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Journal articles on the topic 'Guanidino pyrimidines'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

Durgadas, Mukherjee, and Nath Das Soumendra. "Design, synthesis and spectral characterization of chelates of PdII , PtII and RhIII with 6-guanidino-2,4-dimethyl-3,5-diazine and 6-phenyl guanidino-2,4-dimethyl3,5-diazine-potentialligands with biological interest." Journal of Indian Chemical Society Vol. 85, Jan 2008 (2008): 148–52. https://doi.org/10.5281/zenodo.5808696.

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Department of Chemistry, Mahadevananda Mahavidyalaya, Monirampur, Barrackpore, Kolkata-700 120, India <em>E-mail:</em> durgadas.mukherjee@gmail.com <em>Manuscript received 18 July 2007, revised 7 November 2007, accepted 19 November 2007</em> Complexes of 6-guanidino-2,4-dimethyl-3,5-diazine and 6-phenyl guanidino-2,4-dimethyl-3,5-diazine with Pd<sup>II</sup>, Pt<sup>II</sup> and Rh<sup>III</sup> have been reported. Complexes have been characterised on the basis of analytical, magnetic and spectral characterization and powder diffraction studies. Crystal field parameters have also been calculat

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2

Borrell, José I., Jordi Teixidó, Blanca Martínez-Teipel, et al. "An Unequivocal Synthesis of 4-Amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones and 2-Amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones." Collection of Czechoslovak Chemical Communications 61, no. 6 (1996): 901–9. http://dx.doi.org/10.1135/cccc19960901.

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An unequivocal set of procedures for the synthesis of 4-amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones (7) and 2-amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones (8), in a maximum of four steps from an α,β-unsaturated ester 1, is reported. Thus, the acid hydrolysis of the 2,4-diaminopyrido[2,3-d]pyrimidines 3 yields the 4-amino-2-oxopyrido[2,3-d]pyrimidines 7 while the cyclization of the Michael adducts 9 (formed by reaction of 1 and methyl cyanoacetate) with guanidine affords the corresponding 2-amino-4-oxopyrido[2,3-d]pyrimidines 8. Both isomers were also obtained by hy

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3

Verma, Vishal, Chandra Prakash Joshi, Alka Agarwal, Sakshi Soni, and Udichi Kataria. "A Review on Pharmacological Aspects of Pyrimidine Derivatives." Journal of Drug Delivery and Therapeutics 10, no. 5 (2020): 358–61. http://dx.doi.org/10.22270/jddt.v10i5.4295.

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Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogens at positions 1 and 3 in the ring. Pyrimidines are typically synthesized by the “Principal Synthesis” involving cyclization of beta-dicarbonyl compounds with N-C-N compounds. Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidiones, and guanidines to give 2-aminopyrimidines are typical. Pyrimidines can be prepared via the biginelli reaction. Many other methods

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4

R., S. Dhivare, and S. Rajput S. "Microwave Assisted Synthesis and Microbial Screening of Novel Amino-pyrimidine Derivatives using Bis-chalcones." Journal of Chemistry and Chemical Sciences (An International Research Journal), www.chemistry-journal.org 5, no. 10 (2015): 550–56. https://doi.org/10.5281/zenodo.3909691.

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ABSTRACT A simple and clean one pot method for the preparation of amino-pyrimidine derivatives using chalcones of cyclic imides and guanidine nitrate in presence of neutral alumina under microwave supported solvent free condition is described. Some of the synthesized amino-pyrimidines showed synergistic significant activities against Candida albicans and Aspergillus niger fungal strains.

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5

R., PRASAD REDDY, RAVINDRANATH A., SUDHAKAR B., SUNDARA RAMAIAH T., and VENKATESHWER RAO M. "Azatriterpenes. Part-VIII. Synthesis of Ring-A Fused Pyrimidines of Pentacyclic Triterpenes." Journal of Indian Chemical Society Vol. 65, Oct 1988 (1988): 688–90. https://doi.org/10.5281/zenodo.6076530.

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Department of Chemistry, Nizam College (Osmania University), Hyderabad-500 001 <em> Manuscript received 5 April 1988, accepted 27 July 1988</em> Condensation of urea, guanidine and thiourea with 2-formyl (hydroxymethylene) derivatives of methyl oleanonate (1), 11-oxomethyl oleanonate (2) and methyl betulonate (3) furnished their respective [3,2-d]pyrimidine-2'-ones (4 -6), 2'-imino-[3,2-d]pyrimidines (7-9) and 2'-mercapto [3,2-<em>d</em>]pyrimidines (10 -12). The compounds were characterised by their elemental and spectral data.

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6

R., S. Dhivare, and S. Rajput S. "Microwave assisted synthesis and antimicrobial screening of novel 9-(N-phenyl) - 4, 5-(2″, ‴- methoxyphenol)-9H-1,3,6,8,9-hexa-azo-fluorene-2,7- diamine derivatives using bis-heterocyclic chalcones." INTERNATIONAL JOURNAL OF ADVANCES IN PHARMACY, BIOLOGY AND CHEMISTRY 4, no. 4 (2015): 863–70. https://doi.org/10.5281/zenodo.3909811.

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<strong>ABSTRACT</strong> Amino-pyrimidine derivatives were synthesized by a simple and clean single pot method using bis-chalcones of different substituted phenyl glutarimides and guanidine nitrate with neutral alumina irradiated under the microwave supported solvent less condition is demonstrated. All the compounds were screened for their antimicrobial activities and showed moderate activities. But certain amino-pyrimidines exhibited synergistic and significant activities against <em>Candida albicans</em> and <em>Aspergillus niger</em> fungal genres.

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7

Priyadarsini, P., V. Madhava Rao, and C. Venkata Rao. "Synthesis, Characterization and Anti-inflammatory Activity of New Pyrimidines." Asian Journal of Organic & Medicinal Chemistry 4, no. 1 (2019): 46–50. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p178.

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The synthesis of some pyrimidine derivatives was achieved by conden-sation of 2-hydroxyacetophenone and cinnamic acid as starting materials through 1,3-diketones as intermediates. The resulting diketones have been converted into substituted pyrimidines by reaction with urea, thiourea and guanidine in the presence of trace of triethylamine and pyridine in calculated quantity. The synthesized compounds were characterized by their physical properties, NMR and LC-mass spectroscopic studies and also screened for their anti-inflammatory activity.

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8

Bannunah, Azzah M., Naeem Fqusty, Bayan Tayeb Bokhari, Saad Alghamdi, Waheeb Alharbi, and Mohammad Asif. "Synthesis and in vitro antihyperglycemic evaluation of some new 3-(4-ethyl-6-methyl pyrimidin-2-yl)-2-arylthiazolidin-4-one derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 01 (2025): 85. https://doi.org/10.59467/ijhc.2025.35.85.

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Due to the pharmacological potential of thiazolidinedione derivatives as antidiabetic drugs, six pyrimidine hybrids of aryl thiazolidin-4-ones (2a-f) were synthesized in two steps. In the first step, 4-ethyl-6-methyl-pyrimidin-2-amine (1) was synthesized by reacting 1,3-hexane-2,4-dione with guanidine. Compound 1 reacted with appropriate aryl aldehyde and mercaptoacetic acid to form compounds 2a-f. All the compounds (2a-f) exhibited varying degrees of a-amylase inhibitory activity, particularly compounds 2b (IC50 = 25 μg/mL), 2f (IC50 = 30 μg/mL), 2a and 2c (IC50 = 35 μg/mL) exhibited consider

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9

El-Sawy, Eslam, Adel Mandour, Khaled Mahmoud, Inas Islam, and Heba Abo-Salem. "Synthesis, antimicrobial and anti-cancer activities of some new N-ethyl, N-benzyl and N-benzoyl-3-indolyl heterocycles." Acta Pharmaceutica 62, no. 2 (2012): 157–79. http://dx.doi.org/10.2478/v10007-012-0020-3.

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Synthesis, antimicrobial and anti-cancer activities of some newN-ethyl,N-benzyl andN-benzoyl-3-indolyl heterocyclesA series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2-ene-1-ones (2a, b-4a, b) were prepared and allowed to react with urea, thiourea or guanidine to give pyrimidine derivatives5a, b-13a, b. Reaction of2a, b-4a, bwith ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives14a, b-16a, b. Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives17a, b-19a, b. On the other hand, reaction of2a, b-4a, bwith some hydrazine derivatives,

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10

Jyothi, K., and M. Kannadasan. "Novel Pyrimidine Tethered Benzamide Derivatives as Potential Anticancer Agents: Synthesis, Characterization, Molecular Docking and In vitro Cytotoxicity Evaluation." Asian Journal of Chemistry 36, no. 12 (2024): 2870–78. https://doi.org/10.14233/ajchem.2024.32688.

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Current research work presents the synthesis, characterization, molecular docking study and in vitro cytotoxicity evaluation of novel pyrimidine-tethered benzamide derivatives as potential anticancer agents. The synthesis involved multi-steps procedure, including the synthesis of various chalcones (3a-t) with corresponding ketones (1 and 2) and substituted aldehydes (a-j), followed by pyrimidine amines (5a-t) with condensation of chalcones and guanidine and finally pyrimidinyl benzamide derivatives (8a-t) from compounds 5a-t coupling with acid chloride (7) using DIBAL-H. Synthesized compounds

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11

Zhang, Liang, Mingzhu Zhao, and Xiaoming Zhao. "The synthesis of carbonyl 2-amino-pyrimidines via tandem regioselective heterocyclization of 1,3-diynes with guanidine and selective oxidation." Chemical Communications 51, no. 45 (2015): 9370–73. http://dx.doi.org/10.1039/c5cc02238j.

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A highly efficient one-pot approach for the synthesis of carbonyl 2-amino-pyrimidines from 1,3-diynes and guanidine in the presence of Cs<sub>2</sub>CO<sub>3</sub> and DMSO has been described. This methodology proves to be a tandem regioselective heterocyclization of 1,3-diynes with guanidine and selective oxidation.

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12

Mohammad, Y. Abu Shuheil. "CONDENSATION OF 2-(2-GUANIDINO-4-OXO-4,5-DIHYDROTHIAZOL-5-YL)ACETIC ACID WITH DICARBONYL COMPOUNDS." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 02 (2018): 1020–27. https://doi.org/10.5281/zenodo.1184056.

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A hybrid pharmacophore approach was adopted to design and synthesize new series of pyrimidine-thiazole hybrid compounds via heterocyclization of 2-(2-guanidino-4-oxo-4,5-dihydrothiazol-5-yl)acetic acid with dicarbonyl compounds, such as diketones and derivatives of acetoacetic ester. The structures of the compounds were established by IR, 1H NMR, 13C NMR. The products were obtained in a good yield, short time and a simple experimental procedure. The synthesized compounds were evaluated for their anti-bacterial activity against Grampositive and Gram-negative bacteria. The compounds exhibited ex

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13

Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Novel Highly Substituted Pyrimidines Bearing Furanyl Thiazole Nucleous." International Letters of Chemistry, Physics and Astronomy 60 (September 2015): 47–57. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.60.47.

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A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

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14

Kathrotiya, Haresh G., and Yogesh T. Naliapara. "Synthesis of Novel Highly Substituted Pyrimidines Bearing Furanyl Thiazole Nucleous." International Letters of Chemistry, Physics and Astronomy 60 (September 30, 2015): 47–57. http://dx.doi.org/10.56431/p-0c50ea.

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A series of novel highly substituted pyrimidines bearing furanyl thiazole nucleous have been synthesized. In which reaction of guanidine nitrate with ketene dithioacetals 3c produced substituted pyrimidines 4d which further treated with various aromatic aldehydes to afford title compounds 5(a-t). The chemical structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, FT-IR, elemental analysis, and mass spectral data.

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15

Singh, Prabal, S. Yugandar, S. Kumar, H. Ila, and H. Junjappa. "Synthesis of Novel Five- and Six-Membered Ferrocene-Containing Heterocycles and Heteroaromatics via Cyclocondensation of 1-Ferrocenyl-3,3-bis(methylthio)prop-2-en-1-one with Various Bifunctional Nucleophiles." Synthesis 49, no. 12 (2017): 2700–2710. http://dx.doi.org/10.1055/s-0036-1588966.

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Synthesis and reactions of 1-ferrocenyl-3,3-bis(methylthio)prop-2-en-1-one as a versatile 1,3-bielectrophilic synthon leading to a range of novel ferrocene-containing five- and six-membered heterocycles and heteroaromatics has been reported. Thus its cyclocondensation with various bifunctional heteronucleophiles, such as hydrazine, phenylhydrazine, hydroxylamine, guanidine, and amidine, affords a range of ferrocene-substituted pyrazoles, oxazoles, and pyrimidines in highly regioselective manner. Synthesis of few ferrocenyl-substituted pyridines and thiophenes has also been described. Similar

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16

Elmes, BC, G. Holan, GT Wernert, and DA Winkler. "The Synthesis of Bisguanidinoalkanes and Guanidinoalkanes, N- or N'-Substituted With Pyrimidines, as Analogues of Chlorhexidine." Australian Journal of Chemistry 49, no. 5 (1996): 573. http://dx.doi.org/10.1071/ch9960573.

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A series of N,N???- alkanediylbis [N?-(5-halopyrimidin-2-yl)guanidine] salts has been synthesized along with N,N???-(trans-cyclohexane-1,4-diyl) bis [N'-(5-chloropyrimidin-2-yl)guanidine], N,N???-(cis-cyclohexane-1,4-diyl) bis [N?-(5-chloropyrimidin-2-yl)guanidine] dihydrochloride and N-(cis-4-amino-cyclohexan-1-yl)-N'-(5-chloropyrimidin-2-yl)guanidine dihydrochloride . Furthermore, a series of N-(alkan-1-yl)-N?-(5-chloropyrimidin-2yl)guanidine hydrochlorides and N-(6-aminohexan-1-yl)-N?-(5-chloropyrimidin-2-yl)guanidine dihydrochloride were synthesized. This series of compounds was prepared b

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17

N. J. Siddiqui, S. D. Kawale, G. M. Phadnaik, H. M. Alone, and S. S. Kola. "SYNTHESIS, ANTIMICROBIAL SCREENING AND MOLECULAR DOCKING STUDY OF SOME NEW PYRIMIDIN2-AMINE DERIVATIVES AS POSSIBLE BIOACTIVE AGENTS." RASAYAN Journal of Chemistry 18, no. 02 (2025): 1072–82. https://doi.org/10.31788/rjc.2025.1829273.

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A novel series of 4, 6-disubstituted pyrimidin-2-amine derivatives (5a–f) was synthesized in good yields via a cyclocondensation reaction of chalcone-based intermediates (4a–f) with guanidine hydrochloride using sodium methoxide as the base. The key intermediates, N'-(5-(3-(2,4-disubstituted phenyl)-3-oxoprop-1-enyl)-4-(4- bromophenyl)-6-(3,4-disubstituted phenyl) pyrimidin-2-yl)-N, N-dimethylformamidine derivatives (4a–f), were prepared from aryl and heteroaryl acetophenones (3a–c) and 4,6-diaryl-substituted pyrimidine-5-carboxaldehydes (2a–b) via Claisen–Schmidt condensation. The structures

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18

Solankee, Anjani, and Riki Tailor. "An Efficient Synthesis and Antimicrobial Evaluation of some New Pyrazoline, Pyrimidine and Benzodiazepine Derivatives Bearing 1,3,5-Triazine Core." International Letters of Chemistry, Physics and Astronomy 57 (August 2015): 13–24. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.57.13.

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In our present investigation a new class of diverse sets of acetyl pyrazolines (6a-e), amino pyrimidines (7a-e) and 1,5-benzodiazepines (8a-e) bearing 1,3,5-triazine core were synthesised from chalcones (5a-e). Treatment of chalcone with hydrazine hydrate, guanidine hydrochloride and o-phenylenediamine afforded the corresponding acetyl pyrazoline, amino pyrimidine and 1,5-benzodiazepine derivatives respectively. The structures of all the newly synthesised compounds were assigned on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data as well as elemental analysis. In vitro antimicrobial prof

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19

Solankee, Anjani, and Riki Tailor. "An Efficient Synthesis and Antimicrobial Evaluation of some New Pyrazoline, Pyrimidine and Benzodiazepine Derivatives Bearing 1,3,5-Triazine Core." International Letters of Chemistry, Physics and Astronomy 57 (August 4, 2015): 13–24. http://dx.doi.org/10.56431/p-9i28k7.

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In our present investigation a new class of diverse sets of acetyl pyrazolines (6a-e), amino pyrimidines (7a-e) and 1,5-benzodiazepines (8a-e) bearing 1,3,5-triazine core were synthesised from chalcones (5a-e). Treatment of chalcone with hydrazine hydrate, guanidine hydrochloride and o-phenylenediamine afforded the corresponding acetyl pyrazoline, amino pyrimidine and 1,5-benzodiazepine derivatives respectively. The structures of all the newly synthesised compounds were assigned on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data as well as elemental analysis. In vitro antimicrobial prof

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20

Yokota, Kenichirou, Masayori Hagimori, Naoko Mizuyama, et al. "Synthesis, solid-state fluorescence properties, and computational analysis of novel 2-aminobenzo[4,5]thieno[3,2-d]pyrimidine 5,5-dioxides." Beilstein Journal of Organic Chemistry 8 (February 16, 2012): 266–74. http://dx.doi.org/10.3762/bjoc.8.28.

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New fluorescent compounds, benzo[4,5]thieno[3,2-d]pyrimidine 5,5-dioxides (3a–g), 2-amino-4-methylsulfanylbenzo[4,5]thieno[3,2-d]pyrimidine (6), and 2-amino-4-methylsulfanyl-7-methoxybenzo[4,5]furo[3,2-d]pyrimidine (7), were synthesized in good yields from heterocyclic ketene dithioacetals (1a–c) and guanidine carbonate (2a) or (S)-methylisothiourea sulfate (2b) in pyridine under reflux. Among the fused pyrimidine derivatives, compound 3c, which has an amino group at the 2-position and a benzylamino group at the 4-position of the pyrimidine ring, showed the strongest solid-state fluorescence.

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21

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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22

Nabeel, Zaizafoon, Qassim Abdul-Hussein Jaber, and Nabeel Abed Abdul-Rida. "Novel Benzo[<i>f</i>]coumarin Derivatives as Probable Acetylcholinesterase Inhibitors: Synthesis, In Vitro, and In Silico Studies for Evaluation of Their Anti-AChE Activity." Indonesian Journal of Chemistry 22, no. 1 (2021): 35. http://dx.doi.org/10.22146/ijc.65663.

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Novel benzo[f]coumarin derivatives bearing pyrimidine unit were successfully synthesized. The target is to develop novel acetylcholinesterase inhibitors. The benzo[f]coumarin chalcone 4 was prepared via Claisen-Schmidt condensation between 3-acetyl-5,6-benzocoumarin and 4-hydroxybenzaldehyde in the alkaline medium. Then, the cyclocondensation of chalcone 4 with urea, thiourea, and guanidine HCl in the presence of glacial acetic acid led to the formation of various pyrimidines. Structures of the newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR spectra, and elemental anal

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23

Al-Ghulikah, H. A., A. S. El-Azab, M. S. AL-Saleem, M. S. AL-Towayan, and S. A. Al-Issa. "Green synthesis, characterization, biological evaluation and docking study of some pyrazoline and pyrimidine derivatives." Research Journal of Chemistry and Environment 25, no. 12 (2021): 88–97. http://dx.doi.org/10.25303/2512rjce8897.

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Green and classical techniques have been utilized for preparing of a variety of aryl - substituted pyrazoline and pyrimidine derivatives (2-8). Reactions of chalcones 1 with semicarbazide and thiosemicarbazide, nicotinic acid hydrazide and amino guanidine hydrochloride afforded the corresponding N-substituted pyrazoline derivatives 2-5. Pyrimidine derivatives 6-8 were achieved via reaction of chalcone derivatives 1 with several reagents namely: guanidine nitrate, thiourea and 6-amino-2-thioxo-2,3- dihydropyrimidin-4(1H)-one under conventional and ultrasonic conditions. Ultrasonic method was fo

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24

Cortés-Percino, Alejandra, José Luis Vega-Báez, Anabel Romero-López, et al. "Synthesis and Evaluation of Pyrimidine Steroids as Antiproliferative Agents." Molecules 24, no. 20 (2019): 3676. http://dx.doi.org/10.3390/molecules24203676.

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A small and focused library of steroidal non-fused and fused pyrimidines was prepared from pregnenolone acetate and diosgenin, respectively. The key step was the cycloaddition reaction of nitrogen-containing 1,3-binucleophiles with the steroidal α,β-unsaturated ketone. Urea, thiourea and guanidine reacted in a similar manner and afforded the steroidal pyrimidines in good yields. The antiproliferative tests against human tumor cell lines gave GI50 values in the micromolar range and had no effect on healthy fibroblasts. Additional experiments indicated that the compounds did not act as P-glycopr

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25

Sharma, Megha, and Sanidhyay Upadhyay. "Synthesis and Antimicrobial Activity of 2-(substituted)-4-[2-(10-p-chlorobenzyl) phenothiazinyl]-6-(substituted aryl)pyrimidines." European Journal of Advanced Chemistry Research 5, no. 5 (2024): 1–4. https://doi.org/10.24018/ejchem.2024.5.5.108.

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A series of novel 2-(substituted)-4-[2-(10-pchlorobenzyl)phenothiazinyl]-6-(substituted aryl)pyrimidines have been synthesized by cyclocondensation of chalcones, obtained by the interaction of 2-acetyl phenothiazine with substituted aromatic aldehydes, with urea, thiourea, and guanidine. Structures of title compounds were elucidated by their IR, 1H NMR spectral data, molecular weight determination, and microanalyses. Antimicrobial activities against gram-positive and gram-negative bacteria were evaluated by the Filter Paper Disc Method.

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26

Kumagai, Shinji, Hiroaki Sawamoto, Tomo Takegawa-Araki, et al. "Synthesis and properties of GuNA purine/pyrimidine nucleosides and oligonucleotides." Organic & Biomolecular Chemistry 18, no. 46 (2020): 9461–72. http://dx.doi.org/10.1039/d0ob01970d.

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Facile synthesis of GuNA (guanidine-bridged nucleic acid) phosphoramidites bearing thymine, adenine, guanine, and 5-methylcytosine nucleobases and a robust method for the preparation of GuNA-modified oligonucleotides are described.

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27

Pravin, R. Kawle, and P. Deohate Pradip. "Synthesis of heterocycles containing pyrimidine-acridine rings by microwave irradiation, antimicrobial study and its comparison with classical heating." Journal of Indian Chemical Society Vol. 92, Jun 2015 (2015): 925–28. https://doi.org/10.5281/zenodo.5637765.

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Department of Chemistry, Shri R. L. T. College of Science, Akola-444 001, Maharashtra, India <em>E-mail</em> : pravink280685@rediffmail.com New series of linked heterocycles containing acridine and pyrimidines were prepared in high yield from condensation of <em>N</em>-acridin-9-yl-3-oxo-butyramide with urea or thiourea or guanidine by microwave irradiation and by conventional heating for comparative study purpose. The representative compounds characterized on the basis of IR, <sup>1</sup>H NMR and Mass spectral beside elemental analysis. Microwave assisted synthesized compounds evaluated for

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28

Rajeev, Jain, Shrivastava Sadhana, and Bhadauria Akhilesh. "Synthesis of some pyrazole and pyrimidine derivatives of sulfonamides." Journal of India Chemical Society Vol 81, Aug 2004 (2004): 692–93. https://doi.org/10.5281/zenodo.5830189.

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School of Studies in Chemistry, Jiwaji University. Gwalior-474 011, India <em>E-mail</em>: gwlsosmica@sancharnet.in<em>       Fax </em>: 91-751-2346209 <em>Manuscript received 9 January' 2003, revised 12 January 2004 accepted 6 April 2004</em> 1- Carboxymethylpyridinium-3-aminophenyl-5-methyl-4-(4'-sustituted)sulfonamoy lazopyrazoles (2a-f) and 2-amino-4-methyl- 6-(4' -aminotoIudyl)-5-( 4'-sulfonamoyl)azopyrimidines (3a- f) were synthesized by condensation of 1-aminophenlyl-2-( 4'substituted) sulfonamoylhydrazonohutane-1 ,3-dione

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Mehta, Arvind G., and Avnish A. Patel. "Studies on NovelN4-[4,6-Diaryl-2-pyrimidinyl]-7-chloro-4-quinolinamine and their Microbicidal Efficacy." E-Journal of Chemistry 6, s1 (2009): S406—S412. http://dx.doi.org/10.1155/2009/301426.

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The required chalcones1a-hwere prepared by reaction of substituted acetophenone with different aryl aldehyde, which in turn treated with guanidine nitrate, yielded 4-(substituted phenyl)-6-(substituted phenyl)-2-pyrimidinamine2a-h. Novel pyrimidine quinoline clubbed molecules3a-hhave been prepared by reaction of2a-hwith 4,7-dichloroquinoline. All the compounds were characterized by elemental analysis and spectral studies. The newly synthesized compounds were evaluated for their antibacterial and antifungal activity.

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Panda, Krishna Chandra, Bera Venkata Varaha Ravi Kumar, Biswa Mohan Sahoo, Bimal Krishna Banik, and Abhishek Tiwari. "Microwave Irradiated Eco-friendly Synthesis of Pyrimidine Derivatives as Potential Antitubercular Agents." Asian Journal of Chemistry 34, no. 4 (2022): 907–11. http://dx.doi.org/10.14233/ajchem.2022.23644.

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The microwave irradiation method is applied for the efficient synthesis of pyrimidine derivatives. The synthetic protocol involves Knoevenagel condensation followed by Michael addition reaction and cyclization of equimolar quantities of aromatic aldehydes, ethyl cyanoacetate and guanidine in the presence of ethanolic NaOH solution to produce corresponding pyrimidine derivatives. The reaction mixture was allowed to reflux under microwave radiation at power level-2 for 7-12 min. The microwave heating technique offers a cleaner reaction with a shorter reaction time and improved product yield as c

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31

Reem. S. Najem. "Synthesis of some pyrimidine derivatives from-4- acetyl pyridine." Tikrit Journal of Pure Science 23, no. 3 (2018): 48–55. http://dx.doi.org/10.25130/tjps.v23i3.500.

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Chalcones compounds(1-4) were prepared from - 4 - acetyl pyridine with different aromatic aldehyde benzaldehyde in the presence of KOH solution . The compounds (1-4) were reacted with thiourea to give compounds (5-8), with guanidine to give compounds (9-12). and with urea to give the compounds (13-16), in the presence of KOH as abasic.  The prepared compounds were identified using melting point apparatus , F T. IR spectro photo meter and (1H-NMR) spectrometer for some compounds .

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32

Kalhapure, Vijay, Dhananjay Magar, Nishant Kothalkar, Tushar Khaladkar, and Abhijit Roychowdhury. "Synthesis of Substituted imidazo [1, 5-a] pyrimidine-2-(1H)-one Core Structure." Current Organic Synthesis 17, no. 1 (2020): 23–28. http://dx.doi.org/10.2174/1389200220666191122103445.

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Background and Objective: The objective of our work was to establish a facile and scalable synthesis of imidazopyridone for further use in medicinal chemistry applications. An easy synthesis of a core scaffold will enable the medicinal chemistry community to use imidazopyridone as a privileged scaffold in new chemical entity (NCE) synthesis. Materials and Methods: The synthesis was achieved from commercially available and cheap raw materials like amino acetonitrile hydrochloride or commercially available guanidine. Results: Simple transformation starting from amino acetonitrile hydrochloride l

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Dhanalakshmi, Pandi, and Sivakumar Shanmugam. "Convenient one-pot multicomponent strategy for the synthesis of 6-pyrrolylpyrimidines." RSC Adv. 4, no. 56 (2014): 29493–501. http://dx.doi.org/10.1039/c4ra02891k.

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An easy method to construct diheteroaryls from α-aroylidineketene dithioacetals 2 in a multicomponent fashion. The reaction proceeds with high chemo/regioselectivity to give 4-alkoxy-6-(4-aryl-1H-pyrrol-3-yl)pyrimidin-2-amines in high yields by reacting 2 with p-tolylsulfonyl)methyl isocyanide 3 (TosMIC), guanidine nitrate 5 and alcohol in the presence of NaH/THF via cycloaddition.

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Rammohan, Pal, K. Mandai Tapas, Samanta Swati, and K. Mallik Asok. "An efficient synthesis of E-2-amino-4-aryl-8-(arylmethylene)-5,6, 7,8- tetrahydrobenzo[d]pyrimidines and their lower analogues." Journal of Indian Chemical Society Vol. 87, Jun 2010 (2010): 711–15. https://doi.org/10.5281/zenodo.5790642.

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Department of Chemistry, Jadavpur University, Kolkata-700 032, India <em>E-mail :</em> mallikak52@yahoo.co.in <em>Manuscript received 4 November 2009, accepted 27 November 2009</em> Base-catalyscd cyclocondensation of α,α'-bis(arylmethylene)cyclohexanones with guanidine hydrochloride has been found to generate E-2-amino-4-aryl-8-(arylmethylene)-5,6,7,8-tetrahydrobenzo[d]pyrimidines in high yield, the structures or which have been established from their analytical and spectral data. The corresponding lower analogues, α,α'- bis(arylmethylcne)cyclopcntanones also w

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35

S., Kothari, Singhal M., Vijayvergia D., Vyas R., and L. Verma B. "Synthesis and biocidal activity of some new 2-amino-4,6-diarylsubstituted-pyrimidines." Journal of Indian Chemical Society Vol. 77, Jul 2000 (2000): 329–31. https://doi.org/10.5281/zenodo.5867166.

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Department of Chemistry, Faculty of Science, M. L. Sukhadia University, Udaipur-313 002, India <em>Manuscript received 17 November 1999, accepted 23 March 2000</em> The chalcones (3a-q), derived from 3,5-dibromo-4-hydroxyacetophenone (Ia), 3,5-dibromo-2-hydroxyacet!)phenone (1b), 3-bromo-5- chloro-/5-methyl-2-hydroxyacetophenones (1c,d) and 4-(4'-nitrophenoxy)acetophenone (1e) and prepared by Claisen-Schmidt condensation with different substituted aromatic aldehydes (2a-f) in presence of base, on treatment with guanidine nitrate in ethanol and base give new 2-amino-4,6-diaryl-sub

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36

Trachman, Robert J., and Adrian R. Ferré-D'Amaré. "An uncommon [K+(Mg2+)2] metal ion triad imparts stability and selectivity to the Guanidine-I riboswitch." RNA 27, no. 10 (2021): 1257–64. http://dx.doi.org/10.1261/rna.078824.121.

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The widespread ykkC-I riboswitch class exemplifies divergent riboswitch evolution. To analyze how natural selection has diversified its versatile RNA fold, we determined the X-ray crystal structure of the Burkholderia sp. TJI49 ykkC-I subtype-1 (Guanidine-I) riboswitch aptamer domain. Differing from the previously reported structures of orthologs from Dickeya dadantii and Sulfobacillus acidophilus, our Burkholderia structure reveals a chelated K+ ion adjacent to two Mg2+ ions in the guanidine-binding pocket. Thermal melting analysis shows that K+ chelation, which induces localized conformation

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SHAFI, S. SYED, P. SUBASHINI, S. GAJALAKSHMI, and V. VIJAYA KUMAR. "An Efficient Suitable Synthesis for Pyrazole, Pyrimidine Derivatives and Biological Evaluation." Asian Journal of Chemistry 33, no. 4 (2021): 734–40. http://dx.doi.org/10.14233/ajchem.2021.23095.

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Novel quinazoline derivatives were synthesized by reacting isatoic anhydride and 4-amino acetanilide to synthesize N-(4-(2,4-dioxo-1,2- dihydroquinazolin-3(4H)-yl)phenyl)acetamide which in turn reacted with substituted aromatic aldehydes to synthesize novel chalcones. The chalcones were allowed to react with hydrazine hydrochloride and guanidine to form pyrazoline and pyrimidine derivatives, respectively. The newly synthesized compounds were characterized by IR, NMR (1H, 13C), mass and elemental analysis. All the newly synthesized derivatives were screened for in vitro antimicrobial and antiox

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Ravindra, S. Dhivare, and S. Rajput Shankarsing. "Synthesis, physicochemical probe and antimicrobial assay of bis-chalcone, pyrazole, amino-pyrimidine and malononitrile derivatives from five and six membered cyclic imides." Iranian Journal of Organic Chemistry 8, no. 4 (2017): 1909–18. https://doi.org/10.5281/zenodo.3911281.

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<strong>Abstract </strong> Heterocyclic imides greatly involved in the development of organic synthesis. Coloured flavonoids like bis-chalcones are formed by microwave-assisted solvent-free route using phenyl succinimide, glutarimide, and vanillin. To achieve the <em><strong>pyrazole</strong></em> and <strong><em>amino-pyrimidine</em></strong> derivatives by the cyclization of bis-chalcone with hydrazine hydrate and guanidine nitrate via microwave method. Then <strong><em>dimalononitriles</em></strong> were produced by the active methylene group of dinitrile with cyclic imides. Hence the physi

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Khunt, Hasmukh R., Piyush P. Pipaliya, Satish M. Ghelani, Jayesh S. Babariya, and Yogesh T. Naliapara. "Synthesis and Characterization of Fully Substituted Pyrimidines by Using Ketene Dithioacetal as Potent Antimicrobial Agent." International Letters of Chemistry, Physics and Astronomy 24 (December 2013): 134–41. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.24.134.

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Various ketene dithioacetals of acetoacetanilides were reacted with guanidine nitrate in the presence of base to produce the 2-amino-4-isopropyl-6-alkoxy-N-arylpyrimidine-5-carboxamide derivatives with good yields. All the synthesized compounds were characterized by mass, NMR and IR and also evaluated for antimicrobial activity against five different bacterial and fungal strains. The compounds 4i, 4k and 4l has found comparatively good active against all the bacterial strains.

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Khunt, Hasmukh R., Piyush P. Pipaliya, Satish M. Ghelani, Jayesh S. Babariya, and Yogesh T. Naliapara. "Synthesis and Characterization of Fully Substituted Pyrimidines by Using Ketene Dithioacetal as Potent Antimicrobial Agent." International Letters of Chemistry, Physics and Astronomy 24 (December 26, 2013): 134–41. http://dx.doi.org/10.56431/p-z179r2.

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Various ketene dithioacetals of acetoacetanilides were reacted with guanidine nitrate in the presence of base to produce the 2-amino-4-isopropyl-6-alkoxy-N-arylpyrimidine-5-carboxamide derivatives with good yields. All the synthesized compounds were characterized by mass, NMR and IR and also evaluated for antimicrobial activity against five different bacterial and fungal strains. The compounds 4i, 4k and 4l has found comparatively good active against all the bacterial strains.

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41

Stoss, Peter, Elmar Kaes, Guenter Eibel, and Ulf Thewalt. "Novel pyrimidine and pyrimido[1,2-a]pyrimidine derivatives. By-products of a guanidine based thymine synthesis." Journal of Heterocyclic Chemistry 28, no. 2 (1991): 231–36. http://dx.doi.org/10.1002/jhet.5570280205.

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42

Jadhav, Madhav S., Anilkumar G. Jadhav, Prashant S. Kale, and Shivraj B. Sirsat. "Synthesis of Novel Oxo Pyrimido Pyrimidine and Their Derivatives." International Journal for Research in Applied Science and Engineering Technology 10, no. 8 (2022): 645–51. http://dx.doi.org/10.22214/ijraset.2022.46125.

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Abstract: Pyrimidine derivatives are synthesized to possess various pharmacological and biological activities. In the present work, we have synthesized 3-(4-methoxyphenyl)-1-phenyl prop-2-en-1-one (1) (chalcone) by using 4-methoxybenzaldehyde and acetophenone in the presence of alcoholic KOH by Claisen-Schmidt condensation reaction. After purification and characterization by physical and spectral methods, The synthesized chalcone have been converted into 6-(4-methoxyphenyl)-4- phenyl-1,6-dihydropyrimidin-2-amine (2) by treating with guanidine nitrate in the presence of alcoholic KOH. The struc

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43

Mandhadi, Jithendar R., Theivendren Panneerselvam, and Pavadai Parasuraman. "DESIGN, In silico Modeling, Toxicity study and Synthesis of Novel Substituted Semicarbazide Derivatives of Pyrimidine: An Antitubercular Agent." Current Bioactive Compounds 16, no. 3 (2020): 294–301. http://dx.doi.org/10.2174/1573407214666181001112601.

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Background: A series of 1-(2-(2-amino-5-carbamoyl-6-(1-(substitutedphenyl) prop-1-enyl) pyrimidin-4-yloxy)acetyl) semicarbazide (4a-i) derivatives was synthesized from substituted aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride and characterized by analytical and spectral data, FTIR, 1H-NMR and Mass spectroscopy data. Methods: The antiTB action of the synthesized compounds was screened in comparison with the standard drug Rifampicin using MABA assay method. The SAR of substituted aromatic aldehydes with modification at ortho, meta and para positions with electron withdrawing

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Santos, Mario F. C., Philip M. Harper, David E. Williams, et al. "Anti-parasitic Guanidine and Pyrimidine Alkaloids from the Marine SpongeMonanchora arbuscula." Journal of Natural Products 78, no. 5 (2015): 1101–12. http://dx.doi.org/10.1021/acs.jnatprod.5b00070.

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45

Liu, Mingxing, Jiarong Li, Shu Chen, et al. "One-pot NHC-assisted access to 2,3-dihydropyrimido[4,5-d]pyrimidin-4(1H)-ones." RSC Adv. 4, no. 67 (2014): 35629–34. http://dx.doi.org/10.1039/c4ra05346j.

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An efficient N-heterocyclic carbene-assisted one-pot reaction synthesis of 2,3-dihydropyrimido[4,5-d] pyrimidin-4(1H)-ones from 2-(ethoxymethylene)malononitrile, guanidines (or amidines) and ketones (or aldehyde) has been developed. The novel method provides a highly efficient synthesis of pyrimido[4,5-d]pyrimidinering from materials with no heterocyclic structures.

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46

Hana, A. A. Mageed, F. El Ezabi Reda, and A. Khaled Fayrouz. "In vitro antimicrobial activity screening of new Heterocyclic compounds derived from 5-bromo-2,3-di(furan-2-yl)-1h-indole." In vitro antimicrobial activity screening of new Heterocyclic compounds derived from 5-bromo-2,3-di(furan-2-yl)-1h-indole 3, no. 1 (2021): 889–93. https://doi.org/10.36811/jca.2021.110033.

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This article describes the antimicrobial activity evaluation of new heterocyclic compounds derived from 5-bromo-2,3-di(furan-2-yl)-1h-indole. Heterocyclic moiety serve as perfect framework on which pharmacophores can be effectively attached to produce novel drugs. New compounds were obtained on the basis of derivatives including 1H-indole-2,3-dione derivatives. Acid-catalyzed, three-component reaction (Belinelli synthesis) between 5-bromo-2,3-di(furan-2-yl)1H-indole, acetylacetone and semi carbazide, thiosemicarbazone, urea, thiourea, guanidine constitutes a rapid and facile synthesis of corre

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47

Aggarwal, Natasha N., B. C. Revanasiddappa, Banylla Felicity, Vijay Kumar, and Hemanth Kumar. "SYNTHESIS, IN SILICO ANALYSIS AND ANTICONVULSANT ACTIVITY OF NOVEL PYRIMIDINE DERIVATIVES." Indian Drugs 58, no. 05 (2021): 21–29. http://dx.doi.org/10.53879/id.58.05.12570.

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In this present study, a novel series of chalcones (C1-10) were synthesized by reacting 4-nitro acetophenone and various substituted aromatic aldehydes in an alcohol medium. The title compounds, pyrimidine derivatives (PD1-10), were obtained by the cyclization of chalcones (C1-10) with guanidine carbonate in an alcoholic medium. Each of the newly synthesized compounds was structurally assigned in accordance with FT-IR, 1 H-NMR and mass spectral data. All the synthesized compounds were subjected to in silico analysis among which, some of the synthesized compounds were chosen and evaluated for i

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STOSS, P., E. KAES, G. EIBEL, and U. THEWALT. "ChemInform Abstract: Novel Pyrimidine and Pyrimido(1,2-a)pyrimidine Derivatives. By- Products of a Guanidine- Based Thymine Synthesis." ChemInform 22, no. 31 (2010): no. http://dx.doi.org/10.1002/chin.199131199.

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Narule, Meghasham, Jyotsna Meshram, B. Santhakumari, and A. Shanware. "Synthesis of 2-[4-(10H-Substituted Phenothiazine-3-yl)-6-Pyrimidin-2-Phenylthiol/ol/amine/thiol] Pyrroles." E-Journal of Chemistry 4, no. 1 (2007): 53–59. http://dx.doi.org/10.1155/2007/572543.

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2-[4-Hydroxy benz-1(propene-1-one)]Pyrrole II on treatment with phenyl thiourea, guanidine carbonate, urea and thiourea in alcoholic KOH yielded compounds III, IV, V, VI which on treatment with different aryl anilines gave compounds VII, VIII, IX, X which under goes cyclisation with sulphur and iodine to give 2-[4-(10H-substituted phenothiazine-3-yl)-6-pyrimidin-2-phenylthiol/-ol/-amine/-thiol] pyrrole XI(a-j), XII(a-j), XIII(a-j) and XIV(a-j) respectively. The structural products were characterized by elemental analysis and spectral data.

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Chhatbar, Pratiksha, Kaushik Pambhar, Vijay Khedkar, Anamik Shah, and Ranjan Khunt. "In Silico (3D-QSAR) Designed, Study, Synthesis and Anti-tubercular Evaluation of Pyrazolo-Pyrimidine Derivatives." Anti-Infective Agents 18, no. 2 (2020): 135–43. http://dx.doi.org/10.2174/2211352517666190225143923.

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Background: A 3D-QSAR study based on CoMFA and CoMSIA was performed on these pyrazole-pyrimidine derivatives to correlate their chemical structures with the observed activity against M. tuberculosis. Objective: The current research aimed to synthesize and evaluateed pyrazole-pyrimidine based antitubercular agents by an in vitro microbial study based on our previously reported 3D-QSAR. Methods: The designed molecules were synthesised via chalcone intermediate and cyclisation using guanidine and urea. The molecules were then characterized by various spectroscopic methods like IR, MASS, 1H-NMR, 1

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