TUBERCULAR ACTIVITIES." INDIAN DRUGS 49, no. 03 (2012): 18–24. http://dx.doi.org/10.53879/id.49.03.p0018.

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1, 3, 4-oxadiazoles were synthesized by treating pyrazine-2-carbohydrazide with CS2 and alc. KOH and their derivatives were prepared by using R-Cl compounds. pyrazolones were synthesized by treatingpyrazine-2-carbohydrazide with ethyl acetoacetate. The derivatives of pyrazolone were prepared by refluxing pyrazolone with formaldehyde and different substituted secondary amines. All the synthesized compounds were characterized by IR, 1H-NMR and elemental analysis and evaluated for antibacterial, antifungal and antitubercular activities.
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34

Badavath, Vishnu Nayak, Venkatesan Jayaprakash, Susanta Kumar Mondal, et al. "Pharmacokinetic Studies of Curcumin Based Pyrazoline MAO Inhibitors." Journal of Pharmaceutical Technology, Research and Management 8, no. 2 (2020): 85–89. http://dx.doi.org/10.15415/jptrm.2020.82012.

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Background: Curcumin is a natural phenolic compound obtained from Curcuma longa, with proven human monoamine oxidase (MAO) inhibitory activity, but due to its poor oral bioavailability, blood-brain barrier permeability and extensive metabolism in the liver, it has never been recognized as a drug candidate. Purpose: In this study, the structure-based-drug design (SBDD) was adopted to incorporate the structural features of Curcumin with an aim to improve drug permeability and metabolic stability. Method: A series of ferulic amides (half portion of curcumin) (1-3) and curcumin based pyrazolinesco
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35

Kaur, Manpreet, Jerry P. Jasinski, H. S. Yathirajan, B. Narayana, and K. Byrappa. "N-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-2-(4-nitrophenyl)acetamide." Acta Crystallographica Section E Structure Reports Online 70, no. 6 (2014): o636—o637. http://dx.doi.org/10.1107/s1600536814009738.

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In the title compound, C19H18N4O4, the nitrophenyl and phenyl rings are twisted by 67.0 (6) and 37.4 (4)°, respectively, with respect to the pyrazole ring plane [maximum deviation = 0.0042 (16) Å]. The dihedral angle between the mean planes of the phenyl rings is 59.3 (3)°. The amide group, with a C—N—C—C torsion angle of 177.54 (13)°, is twisted away from the plane of the pyrazole ring in an antiperiplanar conformation. In the crystal, N—H...O hydrogen bonds involving the carbonyl group on the pyrazole ring and the amide group, together with weak C—H...O interactions formingR22(10) graph-set
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36

Savić, Jelena, Marija Antonijević, Milkica Crevar, and Jasmina Brborić. "Docking studies of some pyrazole containing compounds in the cyclooxygenase-2 active site." Arhiv za farmaciju 73, no. 3 (2023): 205–15. http://dx.doi.org/10.5937/arhfarm73-44720.

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Whereas nonselective nonsteroidal anti-inflammatory drugs, such as aspirin, ibuprofen and diclofenac, inhibit both cyclooxygenase-1 and cyclooxigenase-2 enzymes, selective inhibitors target cyclooxygenase-2, which is overexpressed in inflammation, but also in cancer, atherosclerosis, Alzheimer's disease, and Parkinson's disease. Potential cardiovascular and hepatic side effects of cyclooxygenase-2 inhibitors have limited their use. The development of selective and safe cyclooxygenase-2 inhibitors remains a high priority in drug discovery. Based on the structure of previously investigated newly
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37

Hu, Jun, Jikui Wang, Taoyu Zhou, and Yanhua Xu. "Microwave-Assisted Synthesis of Tetrazolyl Pyrazole Amides." Journal of Chemical Research 35, no. 9 (2011): 525–27. http://dx.doi.org/10.3184/174751911x13149561530439.

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38

Stiborová, Marie, and Sylva Leblová. "Effect of heterocyclic compounds and 2-mercaptoethanol on rape alcohol dehydrogenase." Collection of Czechoslovak Chemical Communications 52, no. 8 (1987): 2107–13. http://dx.doi.org/10.1135/cccc19872107.

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Rape alcohol dehydrogenase (ADH) is inhibited by heterocyclic compounds with a five- to six-membered ring (imidazole, pyrazole, 4-methylpyrazole, 3-methylpyrazole, pyridine, nicotine amide) and by o-phenanthroline, a heterocyclic, polycyclic compound. Pyrazole and its derivatives, imidazole and pyridine, are competitive inhibitors with respect to ethanol. Nicotine amide and o-phenanthroline behave as mixed inhibitors (competitive – noncompetitive) with respect to the substrate. The addition of Zn2+-ions to the reaction medium interferes with the competition by o-phenanthroline. 4-Methylpyrazol
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39

Mokrov, G. V., А. S. Pantileev, М. А. Yarkova, et al. "Design, Synthesis, and Study of the Anxiolytic Activity of New Pyrrolo[1,2-<i>a</i>]pyrazine-Containing TSPO Ligands." Биоорганическая химия 49, no. 2 (2023): 188–206. http://dx.doi.org/10.31857/s0132342323020173.

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A new group of 1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamides, in which substituents at the amide nitrogen atom are alkyl, benzyl or alkoxyphenylalkyl groups, amino acid residues or their derivatives, has been obtained in this work. The synthesized compounds have high theoretical affinities for the 18 kDa translocator protein (TSPO) and a favorable profile of ADMET characteristics, which makes them promising for drug development. Anxiolytic activity was detected for eight compounds at doses of 0.1–5.0 mg/kg when administered intraperitoneally under conditions of emotional stress in the open fie
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40

Howells, Rachel L., Scott G. Lamont, Thomas M. McGuire, et al. "Synthesis of Novel Pyrazine-Substituted 1H-Pyrrole-2-carboxamides and Related Tethered Heterocycles." Synthesis 54, no. 09 (2022): 2267–81. http://dx.doi.org/10.1055/s-0040-1719873.

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AbstractAs part of a drug discovery program, 4-pyrazin-2-yl-1H-pyrrole-2-carboxamides were accessed along with a number of bicyclic analogues. Routes to these compounds were largely absent from the scientific literature. The synthesis of a 4-(pyrazin-2-yl)-1H-pyrrole-2-carboxamide and several fused bicyclic analogues all using standard procedures (SNAr, borylation, C–C cross couplings, hydrolysis, amide bond formation, cyclisation, halogenation, and alkylation) from readily available starting materials is reported. The synthetic sequences range from 4–12 steps per final compound, with yields o
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41

Kaur, Manpreet, Jerry P. Jasinski, Brian J. Anderson, H. S. Yathirajan, and B. Narayana. "N-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-2-phenylacetamide." Acta Crystallographica Section E Structure Reports Online 69, no. 12 (2013): o1726—o1727. http://dx.doi.org/10.1107/s1600536813029590.

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The title compound, C19H19N3O2, crystallizes with two independent molecules (AandB) in the asymmetric unit. In moleculeA, the pyrazole ring adopts a slightly disordered half-chair conformation while inBit is planar [r.m.s. deviation = 0.0386 (15) Å]. The dihedral angle between the mean planes of the two phenyl rings is 56.2 (8) inAand 38.2 (3)° inB. TheN-phenyl substituent on the pyrazole ring is twisted by 46.5 (2) inAand 58.6 (4)° inBwhile the extended phenyl ring is twisted by 82.2 (8) inAand 87.5 (9)° inB. The mean plane of the amide group forms an angle of 74.8 (3) inAand 67.7 (1)° inBwit
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42

Berl, Jelena K., Christian Czaschke, Ann-Kathrin Pramor, Christian B. W. Stark, and Joachim Thiem. "Serendipitous Conversion of an Acetylamino Dideoxy-Octonic Acid Derivate into a Functionalized Carbohydrate–Pyrazole Conjugate and Investigation of the Method´s General Applicability." Molecules 29, no. 20 (2024): 4885. http://dx.doi.org/10.3390/molecules29204885.

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By treatment of the peracetylated methylester of 4-acetylamino-2,4-dideoxy-d-glycero-d-galacto-octonic acid (ADOA-PAE) with nitrosyl tetrafluoroborate, a serendipitous formation of a highly functionalized carbohydrate–pyrazole conjugate was observed in 95% yield. This observation is remarkable, as it involves a five-step one-pot synthesis that proceeds via an 1,3-acyl shift and a 1,5-electrocyclization, which usually requires thermal conditions; however, the reaction occurred at a temperature of 0 °C. Additionally, the excellent yield of the carbohydrate-decorated pyrazole and the regiospecifi
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43

Journal, Baghdad Science. "Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid." Baghdad Science Journal 7, no. 1 (2010): 727–36. http://dx.doi.org/10.21123/bsj.7.1.727-736.

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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid
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44

Brimble, MA, MT Brimble, R. Hodges, and GA Lane. "Synthesis of 2-Methylpyrrolo[1,2-a]pyrazin-1(2h)-one." Australian Journal of Chemistry 41, no. 10 (1988): 1583. http://dx.doi.org/10.1071/ch9881583.

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The synthesis of 2-methylpyrrolo[1,2-a]pyrazin-1(2H)-one (2) present in the insect feeding deterrent peramine (1) through oxidation of the saturated lactam (3) is described. The preparation of the related 6- methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one (12) through a Lewis-acid- catalysed cyclization of the amide acetal (7) is also described.
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45

Hasan, Muhammad, Anatoly A. Peshkov, Syed Anis Ali Shah, et al. "Silver(I) triflate-catalyzed post-Ugi synthesis of pyrazolodiazepines." Beilstein Journal of Organic Chemistry 21 (May 8, 2025): 915–25. https://doi.org/10.3762/bjoc.21.74.

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A silver(I) triflate-catalyzed post-Ugi assembly of novel pyrazolo[1,5-a][1,4]diazepine scaffolds is reported offering high yields (up to 98%) under mild conditions. The synthetic sequence involves the Ugi four-component reaction (U4CR) of pyrazole-3-carbaldehydes, primary amines, 3-substituted propiolic acids, and isocyanides, followed by a silver(I) triflate-catalyzed intramolecular heteroannulation of the resulting pyrazole-tethered propargylamides occurring in a 7-endo-dig fashion. The approach is scalable and tolerates a diverse range of substitution patterns.
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46

Bou-Petit, Elisabeth, Arnau Plans, Nieves Rodríguez-Picazo, et al. "C4–C5 fused pyrazol-3-amines: when the degree of unsaturation and electronic characteristics of the fused ring controls regioselectivity in Ullmann and acylation reactions." Organic & Biomolecular Chemistry 18, no. 27 (2020): 5145–56. http://dx.doi.org/10.1039/d0ob00796j.

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The regioselectivity of Ullmann and acylation reactions of C4–C5 fused pyrazol-3-amines is predicted using DFT calculations of the most stable tautomer (1H- or 2H-pyrazole) and occur, mainly, at the NH and non-protonated nitrogen atom, respectively.
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47

Wang, Zhaodong. "Synthesis and Structure of the Copper Complex[Cu2L2ox(SO4)(H2O)4](H2O)4." E3S Web of Conferences 290 (2021): 01010. http://dx.doi.org/10.1051/e3sconf/202129001010.

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The reaction of N-(pyridine-2-ylmethyl)pyrazine-2-carboxamide (HL) and copper(II) sulfate leads to the formation of a new copper complex, [Cu2L2ox(SO4)(H2O)4](H2O)4(1), in which the deprotonated amide L-ligand was oxidized to a imide Lox-exposed to the air in the presence of the Cu ion. The X-ray crystal analysis reveals that it consists of two mononuclear copper unit with different coordination modes, multiple O-H…O hydrogen bonding between water molecules or water and sulfate O atom to form 3D networks. CCDC: 2088935,1.
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48

A., H. SIDDIQUI, SATYANARAYANA Y., and SRINIVAS and K. RAJESHWAR M. "Synthesis of Azasteroids with Pyrazoline and lsoxazoline Rings." Journal of Indian Chemical Society Vol. 69, Dec 1992 (1992): 846–48. https://doi.org/10.5281/zenodo.6032514.

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Department of Chemistry, Nizam College, Hyderabad-500 001 <em>Manuscript received 17 June 1992, accepted 21 September 1992</em> 17-Oxo-5-androsten-3<em>&beta;-</em>YI acetate (1) on reaction with dimethyl oxalate afforded the glyoxalate, 16-carbomethoxycarbonyl&shy;17-oxo-5-androsten-3<em>&beta;</em>-YI&nbsp;acetate (2) which on reaction with hydrazine hydrate, phenylhydrazine and hydroxyl amine hydro&shy;chloride gave the corresponding 3<em>&beta;</em>-acetoxy-5&#39;-carbomethoxyandrost-5-en [17,16-c] pyrazole (3), 3<em>&beta;</em>-acetoxy-5&#39;-carbometh&shy;oxy-1&#39;-phenylandrost-5-en [1
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49

Yang, Zaibo, Pei Li, and Xiuhai Gan. "Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity." Molecules 23, no. 7 (2018): 1798. http://dx.doi.org/10.3390/molecules23071798.

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In this study, a series of novel pyrazole-hydrazone derivatives containing an isoxazole moiety were synthesized. Antiviral bioassays indicated that some of the title compounds exhibited better in vivo antiviral activities against tobacco mosaic virus (TMV). In particular, compounds 6a, 6c and 6q exhibited the best curative activity, protection activity, and inactivation activity against TMV, respectively, which were superior to those of Ningnanmycin. This study demonstrated that this series of novel pyrazole-hydrazone derivatives containing an isoxazole amide moiety could effectively control T
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50

Hawkins, Lelia Nahid, Hannah G. Welsh, and Matthew V. Alexander. "Evidence for pyrazine-based chromophores in cloud water mimics containing methylglyoxal and ammonium sulfate." Atmospheric Chemistry and Physics 18, no. 16 (2018): 12413–31. http://dx.doi.org/10.5194/acp-18-12413-2018.

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Abstract. Simulating aqueous brown carbon (aqBrC) formation from small molecule amines and aldehydes in cloud water mimics provides insight into potential humic-like substance (HULIS) contributors and their effect on local and global aerosol radiative forcing. Previous work has shown that these (Maillard type) reactions generate products that are chemically, physically, and optically similar to atmospheric HULIS in many significant ways, including in their complexity. Despite numerous characterization studies, attribution of the intense brown color of many aqBrC systems to specific compounds r
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