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Journal articles on the topic '2-d]pyrimidin-4-amine'

Author: Grafiati

Published: 5 June 2025

Last updated: 15 July 2025

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1

Fesenko, Anastasia A., and Anatoly D. Shutalev. "Unprecedented synthesis of a 14-membered hexaazamacrocycle." Beilstein Journal of Organic Chemistry 19 (November 15, 2023): 1728–40. http://dx.doi.org/10.3762/bjoc.19.126.

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The transformation of 3-[(ethoxymethylene)amino]-1-methyl-1H-pyrazole-4-carbonitrile into the 14-membered macrocycle, 2,10-dimethyl-2,8,10,16-tetrahydrodipyrazolo[3,4-e:3',4'-l][1,2,4,8,9,11]hexaazacyclotetradecine-4,12-diamine, by the reaction with excess hydrazine under various conditions was studied in detail. The reaction proceeded through the initial formation of 4-imino-2-methyl-2,4-dihydro-5H-pyrazolo[3,4-d]pyrimidin-5-amine followed by dimerization to give the final macrocycle. A convenient synthesis of the latter starting from 4-imino-2-methyl-2,4-dihydro-5H-pyrazolo[3,4-d]pyrimidin-5

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2

Rossa, Thaís A., Jessica C. Neville, Seongmin Paul Jun, Tilo Söhnel, and Jonathan Sperry. "Expanding Heteroaromatic and 2-Aminosugar Chemical Space Accessible from the Biopolymer Chitin." Chemistry 5, no. 3 (2023): 1998–2008. http://dx.doi.org/10.3390/chemistry5030135.

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Herein, we report the expansion of chemical space available from chitin, accessible via the biogenic N-platforms 3A5AF, M4A2C, and di-HAF. The biologically active heteroaromatics furo[3,2-d]pyrimidin-4-one and furo[3,2-d]pyrimidin-4-amine can be selectively accessed from 3A5AF and M4A2C, respectively. The chiral pool synthon di-HAF is a viable substrate for Achmatowicz rearrangement, providing streamlined access to 2-aminosugars possessing a versatile hydroxymethyl group at C5.

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3

Kut, D., M. M. Kut, and R. T. Mariychuk. "SYNTHESIS OF N-ALKENYL(ALKYNYL)-5,6-DIMETHYL-2-(THIOPHEN-2-YL)THIENO[2,3-d]PYRIMIDIN-4-AMINES AND THEIR IN SILICO STUDY ON GROUP II CHITINASE (ChtII) INHIBITION." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 52, no. 2 (2024): 75–82. https://doi.org/10.24144/2414-0260.2024.2.75-82.

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Research in the chemistry of heterocyclic compounds, particularly condensed pyrimidine frameworks, aimed at developing drugs with diverse therapeutic properties. Among these compounds, special attention is given to thieno[2,3-d]pyrimidine derivatives due to their potential as drug candidates. This study presents the synthesis of a series of N-alkenyl(alkynyl)-5,6-dimethyl-2-(thiophen-2-yl)-thieno[2,3-d]pyrimidin-4-amines via the amination reaction of 5,6-dimethyl-2-(thiophen-2-yl)-4-chlorothieno[2,3-d]pyrimidine with unsaturated amines (allyl-, diallyl-, and propargylamine), enabling potential

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4

Tukhsanov, Feruz, Ergash Oripov, Gayrat Haydarov, Makhmasaid Khudayarov, and Turakul Eshboboyev. "Kabachnik-Fields reactions of 2,3-Trimethylene-1,2,3,4-dihydrobenzo[2,3-d]pyrimidin-4-on." E3S Web of Conferences 389 (2023): 03031. http://dx.doi.org/10.1051/e3sconf/202338903031.

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In this research article, 2,3-trimethylene-3,4-dihydrobenzo[2,3-d]pyrimidin-4-one was synthesized from 2-aminobenzoic acid and pyrrolidone-2 in the presence of various substances, such as PCl5, POCl3. Its reduction reaction with NaBH4 was carried out. The resulting three-component coupling of 2,3-trimethylene-1,2,3,4-tetrahydrobenzo[2,3-d]pyrimidin-4-one-carbonyl, amine, and hydrophosphoryl leads to αaminophosphonates. Phosphate acid – formaldehyde; aldehydes in the three-component system; and the synthesis of aminomethylphosphonic acid is based on the condensation reaction. During the experim

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5

Yin, Xuelian, and Yang-Heon Song. "5-Methyl-1-phenyl-3-(thieno[2,3-d]pyrimidin-4-yl)chromeno[4,3-d]pyrazolo[3,4-b]pyridin-6(3H)-one." Molbank 2022, no. 4 (2022): M1469. http://dx.doi.org/10.3390/m1469.

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A chromeno[4,3-d]pyrazolo[3,4-b]pyridinone derivative 3 bearing thieno[2,3-d]pyrimidine moiety, 5-methyl-1-phenyl-3-(thieno[2,3-d]pyrimidin-4-yl)chromeno[4,3-d]pyrazolo[3,4-b]pyridin-6(3H)-one, was efficiently prepared in 75% yield by the reaction of 3-phenyl-1-(thieno[2,3-d]pyrimidin-4-yl)-1H-pyrazol-5-amine 1 with 3-acetyl-2H-chromen-2-one 2 in the presence of FeCl3-SiO2 as a catalyst in refluxing ethanol for 6 h. The structure of the new synthesized compound was characterized by 1H-, 13C- NMR, IR spectroscopy, mass-spectrometry, and elemental analysis.

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6

Harnden, MR, and DT Hurst. "The Synthesis and Chlorination of Some Pyrimidin-4-ols Having 5-Nitrogen Functionality." Australian Journal of Chemistry 43, no. 1 (1990): 47. http://dx.doi.org/10.1071/ch9900047.

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Syntheses of a number of pyrimidin-4-ols having 5-nitrogen functionality are described. Phosphorus oxychloride/diethylaniline chlorination of 6-amino-2-methylthio-5-nitropyrimidin-4-ol gave the corresponding 6-chloro derivative. However, 2-amino-6-methylthio-5-nitropyrimidin-4-ol failed to yield a 4-chloro derivative under the same conditions. Similar chlorination of 2,5-diaminopyrimidine-4,6-diol gave a poor yield of the 4,6-dichloro product but under these conditions 2-amino-5-benzoylaminopyrimidine-4,6-diol* gave 7-chloro-2-phenyloxazolo[5,4-d]pyrimidin-5-amine. 5-Acetylamino-2-methylthiopy

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7

Loidreau, Yvonnick, Marie-Renée Nourrisson, Corinne Fruit, Cécile Corbière, Pascal Marchand, and Thierry Besson. "Microwave-Assisted Synthesis of Potential Bioactive Benzo-, Pyrido- or Pyrazino-thieno[3,2-d]pyrimidin-4-amine Analogs of MPC-6827." Pharmaceuticals 13, no. 9 (2020): 202. http://dx.doi.org/10.3390/ph13090202.

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Efficient microwave-assisted chemical processes were applied to the synthesis of an array of novel N-(4-methoxyphenylamino)-2-methyl benzo-, pyrido- or pyrazino-thieno[3,2-d]pyrimidin-4-amine derivatives. These heteroaromatic systems were envisioned as potent bioisosteric analogues of MPC-6827, an anticancer agent previously developed until phase II clinical studies. A brief evaluation and comparison of their antiproliferative activity on HT-29 and Caco-2, two human colorectal cancer cell lines, were also reported. At the tested concentrations (5 and 10 µM), thieno[3,2-d]pyrimidin-4-amines 4a

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8

Harnden, MR, and DT Hurst. "The Chemistry of Pyrimidinethiols. III. The Synthesis of Some Substituted Pyrimidinthiols and Some Thiazolo[5,4-D]pyrimidines." Australian Journal of Chemistry 43, no. 1 (1990): 55. http://dx.doi.org/10.1071/ch9900055.

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The preparation of a number of pyrimidinethiols and (substituted) thiopyrimidines has been carried out. The reaction of 5-acetylamino-2-aminopyrimidine-4,6-diol with phosphorus penta -sulfide in pyridine gave 5-amino-2-methylthiazolo[5,4-d]pyrimidine-7-thiol which was used to prepare several additional novel pyrimidine derivatives. Hydrolysis of the 4-carboxymethylthio derivative by using 5M hydrochloric acid gave 2,5-diamino-6-mercaptopyrimidin-4-ol hy -drochloride whilst hydrolysis of 2-methyl-7-methylthiothiazolo[5,4-d]pyrimidin-5-amine gave the corresponding 4-hydroxy derivative. Several 4

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9

Guillon, Jean, Mathieu Marchivie, Yvonnick Loidreau, Noël Pinaud, and Thierry Besson. "Structure of N-(3,4-Dimethoxyphenyl)pyrido[3′,2′:4,5]-thieno[3,2-d]pyrimidin-4-amine, a New Inhibitor of CLK1 and DYRK1A Kinases." Journal of Crystallography 2013 (December 23, 2013): 1–4. http://dx.doi.org/10.1155/2013/842803.

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The complete crystal structure of N-(3,4-dimethoxyphenyl)pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-amine, synthesized via a Dimroth rearrangement and designed as new inhibitor of CLK1 and DYRK1A kinases, was established by a single-crystal X-ray diffraction. The crystal is orthorhombic, space group Pca21; a = 13.1593 (9), b = 13.9823 (10), c=8.5403 (7) Å, α=β=γ=90°, V = 1571.4 (2) Å3, and Z=4, C17H14N4O2S. Solid-state data could be used to enlighten the biological mechanism of action.

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10

Kalita, Subarna, Bidyut Das, and Dibakar Deka. "l-Proline-Catalysed One-Pot Regio- and Diastereoselective Synthesis of Spiro[pyrido[2,3-d]pyrimidin-2-amine-6,5′-pyrimidines] in Water." SynOpen 01, no. 01 (2017): 0045–49. http://dx.doi.org/10.1055/s-0036-1588456.

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A simple l-proline-catalysed regio- and diastereoselective synthesis of spiro[pyrido[2,3-d]pyrimidin-2-amine-6,5′-pyrimidines] in water through a strategy of one-pot multicomponent domino reaction of 2,6-diaminopyrimidin-4-one, aldehydes and barbituric acids is described. The notable advantages of the protocol are operational simplicity, mild reaction conditions, simple purification process involving no chromatographic techniques, wide substrate scope, and high yields. The method delivers the desired product within short reaction time and with a diastereoselectivity of 61:39 to 100:0, which ma

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11

Richter, Daniel, John C. Kath, Arnold L. Rheingold, Antonio DiPasquale, and Alex Yanovsky. "5-Chloro-N-[2-(1H-imidazol-4-yl)ethyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine." Acta Crystallographica Section E Structure Reports Online 66, no. 1 (2009): o242. http://dx.doi.org/10.1107/s1600536809054750.

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12

Veltri, Lucia, Bartolo Gabriele, Raffaella Mancuso, et al. "Palladium-Catalyzed Carbonylative Synthesis of Functionalized Benzimidazopyrimidinones." Synthesis 50, no. 02 (2017): 267–77. http://dx.doi.org/10.1055/s-0036-1591835.

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A new and convenient approach to functionalized benzimidazopyrimidinones is reported. It is based on a two-step procedure starting from readily available 1-(prop-2-yn-1-yl)-1H-benzo[d]imidazol-2-amines, consisting of a multicomponent palladium-catalyzed oxidative cyclocarbonylation–alkoxycarbonylation process, followed by base-promoted isomerization of the initially formed mixture of isomeric carbonylated products. Fair to good overall yields of the final alkyl 2-(2-oxo-1,2-dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-3-yl)acetates are obtained, using different alcohols as solvent and nucleophile

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13

Zong, Chaoyang, Huiwen Gu, Lijie Zhang, Yudong Jin, and Yaquan Sun. "Microwave-Accelerated Dimroth Rearrangement for the Synthesis of Pyrido [2, 3-d]pyrimidin-4-amine Derivatives." Chinese Journal of Organic Chemistry 38, no. 5 (2018): 1165. http://dx.doi.org/10.6023/cjoc201711028.

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14

Zong, Chaoyang, Lijie Zhang, Mengting Gu, and Yaquan Sun. "Facile Microwave-Assisted Synthesis of 6, 7-Dihydro-5H-cyclopenta [4, 5]thieno [2, 3-d]pyrimidin-4-amine." Chinese Journal of Organic Chemistry 38, no. 6 (2018): 1422. http://dx.doi.org/10.6023/cjoc201801009.

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15

Abdel Aziz, Yasmine M., Mohamed M. Said, Hosam A. El Shihawy, and Khaled A. M. Abouzid. "Discovery of novel tricyclic pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-amine derivatives as VEGFR-2 inhibitors." Bioorganic Chemistry 60 (June 2015): 1–12. http://dx.doi.org/10.1016/j.bioorg.2015.03.004.

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16

Gong, Tang, Liu та Liu. "Synthesis and Evaluation of Novel 2H-Benzo[e]-[1,2,4]thiadiazine 1,1-Dioxide Derivatives as PI3Kδ Inhibitors". Molecules 24, № 23 (2019): 4299. http://dx.doi.org/10.3390/molecules24234299.

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In previous work, we applied the rotation-limiting strategy and introduced a substituent at the 3-position of the pyrazolo [3,4-d]pyrimidin-4-amine as the affinity element to interact with the deeper hydrophobic pocket, discovered a series of novel quinazolinones as potent PI3Kδ inhibitors. Among them, the indole derivative 3 is one of the most selective PI3Kδ inhibitors and the 3,4-dimethoxyphenyl derivative 4 is a potent and selective dual PI3Kδ/γ inhibitor. In this study, we replaced the carbonyl group in the quinazolinone core with a sulfonyl group, designed a series of novel 2H-benzo[e][1

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17

Dinesh, Kumar Meena, Kishore Sharma Brij, and Parihar Raghuraj. "Quantitative Structure-Activity Relationship Study on the CDK4/6 Inhibitory Activity: The 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amines." British Journal of Medical and Health Research 9, no. 10 (2022): 28–48. https://doi.org/10.5281/zenodo.7270390.

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ABSTRACT Cyclin D dependent kinases namely CDK4 and CDK6 regulate entry into S phase of the cell cycle. These are emerging validated targets for anti-cancer drug discovery. A QSAR study has been carried out on the 4-thiazol-N-(pyridin-2-yl)pyrimidin-2-amine derivatives, which were reported as highly potent and selective inhibitors of CDK4 and CDK6, in terms of Dragon descriptors with the aim to establish the quantitative relationships between the reported activities and molecular descriptors unfolding the substitutional changes. In deriving QSAR models, combinatorial protocol in multiple linea

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18

Mohamed, Hany M., and Ashraf H. F. Abd El-Wahab. "Heteroaromatization with 4-Phenyldiazenyl-1-naphthol. Part IV: Synthesis of Some New Heterocyclic Compounds with Potential Biological Activity." Current Organic Synthesis 16, no. 6 (2019): 931–38. http://dx.doi.org/10.2174/1570179416666190719101727.

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Background: Synthetic azo compounds and their derivatives have been studied extensively due to their biological and pharmacological activities. Pyranopyridines, pyranopyrimidines and tetrazoles derivatives have emerged as a promising and attractive scaffold in the development of potent biological and pharmacological agents. Objectives: To design a series of new benzochromeno(pyridine/pyrimidine/tetrazole) derivatives and evaluate their antimicrobial activity against some bacterial strains (Gram-positive and Gram-negative) and some fungal strains. Materials and Methods: The (E)-7-(4-chloropheny

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19

D., R. Godhani, A. Kaila B., Sanghani A.M., and B. Dobariya P. "Synthesis of some 7 ,9-dimethyl-8-substituted pyrido[3' ,2' : 4,5]thieno[3,2-d]- pyrimidine and their antitubercular activity." Journal of Indian Chemical Society Vol. 90, Dec 2013 (2013): 2257–62. https://doi.org/10.5281/zenodo.5794113.

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Department of Chemistry, DST -FIST Sponsored, Bhavnagar University, Bhavnagar-364 002, Gujarat, India <em>E-mail</em> : drgodhani@yahoo.com <em>Manuscript received 13 December 2011, revised 05 July 2012, accepted 21 January 2013</em> A series of eight new 7,9-dimethyl-8-substituted pyrido[3<em>'</em>,2<em>' </em>: 4,5]thieno[3,2-<em>d</em>]pyrimidines (4a-h) have been synthesised starting from 3-substituted pentan-2,4-dione in three steps. These compounds have been characterized by NMR and mass spectroscopy and checked their antitubercular activity.

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20

Abdel-Maksoud, Mohammed S., Ahmed A. B. Mohamed, Rasha M. Hassan, et al. "Design, Synthesis and Anticancer Profile of New 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-Linked Sulfonamide Derivatives with V600EBRAF Inhibitory Effect." International Journal of Molecular Sciences 22, no. 19 (2021): 10491. http://dx.doi.org/10.3390/ijms221910491.

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A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 µM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 µM. They were further screened on NCI 60 cancer cell lines to reveal that 1

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21

Jean Missa Ehouman, Georges Stéphane Dembélé, Mamadou Guy-Richard Koné, Donourou Diabaté, Yafigui Traoré, and Nahossé Ziao. "Reactivity of three pyrimidine derivatives, potential analgesics, by the DFT method and study of their docking on cyclooxygenases-1 and 2." World Journal of Advanced Research and Reviews 24, no. 2 (2024): 2676–91. https://doi.org/10.30574/wjarr.2024.24.2.3497.

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Three pyrimidine derivatives, namely 4-[4-(dimethylamino)phenyl]-6-(pyridin-4-yl)pyrimidin-2-amine (DMPN), 4-(4-aminophenyl)-6-[4-(dimethylamino)phenyl]pyrimidin-2-ol (DMPO) and 4-(4-aminophenyl)-6-[4-(dimethylamino)phenyl]pyrimidine-2-thiol (DMPS), with analgesic properties established by a QSAR study, were subjected to reactivity parameter studies using the DFT method, at the B3LYP/6-311++G(d,p) level of theory. Studies of the docking of these molecules to cyclooxygenases 1 (PDB ID: 5U6X) and 2 (PDB ID: 5F19) were also carried out using the CB-Dock online program. Reactivity parameter calcul

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22

Jean, Missa Ehouman, Stéphane Dembélé Georges, Guy-Richard Koné Mamadou, Diabaté Donourou, Traoré Yafigui, and Ziao Nahossé. "Reactivity of three pyrimidine derivatives, potential analgesics, by the DFT method and study of their docking on cyclooxygenases-1 and 2." World Journal of Advanced Research and Reviews 24, no. 2 (2024): 2676–91. https://doi.org/10.5281/zenodo.15142640.

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Three pyrimidine derivatives, namely 4-[4-(dimethylamino)phenyl]-6-(pyridin-4-yl)pyrimidin-2-amine (DMPN), 4-(4-aminophenyl)-6-[4-(dimethylamino)phenyl]pyrimidin-2-ol (DMPO) and 4-(4-aminophenyl)-6-[4-(dimethylamino)phenyl]pyrimidine-2-thiol (DMPS), with analgesic properties established by a QSAR study, were subjected to reactivity parameter studies using the DFT method, at the B3LYP/6-311++G(d,p) level of theory. Studies of the docking of these molecules to cyclooxygenases 1 (PDB ID: 5U6X) and 2 (PDB ID: 5F19) were also carried out using the CB-Dock online program. Reactivity parameter calcul

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23

Mardente, Stefania, Michele Aventaggiato, Emanuela Mari, et al. "GO Nanosheets: Promising Nano Carrier for the S29, 1-(2-Chloro-2-(4-chlorophenyl-ethyl)-N-(4-fluorobenzyl)-1H-pyrazolo[3,4-d] pyrimidin-4-amine, Therapeutic Agent in Neuroblastoma." International Journal of Molecular Sciences 21, no. 17 (2020): 6430. http://dx.doi.org/10.3390/ijms21176430.

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Graphene oxide (GO) derivatives are reported as a valid alternative to conventional carriers of therapeutic agents, because they have a large surface area, an excellent electrical and thermal conductivity and a great capacity for selective binding of drugs and therapeutics, due to the functionalization of their surfaces, edges and sides. In this work GO nanosheets, synthesized by electrochemical exfoliation of graphite (patent N 102015000023739, Tor Vergata University), were investigated as possible carriers of an anticancer drug, the S29, an inhibitor of a cytoplasmic tyrosine kinase (c-SRC)

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Valentini, Federica, Andrea Calcaterra, Vincenzo Ruggiero, et al. "Functionalized Graphene Derivatives: Antibacterial Properties and Cytotoxicity." Journal of Nanomaterials 2019 (February 14, 2019): 1–14. http://dx.doi.org/10.1155/2019/2752539.

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In this work, the authors prepared and characterized two different graphene oxides: one chemically synthesized (GO sample) and the other one electrochemically synthesized (GO(LiCl)). Both samples were fully characterized with atomic force microscopy (AFM), Raman and Fourier transform infrared (FTIR) spectroscopies, X-ray photo electron spectroscopy (XPS), thermal analysis (TG/DTA), and Z-potential. The antibacterial properties of both graphene oxides were studied using Gram-negative Escherichia coli ATCC 25922 and Gram-positive Staphylococcus aureus ATCC 25923 by spectrophotometer and viable c

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25

Abeer, Fauzi Al-Rubaye, Jawad Kadhim Mohanad, and Hadi Hameed Imad. "Characterization of Antifungal Secondary Metabolites Produced by Klebsiella pneumoniae and Screening of its Chemical Compounds Using GC-MS." International Journal of Current Pharmaceutical Review and Research 8, no. 2 (2017): 141–48. https://doi.org/10.5281/zenodo.12677888.

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Bioactives were analyzed using gas chromatography-mass spectroscopy (GC-MS) techniques, then the in vitroantibacterial and antifungal activity of the methanolic extract was evaluated. Twenty two bioactive compounds wereidentified in the methanolic extract of Klebsiella pneumoniae. GC-MS analysis of Klebsiella pneumoniae revealed theexistence of the 6,9,12-Octadecatrienoic acid , phenylmethyl ester , (Z,Z,Z)-, 5,7-Dodecadiyn-1,12-diol, 1,4 Decadiyne,10,12-Octadecadiynoic acid, 1-Cyclopropyl-3,4-epoxyhex-5-en-1-yne, N,N-Dimethyl-3-methoxy-4-methylphenethylamine, Ethenetricarbonitrile , 3,4-xylid

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Maher, Michael P., Anindya Bhattacharya, Hong Ao, et al. "Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist." European Journal of Pharmacology 663, no. 1-3 (2011): 40–50. http://dx.doi.org/10.1016/j.ejphar.2011.05.001.

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27

Trilleras, Jorge, Jairo Quiroga, Justo Cobo, et al. "Anhydrous versus hydrated N 4-substituted 1H-pyrazolo[3,4-d]pyrimidine-4,6-diamines: hydrogen bonding in two and three dimensions." Acta Crystallographica Section B Structural Science 64, no. 5 (2008): 610–22. http://dx.doi.org/10.1107/s0108768108019903.

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Ten new N 4-substituted 1H-pyrazolo[3,4-d]pyrimidine-4,6-diamines have been synthesized and the structures of nine of them are reported here, falling into two clear groups, those which are stoichiometric hydrates and those which crystallize in solvent-free forms. In each of N 4-methyl-N 4-phenyl-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine, C12H12N6 (I), N 4-cyclohexyl-N 4-methyl-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine, C12H18N6 (II), and N 4-(3-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine, C11H9ClN6 (III), the molecules are linked into hydrogen-bonded sheets. The molecules of 2-{4-(6-a

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28

Ireland, David R., Diane Guevremont, Joanna M. Williams, and Wickliffe C. Abraham. "Metabotropic Glutamate Receptor-Mediated Depression of the Slow Afterhyperpolarization Is Gated by Tyrosine Phosphatases in Hippocampal CA1 Pyramidal Neurons." Journal of Neurophysiology 92, no. 5 (2004): 2811–19. http://dx.doi.org/10.1152/jn.01236.2003.

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Group I metabotropic glutamate receptor (mGluR) agonists increase the excitability of hippocampal CAl pyramidal neurons via depression of the postspike afterhyperpolarization. In adult rats, this is mediated by both mGluR1 and -5, but the signal transduction processes involved are unknown. In this study, we investigated whether altered levels of tyrosine phosphorylation of proteins are involved in the depression of the slow-duration afterhyperpolarization (sAHP) by the Group I mGluR agonist (RS)-3,5-dihydroxyphenylglycine (DHPG) in CA1 pyramidal neurons of rat hippocampal slices. Preincubation

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Aziz, Yasmine Mohamed Abdel, Mohamed Mokhtar Said, Hosam Ahmed El Shihawy, Mai Fathy Tolba, and Khaled Abouzid Mohamed Abouzid. "Discovery of Potent Antiproliferative Agents Targeting EGFR Tyrosine Kinase Based on the Pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-amine Scaffold." Chemical and Pharmaceutical Bulletin 63, no. 12 (2015): 1015–28. http://dx.doi.org/10.1248/cpb.c15-00592.

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30

Solomyannyi, Roman, Sergii Slivchuk, Donald Smee, et al. "In vitro Activity of the Novel Pyrimidines and Their Condensed Derivatives Against Poliovirus." Current Bioactive Compounds 15, no. 5 (2019): 582–91. http://dx.doi.org/10.2174/1573407214666180720120509.

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Background: Substituted pyrimidine derivatives (non-nucleoside) are found to be associated with various biological activities. The various substituted pyrimidines are also having significant in vitro activity against different DNA and RNA viruses. The present study focuses on the anti-PV activity of new pyrimidines and their condensed derivatives. Methods: A series of novel pyrimidines and their condensed derivatives were synthesized and their structures were confirmed by spectral data. Their antiviral activities against poliovirus type 3 (PV-3) were evaluated in vitro. In cell culture, morpho

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Zhang, Jinfeng, Ziwei Luo, Wenwen Duan, et al. "Dual-acting antitumor agents targeting the A2A adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives." European Journal of Medicinal Chemistry 236 (June 2022): 114326. http://dx.doi.org/10.1016/j.ejmech.2022.114326.

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Shi, Chen, Qian Wang, Xuemei Liao, et al. "Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer." European Journal of Medicinal Chemistry 178 (September 2019): 352–64. http://dx.doi.org/10.1016/j.ejmech.2019.06.005.

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He, Linhong, Da Li, Chufeng Zhang, Peng Bai, and Lijuan Chen. "Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC." Bioorganic & Medicinal Chemistry Letters 27, no. 17 (2017): 4171–75. http://dx.doi.org/10.1016/j.bmcl.2017.07.009.

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Muhammad, Mazhar Fareed, Qasmi Maryam, Zaheer Hira, and Hira. "The in-silico approaches; structural, functional proteins-association elucidation of Moringa oleifera phytochemicals against the tyrosine kinase receptor protein of Diabetes mellitus." European journal of volunteering and community-based projects 1, no. 3 (2021): 1–29. https://doi.org/10.5281/zenodo.5516297.

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The <em>Moringa oleifera</em> also called “Drumstick tree”, to its various pharmacological uses and nutritional adaptability worth is comprehensively all over the earth. The tree parts; stem, bark, gum, roots, and mostly leaves are great provenance of vitamins, minerals, and numerous clinically beneficial secondary-metabolites and also a significant role in diabetic-resistance. The virtual-study may exist significant in terms of expanding the number of successful antidotes derived through this herb and plan to obtain the potent-phytochemicals amalgam of miracle tree even an agent f

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Wang, Yan, Wen-Jian Liu, Lei Yin, et al. "Design and synthesis of 4-(2,3-dihydro-1 H -benzo[ d ]pyrrolo[1,2- a ]imidazol-7-yl)- N -(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships." Bioorganic & Medicinal Chemistry Letters 28, no. 5 (2018): 974–78. http://dx.doi.org/10.1016/j.bmcl.2017.12.068.

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36

Jin, Jian-Chang, Zhao-Hui Sun, Ming-Yan Yang, Jing Wu, and Xing-Hai Liu. "Synthesis, Crystal Structure, and Theoretical Studies of N-(4-((4-chlorobenzyl)oxy)phenyl)-4- (trifluoromethyl)pyrimidin-2-amine." Journal of Chemistry 2013 (2013): 1–5. http://dx.doi.org/10.1155/2013/521757.

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The title compound (C18H13ClF3N3O) were synthesized and recrystallized from CH3OH. The compound was characterized byH1NMR, MS, HRMS, and X-ray diffraction. The compound crystallized in the monoclinic space groupP2(1)/nwitha=8.2354(14),b=12.686(2),c=16.633(3) Å,α=90,β=97.951(3),γ=90∘,V=1721.0(5) Å3,Z=4,andR=0.0376for 1933 observed reflections withI>2σ(I).X-ray analysis reveals that intermolecular N–H⋯N interactions exist in the adjacent molecules. Theoretical calculation of the title compound was carried out with HF/6-31G(d,p), B3LYP/6-31G(d,p). The full geometry optimization was carried out

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Hsin, Ling-Wei, Elizabeth L. Webster, George P. Chrousos, et al. "Synthesis of [3H](4-fluorobutyl)propyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amine: a potent radioligand for corticotropin-releasing hormone type 1 receptor." Journal of Labelled Compounds and Radiopharmaceuticals 43, no. 9 (2000): 899–908. http://dx.doi.org/10.1002/1099-1344(200008)43:9<899::aid-jlcr375>3.0.co;2-n.

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D., E. Turgunov. "SYNTHESIS OF PHOSPHONIC ACIDS OF POLYFUNCTIONAL PYRIDOPYRIMIDINES." June 11, 2023. https://doi.org/10.5281/zenodo.8025261.

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<em>In the article synthesized 2,3-trimethylene-3,4-dihydropyrido[2,3-d] pyrimidin-4-one from 2-Aminonicotinic acid and pyrrolidone-2 in the presence different agents, such as PCl<sub>5</sub>, POCl<sub>3</sub>. Its reduction reaction with NaBH<sub>4</sub> carrying out. Obtained 2,3-trimethylene-1,2,3,4-tetrahydropyrido[2,3-d] pyrimidin-4-one – this three-component coupling of a carbonyl, an amine and a hydrophosphoryl compoud leads to </em><em>α</em><em>-aminophosphonates, phosphorous acid-formaldehyde; aldehydes in three component system; minomethylphosphonic acid synthesis based

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Vicentes, Daniel E., Ricaurte Rodríguez, Justo Cobo, and Christopher Glidewell. "Synthesis of 5-(arylmethylideneamino)-4-(1H-benzo[d]imidazol-1-yl)pyrimidine hybrids: synthetic sequence and the molecular and supramolecular structures of two intermediates and three final products." Acta Crystallographica Section C Structural Chemistry 79, no. 6 (2023). http://dx.doi.org/10.1107/s2053229623003728.

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A concise and versatile synthesis of 5-(arylmethylideneamino)-4-(1H-benzo[d]imidazol-1-yl)pyrimidines has been developed, starting from 4-(1H-benzo[d]imidazol-1-yl)pyrimidines, and we report here the synthesis and spectroscopic and structural characterization of three such products, along with those of two intermediates in the reaction pathway. The intermediates 4-[2-(4-chlorophenyl)-1H-benzo[d]imidazol-1-yl]-6-methoxypyrimidine-2,5-diamine, (II), and 4-[2-(4-bromophenyl)-1H-benzo[d]imidazol-1-yl]-6-methoxypyrimidine-2,5-diamine, (III), crystallize as the isostructural monohydrates C18H15ClN5O

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Alizadeh‐Bami, Farzaneh, Hossein Mehrabi, and Maryam Hosseini‐pour. "2‐Amino‐4‐arylthiophene‐3‐carbonitrile and formamidine acetate as key building units for the synthesis of 5‐arylthieno[2,3‐d]pyrimidin‐4‐amines." Journal of Heterocyclic Chemistry, August 24, 2023. http://dx.doi.org/10.1002/jhet.4727.

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AbstractWe tried to establish a method for the synthesis of 5‐arylthieno[2,3‐d]pyrimidin‐4‐amine analogues via three‐step reactions and examined the changes in the solvent, time, and temperature. A novel condition has been developed for the preparation of substituted 2‐aminothiophenes employing the Knoevenagel condensation followed by the Gewald method and in the last step to form thieno[2,3‐d]pyrimidines by using formamidine acetate. All the synthesized 5‐arylthieno[2,3‐d]pyrimidin‐4‐amines are unknown and were characterized by IR, 1H‐NMR, 13C‐NMR, and CHN analysis.

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Bandaru, Praveen Kumar, Satya Kameswara Rao N, and Shyamala P. "Amide Functionalized Novel Pyrrolo-pyrimidine Derivative as Anticancer Agents: Synthesis, Characterization and Molecular Docking Studies." Anti-Cancer Agents in Medicinal Chemistry 25 (November 6, 2024). http://dx.doi.org/10.2174/0118715206333935241004070350.

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Background: The development of new therapies targeting crucial kinases involved in cancer progression is a promising area of research. Pyrazolo pyrimidine derivatives have emerged as potential candidates for this purpose. Objective: This study aims to synthesize pyrazolo pyrimidine derivatives (5a-5r), evaluate their molecular docking against key kinases, and assess their anticancer activity. Methods: The synthesis involved a multi-step procedure starting with the cyclization of 6-amino-2- methylpyrimidin-4(3H)-one (1) to form 2-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-4-ol (2). This was

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"Design, synthesis and docking studies of N-(2-Fluoro-5-(trifluoromethoxy) benzyl)-2-methylpyrido [2, 3-d] pyrimidin-4-amine." International Journal of Green and Herbal Chemistry 8, no. 1 (2019). http://dx.doi.org/10.24214/ijghc/gc/8/1/06171.

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Cele, Nosipho, Paul Awolade, Pule Seboletswe, et al. "Synthesis,Antidiabetic and Antitubercular Evaluation of Quinoline–pyrazolopyrimidine hybrids and Quinoline‐4‐Arylamines." ChemistryOpen, March 20, 2024. http://dx.doi.org/10.1002/open.202400014.

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AbstractTwo libraries of quinoline‐based hybrids 1‐(7‐chloroquinolin‐4‐yl)‐1H‐pyrazolo[3,4–d]pyrimidin‐4‐amine and 7‐chloro‐N‐phenylquinolin‐4‐amine were synthesized and evaluated for their α‐glucosidase inhibitory and antioxidant properties. Compounds with 4‐methylpiperidine and para‐trifluoromethoxy groups, respectively, showed the most promising α‐glucosidase inhibition activity with IC50=46.70 and 40.84 μM, compared to the reference inhibitor, acarbose (IC50=51.73 μM). Structure‐activity relationship analysis suggested that the cyclic secondary amine pendants and para‐phenyl substituents a

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44

Bakheit, Ahmed H., Tanveer A. Wani, Abdulrahman A. Al-Majed, et al. "Theoretical study of the antioxidant mechanism and structure-activity relationships of 1,3,4-oxadiazol-2-ylthieno[2,3-d]pyrimidin-4-amine derivatives: a computational approach." Frontiers in Chemistry 12 (July 30, 2024). http://dx.doi.org/10.3389/fchem.2024.1443718.

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A theoretical thermodynamic study was conducted to investigate the antioxidant activity and mechanism of 1,3,4-oxadiazol-2-ylthieno[2,3-d]pyrimidin-4-amine derivatives (OTP) using a Density Functional Theory (DFT) approach. The study assessed how solvent environments influence the antioxidant properties of these derivatives. With the increasing prevalence of diseases linked to oxidative stress, such as cancer and cardiovascular diseases, antioxidants are crucial in mitigating the damage caused by free radicals. Previous research has demonstrated the remarkable scavenging abilities of 1,3,4-oxa

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Shablykin, Oleh V., Volodymyr S. Brovarets, and Olga V. Shablykina. "Recyclization of 5‐Amino‐ oxazoles as a Route to new Functionalized Heterocycles (Developments of V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the NAS of Ukraine)." Chemical Record, October 26, 2023. http://dx.doi.org/10.1002/tcr.202300264.

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AbstractThe recyclizations of 5‐amino‐ and 5‐hydrazine‐1,3‐oxazoles mainly with electron‐withdrawing group in 4th position are considered. The chemical behavior of these heterocycles is due to the presence of two hidden amide fragments; therefore, the recyclization processes include a stage of nucleophile attack on 2nd or 5th position of the oxazole cycle. When the nitrile group is present in 4th position, it is often involved in the recyclization forming α‐aminoazoles. 5‐Amino/hydrazine‐1,3‐oxazoles undergo recyclization both in nucleophilic (amines, hydrazine, thionating agents) and electrop

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Valentini, Federica, Simonetta Antonaroli, Giulia Iovenitti, Maurizio Botta, and Maurizio Talamo. "Graphene electrochemical sensors for the detection of S 29:1-(2-chloro-2-(4-chlorophenyl)ethyl)-N-(4-fluorobenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine: an anticancer drug." Frontiers in Nanoscience and Nanotechnology 4, no. 3 (2018). http://dx.doi.org/10.15761/fnn.1000s1003.

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Spellman, Michael, Safa Samimi, Ryan Kurtz, and Blythe Shepard. "Signaling of GPR17 in Hepatic and Renal Tissues." Physiology 39, S1 (2024). http://dx.doi.org/10.1152/physiol.2024.39.s1.1524.

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G protein-coupled receptors (GPCRs) are the largest class of proteins in the human body and are considered to be excellent targets for drug discovery. However, the vast majority of GPCRs are understudied. Using a large-scale TaqMan array screen on both male and female C57BL6 murine livers, we identified GPR17 as one of the most highly expressed orphan receptors within the liver (ΔCt = 19.9, normalized to GAPDH). GPR17 expression in the liver was confirmed using reverse transcriptase polymerase chain reaction (RT-PCR) and was also identified in murine whole kidney from both males and females in

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"Orphan designation: N-[(1R)-1-phenylethyl]-6-{1H-pyrazolo[3,4-d]pyrimidin-4-yl}quinazolin-2-amine, Treatment of fragile X syndrome." Case Medical Research, April 8, 2019. http://dx.doi.org/10.31525/cmr-fa2942.

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"Orphan designation: N-[(1R)-1-phenylethyl]-6-{1H-pyrazolo[3,4-d]pyrimidin-4-yl}quinazolin-2-amine, Treatment of fragile X syndrome." Case Medical Research, April 8, 2019. http://dx.doi.org/10.31525/cmr-fa7181.

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Al-Rubaye, Abeer Fauzi, Mohanad Jawad Kadhim, and Imad Hadi Hameed. "Characterization of Antifungal Secondary Metabolites Produced by Klebsiella pneumoniae and Screening of its Chemical Compounds Using GC-MS." International Journal of Current Pharmaceutical Review and Research 8, no. 02 (2017). http://dx.doi.org/10.25258/ijcprr.v8i02.9198.

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Bioactives were analyzed using gas chromatography-mass spectroscopy (GC-MS) techniques, then the in vitro antibacterial and antifungal activity of the methanolic extract was evaluated. Twenty two bioactive compounds were identified in the methanolic extract of Klebsiella pneumoniae. GC-MS analysis of Klebsiella pneumoniae revealed the existence of the 6,9,12-Octadecatrienoic acid , phenylmethyl ester , (Z,Z,Z)-, 5,7-Dodecadiyn-1,12-diol, 1,4 Decadiyne, 10,12-Octadecadiynoic acid, 1-Cyclopropyl-3,4-epoxyhex-5-en-1-yne, N,N-Dimethyl-3-methoxy-4-methylphenethylamine, Ethenetricarbonitrile , 3,4-x

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