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Journal articles on the topic '5-a]pyrimidine derivatives'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Dabaeva, V. V., M. R. Baghdasaryan, I. M. Barkhudaryants, E. G. Paronikyan, and Sh Sh Dashyan. "Synthesis of new fused 3(4)-substituted 11-furylthieno[3,2-<i>d</i>]pyrimidine derivatives." Журнал общей химии 93, no. 9 (2023): 1351–57. http://dx.doi.org/10.31857/s0044460x23090056.

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A method was developed for the synthesis of new fused 3-alkyl-substituted derivatives of thieno[3,2- d ]pyrimidin-4(3 H )-ones based on 11-(2-furyl)-8,8-dimethyl-7,10-dihydro-8 H -pyrano[3′′,4′′:5′,6′]pyrido[3′,2′:4,5]-thieno[3,2- d ]pyrimidin-4(3 H )-one via nucleophilic substitution in the pyrimidine ring. A series of fused 4-amino-substituted 11-furylthieno[3,2- d ]pyrimidine derivatives was also synthesized from the corresponding 4-chloro derivative.

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2

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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3

Huppatz, JL. "Systemic Fungicides. The Synthesis of Pyrazolo[1,5-a]pyrimidine Analogues of Carboxin." Australian Journal of Chemistry 38, no. 1 (1985): 221. http://dx.doi.org/10.1071/ch9850221.

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The synthesis of a series of pyrazolo [1,5-a] pyrimidine derivatives, structural analogues of the systemic fungicide carboxin, is described. A common intermediate incorporating structural features desirable for fungicidal activity, N-phenyl-3(5)-amino-5(3)-methylpyrazole-4- carboxamide (6), was used to prepare pyrazolo [1,5-a] pyrimidines variously substituted in positions 5 and 7 of the ring system. Bromination of N-phenyl-2-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide (8) occurred preferentially in the phenyl ring and the 6-bromo derivative was prepared by bromination of the corresponding 3

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4

Agarkov, Artem S., Dilyara O. Mingazhetdinova, Anna A. Nefedova, et al. "Synthesis and Structure of 6-Acetyl-2-Arylhydrazone Derivatives of Thiazolo[3,2-a]Pyrimidine." Organics 4, no. 3 (2023): 438–46. http://dx.doi.org/10.3390/org4030031.

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Triazolo[4,3-a]pyrimidine is one of the promising structural fragments for the development of drugs, including anticancer drugs. This work is devoted to the synthesis of a number of new 2-arylhydrazone derivatives of thiazolo[3,2-a]pyrimidine, which are synthetic precursors for triazolo[4,3-a]pyrimidines. The crystal structure of 6-acetyl-7-methyl-5-phenyl-2-(2-phenylhydrazineylidene)-5H-thiazolo[3,2-a]pyrimidin-3(2H)-one was established by SCXRD. In the reduction reaction of the compound, the following system was used: vanadium(V) oxide, and sodium borohydride in ethanol at room temperature,

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5

Abdelhamid, Abdou O., Zeineb H. Ismail, and Anhar Abdel-Aziem. "Reactions with Hydrazonoyl Halides 601: Synthesis of Thieno[2′,3′:4,5] Pyrimidino[1,2-b][1,2,4,5]tetrazines, [1]benzothieno[2′,3′:4,5]pyrimidino [1,2-b][1,2,4,5]tetrazines, Pyrazolo[3′,4′:4,5]pyrimidino[1,2-b] [1,2,4,5]tetrazines and Pyrazolo[3,4-d]pyridazines." Journal of Chemical Research 2007, no. 10 (2007): 609–16. http://dx.doi.org/10.3184/030823407x256118.

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Thieno[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, [1]benzothieno-[2′,3′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, pyrazolo [3′,4′:4,5]pyrimidino[1,2- b][1,2,4,5]tetrazine, triazolo[4,3- a]pyrimidin-5(1 H)-one, 1-{[2-(1-benzofuran-2-yl)-5-phenyl-4,5-dihydro-1 H-pyrazol-1-yl]-4-substituted-1,3-thiazol-5-yl}-2-phenyldiazene, 3-acyl-4-(1-benzofuran-2-ylcarbonyl) pyrazole and pyrazolo[3,4- d]pyridazine derivatives could be obtained via reactions of hydrazonoyl halides with the appropriate pyrimidine-2-thione, 3-amino-5,6-dimethyl-2-sulfanylthieno[2,3- d]pyrimidin-4(3 H)-one, 5-amino-6-mercapto

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6

Ho, Yuh-Wen, and Maw Cherng Suen. "Thioxopyrimidine in Heterocyclic Synthesis I: Synthesis of Some Novel 6-(Heteroatom-substituted)-(thio)pyrimidine Derivatives." Journal of Chemistry 2013 (2013): 1–15. http://dx.doi.org/10.1155/2013/765243.

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A series of novel N-cycloalkanes, morpholine, piperazines, pyrazole, pyrimidine, benzimidazolo[1,2-a]pyrimidine, 1,2,3,4-tetrazolo[1,5-a]pyrimidine, azopyrazolo[1,5- a]pyrimidine, pyrimido[4', 5':3,4]pyrazolo[1,5-a]pyrimidines and pyridine derivatives incorporating a 5-cyano-4-methyl-2-phenyl-(thio)pyrimidine moiety were obtained by the intramolecular cyclization of 6-methylthio-pyrimidine, 6-(benzoylmethyl)thio- pyrimidine and 2-[(5-cyano-4-methyl-2-phenylpyrimidin-6-yl)thio]-3-dimethyl- amino-1-phenyl-prop-2-en-1-one with appropriate amines and enaminone compounds, respectively. The structur

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7

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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8

Hussein, Khlood Abdulla Ahmed, and Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine." University of Aden Journal of Natural and Applied Sciences 25, no. 2 (2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted

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9

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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10

A-Ani, Zaid S. M., Sana A. Abdulmawjood, Adel O. A. Al-Hussain, and Shihab A. Al-Bajari. "Synthesis and Biological Activity of few Pyrimidines Derivatives against Hepatic Injury Stimulated by Carbon Tetrachloride in Male Rats." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, no. 04 (2022): 1496–501. http://dx.doi.org/10.25258/ijddt.12.4.02.

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In the presence of sodium hydroxide, substituted chalcones are reacted with cyanoguandine in ethanol, and some chalcone compounds are used as a nucleus in the preparation of some five-, hexa-, and hepta-, heterocyclic compounds pyrimidine (pyrimidines derivatives), pyrimidine derivatives (A1, A2, and A3). Contains therapeutic properties and bioactivity, and has been used to treat various ailments. This study aimed to learn more about how pyrimidine derivatives could help mitigate the undesirable implications of carbon tetrachloride. a group of 50 male rats were separated into 5 groups: healthy

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11

Nerkar, A. G., S. A. Ghone, and A. K. Thaker. "In SilicoScreening of the Library of Pyrimidine Derivatives as Thymidylate Synthase Inhibitors for Anticancer Activity." E-Journal of Chemistry 6, no. 3 (2009): 665–72. http://dx.doi.org/10.1155/2009/352717.

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We here report the virtual screening of several series of pyrimidine derivatives forin silicoThymidylate Synthase (TS) inhibition to arrive at possible potential inhibitors of TS with acceptable pharmacokinetic or ADME (Absorption, Distribution, Metabolism and Excretion) properties. Library of the molecules was constructed based upon structural modifications of pyrimidines nucleus. Structural modifications in descending order were performed for the series of pyrimidines,vizfrom pyrimidines with five membered heterocyclic ring to pyrimidines with four membered heterocyclic ring to simple pyrimi

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12

El Ashry, E. S. H., Y. El Kilany, N. Rashed, A. Mousaad, and H. Assafir. "Synthesis and Dimroth Rearrangement of 6-Cyano-l,2,4-triazolo- [4,3-a]pyrimidin-5- and 7-ones. A Novel Alkylation with Orthoesters and a New Participation of the Cyano Group in the Rearrangement." Zeitschrift für Naturforschung B 53, no. 10 (1998): 1203–12. http://dx.doi.org/10.1515/znb-1998-1017.

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AbstractThe cyclization products of 5-cyano-2-hydrazino-6-phenyl-3,4-dihydropyrimidin-4-one (6) with one carbon inserting agents have been confirmed to be of the 1,2,4-triazolo[4,3-a]pyrimidin- 5(8H)-ones type and not the respective 7-ones, by comparing their alkylated derivatives 10a, 11a, 27 and 28 with the product from the cyclization of the 3-methyl and 3-benzyl derivatives of 6. A novel alkylation process was found when triethyl orthoformate was used as a cyclizing agent. Dimroth rearrangement of 8, 14, 15, 24, 34 and 36 with 2% ethanolic KOH gave the respective triazolo[1,5-a]pyrimidinon

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13

Velihina, Y. S., S. G. Pilyo, I. V. Ivanova, and V. S. Brovarets. "Synthesis of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives and study of their vasodilator activity." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 2 (May 2023): 51–60. http://dx.doi.org/10.32434/0321-4095-2023-147-2-51-60.

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A number of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives were synthesized and characterized. Pyrazolo[1,5-a][1,3,5]triazines with various substituents in the fourth position and a dichloromethyl group in the second position were obtained by the heterocyclization reaction of available N-(2,2-dichloro-1-cyanoethenyl)carboxamides and 5-aminopyrazoles. Oxazolo[4,5-d]pyrimidines were obtained by treating 2-phenyl-4-dichloromethylene-1,3-oxazol-5(4H)-one with the corresponding arylamidine hydrochloride in the presence of triethylamine. The resulting 4,5-dihydro-1H-imidazol

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14

Povidaichyk, M., О. Onysko, and M. Onysko. "SYNTHESIS OF TERMINAL 2-ALKENYL(ALKYNYL)THIO-5-CYANO-6-(p-DIMETHYLAMINOPHENYL)PYRIMIDIN-4-ONES." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, no. 2 (2023): 79–83. http://dx.doi.org/10.24144/2414-0260.2022.2.79-83.

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Functionalized pyrimidines possess a wide spectrum of biological activity. In particular, they have antitumor, antiviral, and anticonvulsant activities, exhibit anti-inflammatory and analgesic effects, and they are inhibitors of aldose reductase, SecA ATPase, azide, and plant growth. The search for methods of synthesis of new functionalized and condensed pyrimidine derivatives is an urgent problem. Alkenyl-functionalized mono- and polycyclic pyrimidines are promise substrates for studying the regioselectivity of electroph ilic heterocyclization reactions under the influence of halogen-co

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15

Abdelhamid, Abdou O., and Sobhi M. Gomha. "Synthesis of New Pyrazolo[1,5-a]pyrimidine, Triazolo[4,3-a]pyrimidine Derivatives, and Thieno[2,3-b]pyridine Derivatives from Sodium 3-(5-Methyl-1-phenyl-1H-pyrazol-4-yl)-3-oxoprop-1-en-1-olate." Journal of Chemistry 2013 (2013): 1–7. http://dx.doi.org/10.1155/2013/327095.

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Condensation of sodium 3-oxo-3-(1-phenyl-1H-pyrazol-4-yl)prop-1-en-1-olate (2) with several heterocyclic amines, cyanoacetamide, cyanothioacetamide, and 2-cyanoacetohydrazide gives pyrazolo[1,5-a]pyrimidines (5a–d), pyrido[2′,3′:3,4]pyrazolo[1,5-a]pyrimidine (9), benzo[4,5]imidazo[1,2-a]pyrimidine (10), [1,2,4]triazolo[1,5-a]pyrimidine (11), and pyridine derivatives (12–14). Also, thieno[2,3-b]pyridines (15–18) were synthesized via pyridinethione (13) withα-halo ketones andα-halo ester. Structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, alternat

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16

Abdelhamid, Ismail A., Amr M. Abdelmoniem, Farid M. Sroor, Muhammed A. Ramadan, and Said A. S. Ghozlan. "Hantzsch-Like One-Pot Three-Component Synthesis of Heptaazadicyclopenta[a,j]anthracenes: A New Ring System." Synlett 31, no. 09 (2020): 895–98. http://dx.doi.org/10.1055/s-0040-1708001.

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A concise and efficient approach to novel tetrahydroheptaazadicyclopenta[a,j]anthracene-5,7-diones, by the reaction of aldehydes with two moles of 7-amino-2-methyl-3-phenylpyrazolo[1,5-a]pyrimidin-5-one is reported. Also, pyrazolo[1,5-a]pyrido[3,2-e]pyrimidine-7-carbonitrile derivatives were prepared by a three-component reaction of aldehydes, 7-amino-2-methyl-3-phenylpyrazolo[1,5-a]pyrimidin-5-one, and 3-aminocrotononitrile.

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17

Tkachenko, Irina G., Sergey A. Komykhov, Vladimir I. Musatov, et al. "In water multicomponent synthesis of low-molecular-mass 4,7-dihydrotetrazolo[1,5-a]pyrimidines." Beilstein Journal of Organic Chemistry 15 (October 8, 2019): 2390–97. http://dx.doi.org/10.3762/bjoc.15.231.

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The three-component reaction of 5-aminotetrazole with aliphatic aldehydes (formaldehyde, acetaldehyde) and acetoacetic ester derivatives in water under microwave irradiation leads to the selective formation of 4,7-dihydrotetrazolo[1,5-a]pyrimidine derivatives. Under similar conditions using 4,4,4-trifluoroacetoacetic ester 5-hydroxy-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidines are obtained. The analogous reaction with acetylacetone requires scandium(III) triflate as catalyst. The antioxidant activity of selected compounds was assayed with 1,1-diphenyl-2-picrylhydrazyl.

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18

Severina, Hanna, Olga O. Skupa, Natalya I. Voloshchuk, Marharyta M. Suleiman, and Victoriya A. Georgiyants. "Synthesis and anticonvulsant activity of 6-methyl-2-((2-oxo-2-arylethyl)thio)pyrimidin-4(3 H)-one derivatives and products of their cyclization." Pharmacia 66, no. 3 (2019): 141–46. http://dx.doi.org/10.3897/pharmacia.66.e38137.

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The alkylation of 6-methyl-2-thioxo-2,3-dihydro-1H-pyrimidine-4-one phenacyl bromides under different conditions was investigated. It was found that during the reaction in the medium of DMF/K2CO3 a mixture of 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one and 3-hydroxy-3-aryl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-5-one was formed. The holding of the resulting mixture in the concentrated sulphuric acid leads to the formation of cyclization products - derivatives of 3-aryl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one with high yields. Individual S-alkylated derivatives – 2-(2-

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19

Severina, Hanna I., Olga O. Skupa, Natalya I. Voloshchuk, Marharyta M. Suleiman, and Victoriya A. Georgiyants. "Synthesis and anticonvulsant activity of 6-methyl-2-((2-oxo-2-arylethyl)thio)pyrimidin-4(3 H)-one derivatives and products of their cyclization." Pharmacia 66, no. (3) (2019): 141–46. https://doi.org/10.3897/pharmacia.66.e38137.

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The alkylation of 6-methyl-2-thioxo-2,3-dihydro-1H-pyrimidine-4-one phenacyl bromides under different conditions was investigated. It was found that during the reaction in the medium of DMF/K<sub>2</sub>CO<sub>3</sub> a mixture of 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one and 3-hydroxy-3-aryl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-5-one was formed. The holding of the resulting mixture in the concentrated sulphuric acid leads to the formation of cyclization products - derivatives of 3-aryl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one with high yields. Individual S-alkylat

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20

Thanki, Pragna H., Dhaval V. Hingrajiya, Jayesh J. Modha, and Jalpa H. Vadgama. "Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile." Current Chemistry Letters 12, no. 3 (2023): 537–44. http://dx.doi.org/10.5267/j.ccl.2023.3.002.

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Extensive research work has been published on Tetrahydro and Dihydropyrimidine derivatives. Pyrimidine-5-Carbonitrile and its analogs have demonstrated a large number of activities. Some 6-Halogenosubstituted pyrimidine analogs have also been reported to be biologically active to a certain extent, but the literature survey reveals not much report on 6-alkylated pyrimidine derivatives. Targeting enhancement in biologically useful properties of a lead molecule through the association of it with active pharmacophoric groups or molecules is a conventional method in pharmaceutical research. With an

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21

Hassaneen, Hamdi M., Fatma M. Saleh, Tayseer A. Abdallah, et al. "Synthesis, Cytotoxicity, Antimicrobial and Docking Simulation of Novel Pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[3,4-c] pyrimidine Derivatives." Mini-Reviews in Medicinal Chemistry 19, no. 8 (2019): 657–70. http://dx.doi.org/10.2174/1389557518666181017162459.

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Background:Isobutyrohydrazonoyl bromide 1 was used as a precursor for the synthesis of 4-imino-3-isopropyl-1-(4-nitrophenyl)-1,4-dihydro-5H-pyrazolo[3,4-d]pyrimidin-5-amine 4, which was converted into hydrazino derivative 5 by heating with hydrazine hydrate at reflux. Hydrazino, as well as imino-amino derivatives, underwent condensation and cyclization reactions to give pyrazolo[ 3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[3,4-c]pyrimidine derivatives, respectively.Method:Antimicrobial studies are performed using two-gram positive bacteria and two-gram negative bacteria.Results:Data re

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22

Pinheiro, Alessandra C., Thaís C. M. Nogueira, Cristiane França da Costa, et al. "A study of antituberculosis activities and crystal structures of (E)-2-[2-(arylidene)hydrazinyl]pyrimidine and (E)-N1-(arylidene)pyrimidine-2-carbohydrazide derivatives." Zeitschrift für Naturforschung B 75, no. 12 (2020): 1011–28. http://dx.doi.org/10.1515/znb-2020-0108.

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AbstractA study of the anti-tuberculosis activity against Mycobacterium tuberculosis ATTC 27294 and an X-ray structural determination of (E)-2-[2-(arylidene)hydrazinyl]pyrimidine, 1, and (E)-N1-(arylidene)pyrimidine-2-carbohydazide, 2, derivatives are presented. The effect of the substituents in the aryl moiety on the antituberculosis (anti-TB) activities of 1 and 2 is compared with that of other heteroaryl hydrazonyl and acylhydrazonyl derivatives. The biological activities of 1 do not depend on the coordinating ability of the substituted aryl group: in 2, the most effective aryl group is 5-n

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23

Ogorodnik, A. G., V. A. Yanchenko, L. S. Bobkova, N. M. Seredinska та A. M. Demchenko. "Synthesis and anаlgеsic activity 5-methyl-3-aryl[1,2,4]triazolo[4,3-a]pyrimidin-7-oles derivatives". Farmatsevtychnyi zhurnal, № 2 (14 серпня 2018): 55–61. http://dx.doi.org/10.32352/0367-3057.2.17.07.

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Pain is a signal of inflammation and disruption of the body. It is the most important protective and adaptive mechanism that ensuring the safety of the individual. A strong and prolonged effect of "pain" irritant arising in injuries or after surgical manipulation transforms the protective reaction of the body to harmful factor that is the cause of secondary violations physiological processes. The aim of this work was the synthesis of substances in a series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol and study the analgesic effect of the synthesized compounds. The ob

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Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Chalcone, Pyrazoline, Pyrimidine - 2 - One, Pyrimidine - 2 - Thione,para-Acetanilide Sulphonyl and Benzoyl Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 30–41. http://dx.doi.org/10.1155/2005/953107.

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1, 2 - Dichloro benzene on chlorosulphonation by chlorosulphonic acid gives 1, 2 - [dichloro] - benzene sulphonyl chloride which on condensation withp–amino acetophenone gives 1-[acetyl] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative. This derivative undergo condensation with 2,4- dichloro benzaldehyde gives 1- [3” - (sub. phenyl) - 2” - propene - 1” - one] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative which on reaction with 99% hydrazine hydrate and glacial acetic acid gives 1-[acetyl]-3- [1’ , 2’ - (dichloro) - dibenz sulphonamide] -5 - [2” , 4” - dichloro phenyl] - 2 - py

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25

Aly, Aly A. "A Facile Synthesis and Heteroannulation of Thiazolopyrimidine and Related Heterocyclic Systems." Journal of Chemical Research 2007, no. 9 (2007): 552–56. http://dx.doi.org/10.3184/030823407x248621.

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Reaction of pyrimidinylacetic acid 2 with different electrophilic and nucleophilic reagents gave annulated pyrimidine derivatives 3–11, respectively. Compound 3 ([7-(dibenzothien-2-yl)-5-phenyl-2,3-dihydro-5H-thiazolo[3,2-a]-pyrimidin-6-yl]acetic acid) was transformed to pyrimidinylacetyl azide 12, which upon heterocyclisation with active methylene compounds, acidic and basic reagents furnished functionally substituted heteroaromatic compounds 13–21, respectively. The structures of the synthesised derivatives were elucidated by elemental and spectral analyses.

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Kim, Juhyeon, Yoon Jung Kim, Ashwini M. Londhe, et al. "Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT2C Agonists." Molecules 24, no. 18 (2019): 3234. http://dx.doi.org/10.3390/molecules24183234.

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Here, we describe the synthesis of disubstituted pyrimidine derivatives and their biological evaluation as selective 5-HT2C agonists. To improve selectivity for 5-HT2C over other subtypes, we synthesized two series of disubstituted pyrimidines with fluorophenylalkoxy groups at either the 5-position or 4-position and varying cyclic amines at the 2-position. The in vitro cell-based assay and binding assay identified compounds 10a and 10f as potent 5-HT2C agonists. Further studies on selectivity to 5-HT subtypes and drug-like properties indicated that 2,4-disubstituted pyrimidine 10a showed a hig

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Yakovlev, Dmitry S., Pavel M. Vassiliev, Yana V. Agatsarskaya, et al. "Searching for novel antagonists of adenosine A1 receptors among azolo[1,5-a]pyrimidine nitro derivatives." Research Results in Pharmacology 8, no. (2) (2022): 69–75. https://doi.org/10.3897/rrpharmacology.8.77854.

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Introduction: Ligands of adenosine A<sub>1</sub>Rs are potential candidates for the development of drugs for the treatment of paroxysmal supraventricular tachycardia, angina pectoris, hypertriglyceridemia, type 2 diabetes mellitus, neuropathic pain, and heart failure. At the same time, there is a deficiency of drugs that can regulate the functions of A<sub>1</sub> receptors. A number of A<sub>1</sub>-antagonists are at the various stages of clinical trials; other drugs are not very selective or are characterized by an insufficient breadth of their therapeutic action. Therefore, the search for

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Sharma, M. C. "QSAR STUDIES ON PYRAZOLO [1, 5-A] PYRIMIDINE-BASED PIM-1 KINASE INHIBITORS." INDIAN DRUGS 53, no. 11 (2016): 12–19. http://dx.doi.org/10.53879/id.53.11.10594.

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Quantitative structure-activity relationships (QSAR) have been applied in order to explain the structural requirements of Pim-1 kinase activity of pyrazolo [1, 5-a] pyrimidine derivatives. The QSAR model was an internal predictive power (q2 = 0.7866) of 78% and a predictivity for the external test set (pred_r2 = 0.7742) of about 77%. The developed significant QSAR model indicates that HUMO energy, SsOHcount, SsNH2Count and T_O_O_4 potential of whole molecule play an important role in Pim-1 kinase inhibitor of pyrimidine. Consequently, these results can be useful in identifying the structural r

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29

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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30

Zeng, Qing, Demin Ren, Aiting Zheng, and Xiaofang Li. "Synthesis of Octahydropyrano[2,3-d]Pyrimidine Derivatives via Tetrahydropyrano[3,2-e][1,3]Thiazolo[3,2-a]Pyrimidine and 2,6-Dichlorobenzonitrile Oxide." Journal of Chemical Research 42, no. 6 (2018): 317–19. http://dx.doi.org/10.3184/174751918x15293130141511.

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N1-substituted octahydro-1 H-pyrano[2,3- d]pyrimidines derivatives were prepared in moderate yield by the reaction of methyl [(4a RS,5 SR,10a RS)-5-aryl-2-oxo-3,4,4 a,10 a-tetrahydro-2 H,5 H-pyrano[3,2- e][1,3]thiazolo[3,2- a]pyrimidin-8(9 H)-ylidene]acetate and 2,6-dichorobenzonitrile oxide via a domino 1,3-dipolar cycloaddition/ring-opening/dethionation process. The structures of the products were characterised by spectroscopic and X-ray crystallographic analysis.

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31

Kokorekin, Vladimir A., Sergey V. Neverov, Vera N. Kuzina, and Vladimir A. Petrosyan. "A New Method for the Synthesis of 3-Thiocyanatopyrazolo[1,5-a]pyrimidines." Molecules 25, no. 18 (2020): 4169. http://dx.doi.org/10.3390/molecules25184169.

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In this article, we demonstrate how an original effective “metal-free” and “chromatography-free” route for the synthesis of 3-thiocyanatopyrazolo[1,5-a]pyrimidines has been developed. It is based on electrooxidative (anodic) C–H thiocyanation of 5-aminopyrazoles by thiocyanate ion leading to 4-thiocyanato-5-aminopyrazoles (stage 1, yields up to 87%) following by their chemical condensation with 1,3-dicarbonyl compounds or their derivatives (stage 2, yields up to 96%). This method is equally effective for the synthesis of 3-thiocyanatopyrazolo[1,5-a]pyrimidines, both without substituents and wi

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32

El-Bayouki, Khairy Abdelhameed Mohsen, Wahid Mohmoud Basyouni, and Eslam Attya Mostafa. "Synthesis of new pyrrole and pyrrolo[2,3-d]pyrimidine derivatives of potential antioxidant activity." Collection of Czechoslovak Chemical Communications 75, no. 8 (2010): 813–34. http://dx.doi.org/10.1135/cccc2009566.

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New 2-amino-3-cyanopyrrole derivatives were prepared and converted to 7-deazapurines. 7-Deazaadenine 6 was synthesized by different methods and alkylated with alkyl iodides to afford the quaternized 3-alkylpyrrolopyrimidinium iodide salts 8. The latter salts were dequaternized to N-alkylpyrrolo[2,3-d]pyrimidin-4-amines 12. Compounds 12 were identical to the products obtained from reactions of 4-chloro-7-(4-fluorophenyl)-5-p-tolyl-7H-pyrrolo[2,3-d]pyrimidine 11 with methyl- or ethylamine in the presence of a catalyst. The thione 13 and its related 4-methylthio- and 4-ylcarbonothioate derivative

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33

Leškovskis, Kristaps, Anatoly Mishnev, Irina Novosjolova, and Māris Turks. "SNAr Reactions of 2,4-Diazidopyrido[3,2-d]pyrimidine and Azide-Tetrazole Equilibrium Studies of the Obtained 5-Substituted Tetrazolo[1,5-a]pyrido[2,3-e]pyrimidines." Molecules 27, no. 22 (2022): 7675. http://dx.doi.org/10.3390/molecules27227675.

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A straightforward method for the synthesis of 5-substituted tetrazolo[1,5-a]pyrido[2,3-e]pyrimidines from 2,4-diazidopyrido[3,2-d]pyrimidine in SNAr reactions with N-, O-, and S- nucleophiles has been developed. The various N- and S-substituted products were obtained with yields from 47% to 98%, but the substitution with O-nucleophiles gave lower yields (20–32%). Furthermore, the fused tetrazolo[1,5-a]pyrimidine derivatives can be regarded as 2-azidopyrimidines and functionalized in copper(I)-catalyzed azide-alkyne dipolar cycloaddition (CuAAC) and Staudinger reactions due to the presence of a

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34

Kordian, Marcus, Holger Feist, and Klaus Peseke. "Anellation and Ring Transformations of Push-pull-functionalized Deoxypyranosiduloses." Zeitschrift für Naturforschung B 64, no. 6 (2009): 676–82. http://dx.doi.org/10.1515/znb-2009-0613.

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Reaction of (E)-3-aminomethylene-α-D-erythro-hexopyranosid-2-ulose 5 with substituted 5- aminopyrazoles afforded the pyrano-anellated pyrazolo[1,5-a]pyrimidines 8. The treatment of the corresponding (E)-2-aminomethylene-α-D-erythro-hexopyranosid-3-ulose 6 with 5-aminopyrazoles and (benzimidazol-2-yl)acetonitrile yielded in a ring transformation process the D-erythronoyl-pyrazolo[ 1,5-a]pyrimidine-3-carbonic acid derivatives 10 and D-erythronoyl-pyrido[1,2-a]benzimidazole- 4-carbonitrile (12), respectively

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35

Votruba, Ivan, Antonín Holý, Hana Dvořáková та ін. "Synthesis of 2-Deoxy-β-D-ribonucleosides and 2,3-Dideoxy-β-D-pentofuranosides on Immobilized Bacterial Cells". Collection of Czechoslovak Chemical Communications 59, № 10 (1994): 2303–30. http://dx.doi.org/10.1135/cccc19942303.

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Alginate gel-entrapped cells of auxotrophic thymine-dependent strain of E. coli catalyze the transfer of 2-deoxy-D-ribofuranosyl moiety of 2'-deoxyuridine to purine and pyrimidine bases as well as their aza and deaza analogs. All experiments invariably gave β-anomers; in most cases, the reaction was regiospecific, affording N9-isomers in the purine and N1-isomers in the pyrimidine series. Also a 2,3-dideoxynucleoside can serve as donor of the glycosyl moiety. The acceptor activity of purine bases depends only little on substitution, the only condition being the presence of N7-nitrogen atom. On

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36

El-mahdy, Kamelia, Azza El-Kazak, Mohamed Abdel-Megid, Magdy Seada, and Osama Farouk. "Synthesis, Characterization and Biological Evaluation of some New Thieno[2,3-d]Pyrimidine Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 5, no. 1 (2009): 581–91. http://dx.doi.org/10.24297/jac.v5i1.937.

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10-Oxo-4,6,7,8,9,10-hexahydroprazolo[1,5-a][1]benzothieno[2,3-d]pyrimidine-3-carbaldehyde (2) was prepared by Vilsmeier-Haack reaction of 3-amino-2-methyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one (1). Reaction of carbaldehyde derivative 2 with malononitrile afforded arylidene malononitrile 3. Cyclization of the latter compound with thiourea yielded pyrimidinethione 4. Interaction of carbaldehyde derivative 2 in presence of thiourea with keto- compounds such as ethyl acetoacetate, or acetylacetone, or dimedone or ethyl cyanoacetate gave pyrimidine derivatives 5-8. Hydrazinolys

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37

Banfield, JE, GD Fallon, and BM Gatehouse. "Heterocyclic-Derivatives of Guanidine. VI. Formation and X-Ray Structure Determination of 2-Dimethylamino-7,8-diphenyl-4,6-dihydropyrrolo[1,2-a]pyrimidine-4,6-dione." Australian Journal of Chemistry 40, no. 5 (1987): 1003. http://dx.doi.org/10.1071/ch9871003.

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The structure N-(2-dimethylamino-4-oxo-7,8-diphenyl-4,6-dihydropyrrolo [l,2-a]pyrimidi n-6-yl-idene)acetamide (3) is proposed for a compound derived from the action of ketene on 2-(2-imino- 3,4-diphenyl-2H-pyrrol-5-yl)-1,1,3-trimethylguanidine (1; R1 = R2 = R3 = Me) on the basis of the crystal structure of its hydrolysis product, the oxo-compound 2-dimethylamino-7,8-diphenyl-4,6-dihydropyrrolo[l,2-a]pyrimidine-4,6-dione (4), the structure of which was determined by X-ray analysis. A lower homologue of (3), N-(2-methylamino-4-oxo-7,8-diphenyl-4,6-dihydro- pyrrolo[l,2-a]pyrimidin-6-ylidene)aceta

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38

Arshad, Uzma, Sibtain Ahmed, Nusrat Shafiq, et al. "Structure-Based Designing, Solvent Less Synthesis of 1,2,3,4-Tetrahydropyrimidine-5-carboxylate Derivatives: A Combined In Vitro and In Silico Screening Approach." Molecules 26, no. 15 (2021): 4424. http://dx.doi.org/10.3390/molecules26154424.

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Objective: In this study, small molecules possessing tetrahydropyrimidine derivatives have been synthesized having halogenated benzyl derivatives and carboxylate linkage. As previously reported, FDA approved halogenated pyrimidine derivatives prompted us to synthesize novel compounds in order to evaluate their biological potential. Methodology: Eight pyrimidine derivatives have been synthesized from ethyl acetoacetate, secondary amine, aromatic benzaldehyde by adding catalytic amount of CuCl2·2H2O via solvent less Grindstone multicomponent reagent method. Molecular structure reactivity and vir

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39

Sultana, Shameem, and Shiva kumar. "Novel Pyrimidine Carboxamide Derivatives - Potential Anticancer Agents: Synthesis and Characterization." Der Pharma Chemica 14, no. 10 (2022): 9. https://doi.org/10.4172/0975-413X.14.10.34-42.

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Background: Cancer was credited as the second leading cause to global death rate with estimated toll of deaths more than 18 million. Though many anticancer agents are available in the market, there is an essential need to explore novel drug candidates for cancer treatment due to the various adverse effects associated with the current anticancer agents. Pyrimidine scaffold is a ubiquitous heterocyclic system present in important anticancer agents. Current investigation aims to find the newer class of anticancer lead molecules with pyrimidine as the central pharmacophore. Objective: Primary obje

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40

S. AL-Rawi, Muna, Huda A. Hassan, Dheefaf F. Hassan та Ismaeel Y. Majeed. "New Series of Substituted Heterocyclics Derived from α , β – Unsaturated Ketone and Their Cytotoxic Activity Tumor Cell Lines". Oriental Journal of Chemistry 34, № 6 (2018): 2826–31. http://dx.doi.org/10.13005/ojc/340620.

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The aldol condensation of 2-acetylnaphthalene with 9-anthracene carboxaldehyde afforded α, β-unsaturated keton (1) . New heterocyclic compounds containing: cyclohexenone[2], indazole[3], pyrimidinethion [4], thiazolo fused pyrimidine[5], isoxazoline[6], substituted pyrazoline[7]a-d and pyrimidinone[8] rings system were synthesized from α, β-unsaturated keton[1]. Cyclization of [1] with ethylacetoacetate gave the mentioned heterocycle cyclohexanone [2]. The cyclo condensation of [2] with hydrazine gave the new indazole derivative [3]. furthermore, the reation of [1]with thiourea gives thiopyrmi

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41

Gorneva, Galina, Rada Mateva, Roumyana Gugova, and Evgeny Golovinsky. "The study of the apoptogenic effect of pyrimidine derivatives on murine leukemia cells." Archive of Oncology 13, no. 2 (2005): 62–64. http://dx.doi.org/10.2298/aoo0502062g.

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BACKGROUND: In the light of the recent findings concerning the role of apoptosis and of tumor cell enzymes in cancer chemotherapy, the interest in pyrimidine derivatives has greatly increased. Thio- and hydrazine- pyrimidines were synthesized as potential antimetabolites inhibiting the biosynthesis of nucleic acids. Some of them demonstrated biological activity, including antibacterial and antitumor action. The aim of this study was to analyze the cytotoxic activity and the ability of some derivatives to induce apoptosis in murine leukemia cells. METHODS: Exponentially growing cells were incub

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42

Verma, Mohan, and Prabhakar Kumar Verma. "Synthesis, characterization, antimicrobial and anticancer evaluation of (E)-N'-benzylidene-6-methyl-4-(2-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carbohydrazide derivatives." Journal of medical pharmaceutical and allied sciences 11, no. 2 (2022): 4498–502. http://dx.doi.org/10.55522/jmpas.v11i2.2190.

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The synthesis of a novel family of pyrimidine derivatives has been completed. Infrared–infrared (IR) and proton nuclear magnetic resonance (1H NMR) spectrum data were used to describe these pyrimidine derivatives. All the compounds were evaluated for their in vitro antimicrobial activity against Gram negative strain (Escherichia coli) and Gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strain (Candida albicans and Aspergillus niger) and anticancer potential against Human breast cancer cell line (MCF-7). Results of antimicrobial and anticancer study revealed that

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43

Sushma Somkuwar and Neelesh Chaubey. "Pyrimidine derivatives: Their significance in the battle against malaria, cancer and viral infections." GSC Biological and Pharmaceutical Sciences 25, no. 2 (2023): 076–83. http://dx.doi.org/10.30574/gscbps.2023.25.2.0451.

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Pyrimidine derivatives play a significant role in combating viral infections, malaria, and cancer due to their diverse pharmacological properties. Pyrimidine derivatives, particularly nucleoside analogs, have been widely used as antiviral agents. They interfere with viral replication by inhibiting DNA or RNA synthesis.Examples include drugs like acyclovir (used against herpes viruses), lamivudine (for HIV and hepatitis B), and remdesivir (for COVID-19). These compounds help to manage and treat various viral infections, reducing their severity and spread. Pyrimidine derivatives are key componen

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44

Sushma, Somkuwar, and Chaubey Neelesh. "Pyrimidine derivatives: Their significance in the battle against malaria, cancer and viral infections." GSC Biological and Pharmaceutical Sciences 25, no. 2 (2023): 076–83. https://doi.org/10.5281/zenodo.10608620.

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Pyrimidine derivatives play a significant role in combating viral infections, malaria, and cancer due to their diverse pharmacological properties. Pyrimidine derivatives, particularly nucleoside analogs, have been widely used as antiviral agents. They interfere with viral replication by inhibiting DNA or RNA synthesis.Examples include drugs like acyclovir (used against herpes viruses), lamivudine (for HIV and hepatitis B), and remdesivir (for COVID-19). These compounds help to manage and treat various viral infections, reducing their severity and spread. Pyrimidine derivatives are key componen

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45

Hafez, Hend N., Abdel-Rhman B. A. El-Gazzar, and Magdi E. A. Zaki. "Simple approach to thieno[3,2-d]pyrimidines as new scaffolds of antimicrobial activities." Acta Pharmaceutica 66, no. 3 (2016): 331–51. http://dx.doi.org/10.1515/acph-2016-0029.

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Abstract 6ʹ-(4-Chlorophenyl)-spiro[cyclohexane-1,2ʹ-thieno[3,2-d][1,3] oxazin]-4ʹ(1ʹH)-one (1) was synthesized and used as a starting material for the synthesis of a novel series of spiro compounds having biologically active sulfonamide 2a-e and 3ʹ-(4-acetylphenyl)-6ʹ- (4-chlorophenyl)-1ʹH-spiro[cyclohexane-1,2ʹ-thieno[3,2-d] pyrimidine-4ʹ(3ʹH)-one (3). Compound 2a was used as a key intermediate for the synthesis of sulfonyl carbothioamide derivatives 4a-c. Also, compound 3 was used as an intermediate for the synthesis of 3ʹH-spiro[cyclohexane-1,2ʹ-thieno[3,2-d]pyrimidin]-3ʹ-yl] phenyl}-2-imin

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46

Gu, Yi-Fei, Yue Zhang, Feng-li Yue, et al. "Synthesis of Novel 2-(Pyridin-2-yl) Pyrimidine Derivatives and Study of Their Anti-Fibrosis Activity." Molecules 25, no. 22 (2020): 5226. http://dx.doi.org/10.3390/molecules25225226.

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A pyrimidine moiety exhibiting a wide range of pharmacological activities has been employed in the design of privileged structures in medicinal chemistry. To prepare libraries of novel heterocyclic compounds with potential biological activities, a series of novel 2-(pyridin-2-yl) pyrimidine derivatives were designed, synthesized and their biological activities were evaluated against immortalized rat hepatic stellate cells (HSC-T6). Fourteen compounds were found to present better anti-fibrotic activities than Pirfenidone and Bipy55′DC. Among them, compounds ethyl 6-(5-(p-tolylcarbamoyl)pyrimidi

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47

Agarkov, Artem S., Anna A. Nefedova, Elina R. Gabitova, et al. "Synthesis, Self-Assembly in Crystalline Phase and Anti-Tumor Activity of 2-(2-/4-Hydroxybenzylidene)thiazolo[3,2-a]pyrimidines." Molecules 27, no. 22 (2022): 7747. http://dx.doi.org/10.3390/molecules27227747.

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A series of new thiazolo[3,2-a]pyrimidines different by aryl substituents in 2 and 5 positions are synthesized and characterized in solution as well as in the crystalline phase using 1H and 13C NMR-, IR-spectroscopies, mass-spectrometry methods, and single crystal X-ray diffraction (SCXRD). The SCXRD study revealed the role of intermolecular H-bonding in the formation of supramolecular architectures (racemic monomers, centrosymmetric racematic dimers, or homochiral 1D chains) of obtained thiazolo[3,2-a]pyrimidines derivatives depending on solvents (aprotic DMSO or protic EtOH) used upon the cr

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48

Kezin, Vasily A., Elena S. Matyugina, Mikhail S. Novikov, et al. "New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity." Molecules 27, no. 9 (2022): 2866. http://dx.doi.org/10.3390/molecules27092866.

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Pyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through various mechanisms. Among the 5-substituted pyrimidine nucleosides, there are not only the classical nucleoside inhibitors of the herpes family viruses, 2′-deoxy-5-iodocytidine and 5-bromovinyl-2′-deoxyuridine, but also derivatives of 1-(benzyl)-5-(phenylamino)uracil, which proved to be non-nucleoside i

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49

Jeon, Hyejin, Yong-Guy Kim, Jin-Hyung Lee, and Jintae Lee. "Antibiofilm Activities of Halogenated Pyrimidines Against Enterohemorrhagic Escherichia coli O157:H7." International Journal of Molecular Sciences 26, no. 3 (2025): 1386. https://doi.org/10.3390/ijms26031386.

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Enterohemorrhagic Escherichia coli (EHEC) is a significant public health concern due to its ability to form biofilms, enhancing its resistance to antimicrobials and contributing to its persistence in food processing environments. Traditional antibiotics often fail to target these biofilms effectively, leading to increased bacterial resistance. This study aims to explore the efficacy of novel antibiofilm agents, specifically halogenated pyrimidine derivatives, against EHEC. We screened pyrimidine and 31 halogenated pyrimidine derivatives for their antimicrobial and antibiofilm activities agains

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50

Hammouda, M., A. S. El-Ahl, Y. M. El-Toukhee, and M. A. Metwally. "Reactions of Ketonic Mannich Bases with Malononitrile and Malononitrile dimer." Journal of Chemical Research 2002, no. 2 (2002): 89–94. http://dx.doi.org/10.3184/030823402103171258.

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The reaction of malononitrile with the tertiary Mannich base hydrochloride derived from acetophenone and some related compounds 1, 3, 5 and 7, in piperidine at 50°C afforded the pyrido[1,2-a]pyrimidine derivatives 2, tetrahydronaphthalene derivative 4 substituted quinolines 6 and benzopyran derivatives 8. While the condensation of malononitrile dimer with acetophenone, cyclohexanone and/ or α-tetralone Mannich bases hydrochloride 1, 3 and 9 gave the pyridine, isoquinoline and benzo[f]isoquinoline derivatives 10–12 in moderate to good yield.

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