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Journal articles on the topic 'Amino-pyrimidines and Antimicrobial activity'

Author: Grafiati

Published: 4 June 2025

Last updated: 1 August 2025

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1

KHADIGA, M. GHONBIM, EL-TELBANY FARAG, and YOUSSEF KHAIRIA. "Synthesis and Evaluation of some 2-, 4- and 2,4- Di-substituted.-6-methylpyrimidine Derivatives for Antimicrobial Activity." Journal of Indian Chemical Society Vol. 63, Oct 1986 (1986): 914–17. https://doi.org/10.5281/zenodo.6302313.

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Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt <em>Manuscript received</em> <em>23 September 1986, accepted 2 August 1986</em> The reaction of 2-amino-4-cbloro-, 4-amino-2-chloro- and 2,4-dichloro-6-methylpyrimidines with primary aromatic amines under acidic conditions is presented. 2-, and 4-<sup>\(\omega\)</sup>-substituted-thioureido-6-methylpyrimidines were synthesised via the reaction of 2-amino-and 4-amino-6-metbylpyrimidine derivatives with arylisocyanates. Six compounds were evaluated for their antimicrobial activity and most of them sh

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2

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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3

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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4

Mohamed, Mosaad, Ramdan El-Domany, and Rania Abd El-Hameed. "Synthesis of certain pyrrole derivatives as antimicro-bial agents." Acta Pharmaceutica 59, no. 2 (2009): 145–58. http://dx.doi.org/10.2478/v10007-009-0016-9.

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Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds

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5

Hossain, M. I., and M. M. H. Bhuiyan. "Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives." Journal of Scientific Research 1, no. 2 (2009): 317–25. http://dx.doi.org/10.3329/jsr.v1i2.2299.

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Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6 dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitril

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6

Vaghasia, S. J., and V. H. Shah. "Microwave assisted synthesis and antimicrobial activity of some novel pyrimidine derivatives." Journal of the Serbian Chemical Society 72, no. 2 (2007): 109–17. http://dx.doi.org/10.2298/jsc0702109v.

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The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidi

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7

Butta, Ragavendra, Sowmya Donthamsetty V, Padmaja Adivireddy, and Padmavathi Venkatapuram. "Synthesis and Antimicrobial Activity of Azolyl Pyrimidines." Journal of Heterocyclic Chemistry 54, no. 1 (2016): 524–30. http://dx.doi.org/10.1002/jhet.2615.

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8

Mohamed, Mounir A. A., Adnan A. Bekhit, Omyma A. Abd Allah, et al. "Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety." RSC Advances 11, no. 5 (2021): 2905–16. http://dx.doi.org/10.1039/d0ra08189b.

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9

Yadav, Bodke, and S. Sangapure S. "Synthesis and biological activity of some benzofuro[3,2-d]pyrimidines." Journal of Indian Chemical Society Vol. 80, Mar 2003 (2003): 187–89. https://doi.org/10.5281/zenodo.5839259.

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Department of Studies and Research in Chemistry. Gulbarga University, Gulbarga-585 106, India <em>E-mail :</em> bodke___yd@rediffmail.com <em>Manuscript received 21 December 2001 .revised 18 April 2002, accepted 12 December 2002</em> The condensation of ethyl 3-amino-2-benzofuran carboxylate (1) with phenyl isocyanate gave 3-phenylureido-2-benzofuran carboxylate (2), which upon treatment with phosphorus oxychloride gave 2-chloro-3-phenyl-3,4-dihydro-4-oxohenzofnro[3,2-<em>d</em>]pyrimidine (4). The reaction of 4 with alicyclic amines like piperidine and morpholine yielded 2-piperidino/mor

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10

Gomha, Sobhi, Ikhlass Abbas, Mohamed Elneairy, Mahmoud Elaasser, and Bazada Mabrouk. "Antimicrobial and anticancer evaluation of a novel synthetic tetracyclic system obtained by Dimroth rearrangement." Journal of the Serbian Chemical Society 80, no. 10 (2015): 1251–64. http://dx.doi.org/10.2298/jsc141222022g.

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A series of pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidines were prepared via oxidative cyclization of 4-(2-arylidenehydrazinyl)pyrido [3',2':4,5]thieno[3,2-d] pyrimidines. Dimroth rearrangement of such a series yielded pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidines. The reaction mechanism was proposed and the products were screened for their antimicrobial and anticancer activities. From the antimicrobial screening results, it can be seen that compounds 8c, 9f and 10c showed excellent activity against gram positive bacteria while compounds 10d and 8c showed the

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11

Greco, Chiara, Rosa Catania, Dario Leonardo Balacco, et al. "Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors." Molecules 25, no. 22 (2020): 5354. http://dx.doi.org/10.3390/molecules25225354.

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Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results repre

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12

I.H. El-Qaliei, Mohamed, Sayed A.S. Mousa, Esam A. Ishak, Hamdi M.D. Nasr, Modather F Hussein, and Abdallah M.A. Hassane. "Synthesis, characterization, antimicrobial, antioxidant activities, and in silico study of new azo disperse dyes containing pyrazole and pyrazolo[1,5-a]pyrimidine rings." Bulletin of the Chemical Society of Ethiopia 39, no. 7 (2025): 1411–24. https://doi.org/10.4314/bcse.v39i7.13.

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New N,N-dimethyl-N'-(5-oxo-4-(aryldiazenyl)-2,5-dihydro-1H-pyrazol-3-yl)formimidamide 5a-c are formed by reaction of 5-amino-1H-pyrazol-3(2H)-one derivatives 4a-c with N,N-dimethylformamide dimethyl acetal (DMF-DMA). Compounds 5a-c serve as excellent precursors for the synthesis of new disazo pyrazole disperse dyes, When refluxed with hydrazine hydrate or active methylene reagents 8a,b, leading to N''-(3-hydroxy-4-(arylaza)-1H-pyrazol-5-yl)formimidohydrazide 7a-c or pyrazolo[1,5-a]. pyrimidines 11a–e. In vitro studies were carried out to evaluate antioxidant properties of the produced compound

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13

Zhylko, Vasyl, Lesya Saliyeva, Nataliia Slyvka, et al. "Synthesis, Antimicrobial and Antioxidant Activity of 3-Aryl-6,7-Dihydro-5H-[1,3]Thiazolo[3,2-a]Pyrimidines." Chemistry & Chemical Technology 19, no. 2 (2025): 250–58. https://doi.org/10.23939/chcht19.02.250.

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A series of 3-aryl-6,7-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidines was obtained by cyclocondensation of tetrahydropyrimidin-2(1H)-one with 2-bromo-1-arylethanones. It was established that the nature of the substituent in the aromatic nucleus of phenacyl bromide significantly affects the course of this type of reaction. In particular, in the case of 2-bromo-1-(4-hydroxyphenyl)ethanone, the target bicyclic product is formed as a result of boiling in ethanol for 4 hours, whereas the reaction time for the cyclocondensation of tetrahydropyrimidine-2(1H)-thione with other bromomethylaryl ketones was

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14

Osipov, A. O., P. P. Purygin, A. V. Dubishchev, and A. A. Osipova. "PHARMACOLOGICAL ACTIVITY OF A PYRIMIDINE DERIVATIVES." Vestnik of Samara University. Natural Science Series 17, no. 8 (2017): 167–72. http://dx.doi.org/10.18287/2541-7525-2011-17-8-167-172.

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The main directions of the search of biologically active compounds, pyrimi-dine derivatives are described.The synthesis of pyrimidines with anticancer, antimicrobial, antiviral activity is shown as the most frequent in recent years. The examples of compounds are given, which are already being used in medicine practice or may be good starting points for obtaining new drugs.

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15

J., R. DESAI, R. PARIKH A., and A. CHAUHAN N. "Thieno[3,2-d]pyrimidines. Part-I. Preparation and Antimicrobial Activity of 3-N-Substituted-thioureido-2-methyl-6-phenylthieno[3,2-d]pyrimidin-4(3H)-ones." Journal of Indian Chemical Society Vol. 74, Feb 1997 (1997): 160. https://doi.org/10.5281/zenodo.5876092.

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Department of Chemistry. Saurashtra Universitty, Rajlot-360 005 <em>Manuscript received 21 December 1994. revised 5 July 1995, accepted 26 July 1995</em> Thieno[3,2-<em>d</em>]pyrimidines. Part-I. Preparation and Antimicrobial Activity of 3-<em>N</em>-Substituted-thioureido-2-methyl-6-phenylthieno[3,2-<em>d</em>]pyrimidin-4(3<em>H</em>)-ones.

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16

Bergh, J. J., J. C. Breytenbach, and S. Van Dyk. "In vitro antimikrobiese aktiwiteit en in vitro-toksisiteit van die afbraakprodukte van trimetoprim." Suid-Afrikaanse Tydskrif vir Natuurwetenskap en Tegnologie 10, no. 4 (1991): 153–54. http://dx.doi.org/10.4102/satnt.v10i4.505.

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The in vitro antimicrobial activity and in vitro toxicity of five pyrimidines, degradation products of trimethoprim, was determined. These compounds, formed on hydrolysis or oxidation of the drug, are mostly biologically inactive. With the exception of the ketone, which is active against only one of the micro organisms used in the test, all other compounds are devoid of antimicrobial activity and none possesses acute toxicity or phototoxicity.

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17

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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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 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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19

Naglah, Ahmed M., Ahmed A. Askar, Ashraf S. Hassan, Tamer K. Khatab, Mohamed A. Al-Omar, and Mashooq A. Bhat. "Biological Evaluation and Molecular Docking with In Silico Physicochemical, Pharmacokinetic and Toxicity Prediction of Pyrazolo[1,5-a]pyrimidines." Molecules 25, no. 6 (2020): 1431. http://dx.doi.org/10.3390/molecules25061431.

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Pyrazolo[1,5-a]pyrimidines 5a–c, 9a–c and 13a–i were synthesized for evaluation of their in vitro antimicrobial properties against some microorganisms and their immunomodulatory activity. The biological activities of pyrazolo[1,5-a]pyrimidines showed that the pyrazolo[1,5-a]pyrimidines (5c, 9a, 9c, 13a, 13c, 13d, 13e and 13h) displayed promising antimicrobial and immunomodulatory activities. Studying the in silico predicted physicochemical, pharmacokinetic, ADMET and drug-likeness properties for the pyrazolo[1,5-a]pyrimidines 5a–c, 9a–c and 13a–i confirmed that most of the compounds (i) were w

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Hafez, Hend N., Abdulrahman G. Alshammari, and Abdel-Rhman B. A. El-Gazzar. "Facile heterocyclic synthesis and antimicrobial activity of polysubstituted and condensed pyrazolopyranopyrimidine and pyrazolopyranotriazine derivatives." Acta Pharmaceutica 65, no. 4 (2015): 399–412. http://dx.doi.org/10.1515/acph-2015-0037.

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Abstract Reaction of 6-amino-3-methyl-4-(substituted phenyl)-1,4- dihydropyrano[2,3-c]pyrazole-5-carbonitrile (1) with triethylorthoformate followed by treatment with hydrazine hydrate, formic acid, acetic acid, phenylisocyanate, ammonium thiocyanate and formamide afforded the corresponding pyranopyrimidine derivatives 2-6. Cyclocondensation of 1 with cyclohexanone afforded pyrazolopyranoquinoline 7. One-pot process of diazotation and de-diazochlorination of 1 afforded pyrazolopyranotriazine derivative 8, which upon treatment with secondary amines afforded 9 and 10a- c. Condensation of 2 with

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21

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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22

Imran, M., and SA Khan. "Synthesis and Antimicrobial Activity of Some 2-Amino-4-(7- Substituted/Unsubstituted Coumarin-3-yl)-6-(Chlorosubstitutedphenyl) Pyrimidines." Tropical Journal of Pharmaceutical Research 14, no. 7 (2015): 1265. http://dx.doi.org/10.4314/tjpr.v14i7.20.

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Abu-Hashem, Ameen Ali, and Sami A. Al-Hussain. "The Synthesis, Antimicrobial Activity, and Molecular Docking of New 1, 2, 4-Triazole, 1, 2, 4-Triazepine, Quinoline, and Pyrimidine Scaffolds Condensed to Naturally Occurring Furochromones." Pharmaceuticals 15, no. 10 (2022): 1232. http://dx.doi.org/10.3390/ph15101232.

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This study aims to synthesize a new series of furochromone derivatives, evaluate their antimicrobial properties, and improve the permeability of potent compounds to inhibit different types of bacteria and fungi. Hence, Substituted furo[3,2-g]chromene-6-carbonitrile (3a,b) readily form 7-amino-5-methyl-furo [3,2-g]chromene-6-carbonitrile (4a,b) via reduction using sodium borohydride in methanol. The same compounds of (4a,b) were used as starting materials for the synthesis of new furochromone derivatives such as furochromeno [2,3-d]pyrimidines, N- (6-cyano- 5-methyl-furochromene) acetamide, N-(

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Sedaghati, Bita, Afshin Fassihi, Shirin Arbabi, et al. "Synthesis and antimicrobial activity of novel derivatives of Biginelli pyrimidines." Medicinal Chemistry Research 21, no. 12 (2011): 3973–83. http://dx.doi.org/10.1007/s00044-011-9931-7.

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Kayathi, Narendra Babu, Donthamsetty V. Sowmya, Padmaja Adivireddy, and Padmavathi Venkatapuram. "Synthesis of Benzazolyl Pyrimidines Under Ultrasonication and Their Antimicrobial Activity." Journal of Heterocyclic Chemistry 55, no. 4 (2018): 1024–32. http://dx.doi.org/10.1002/jhet.3134.

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Borysiuk, Olha, Vasyl Zhylko, Lesya Saliyeva, et al. "Synthesis and biological activity of 2-arylidene-5,6-dihydroimidazo[2,1-b]thiazoles and 6,7-dihydro-5h-[1,3]thiazolo[3,2-a]pyrimidines." ScienceRise: Pharmaceutical Science, no. 2 (54) (April 30, 2025): 22–28. https://doi.org/10.15587/2519-4852.2025.326521.

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The aim. The present study is devoted to searching for potential biologically active agents among functionalized imidazo[2,1-b]thiazoles and thiazolo[3,2-a]pyrimidines. Materials and methods. The interaction of preparatively available 5,6-dihydroimidazo[2,1-b]thiazolone and 6,7-dihydro-2H-thiazolo[3,2-a]pyrimidinone with several substituted benzaldehydes in boiling acetic acid in the presence of anhydrous sodium acetate leads to new 2-arylidene-substituted 5,6-dihydroimidazo[2,1-b]thiazoles and 6,7-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidines as potential pharmacological agents. Their antimicrob

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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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Rizak, Galina. "SEARCH FOR BİOLOGİCALLY ACTİVE SUBSTANCES USİNG THE EXAMPLE OF 2.4-DIOXO- AND 4-IMINO-2-OXO- 3-PHENYL-5-R-6-R`-THIENO[2.3-D]PYRIMIDINES, ROSPECTS FOR THEİR USE İN PHARMACY AND MEDİCİNE." Azerbaijan Pharmaceutical and Pharmacoterapy Journal 23, no. 1 (2023): 29–46. http://dx.doi.org/10.58495/bucc4973.

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The purpose of this paper was the development of new bioactive substances – derivatives of 2.4-dioxo- and 4-imino-2-oxo-3-phenyl-5-R-6-R`-thieno[2.3-d]pyrimidines; researching the structure of invented substances and conducting their pharmacological analysis. Such research methods were used as synthesis of ethyl 4-R-5-R`-2-aminothiophene-3-carboxylates, nitriles of 4- R-5-R`-2-aminothiophene-3-carboxylic acids, their ureide derivatives 2.4-dioxo- and 4-imino-2- oxo-3-phenyl-5-R-6-R`-thieno[2.3-d]pyrimidines, their alkyl, acyl and cyanoethyl derivatives and products of their chemical transforma

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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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SABIU, RABILU ABDULLAHI, MUHD SHAFI'I ABUBAKAR, RAGHAV SAPNA, and ABDULMUMIN MUHAMMAD MA'ARUF. "Pyrimidine derivatives: Recent discoveries and development towards its medicinal impact." GSC Biological and Pharmaceutical Sciences 20, no. 1 (2024): 114–28. https://doi.org/10.5281/zenodo.13640628.

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Pyrimidine derivatives' many biological functions and possible therapeutic uses have attracted a lot of research in the field of medicinal chemistry. Recent developments in the synthesis, biological assessment, and therapeutic uses of molecules based on pyrimidines are highlighted in this review. The significance of pyrimidine derivatives in treating a range of ailments, including cancer, infectious diseases, and metabolic disorders, is discussed, along with innovative synthesis approaches and important pharmacological findings. In order to give a thorough picture of the present status of pyri

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K, Ishwar Bhat, and Abhishek Kumar. "PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS." Asian Journal of Pharmaceutical and Clinical Research 10, no. 6 (2017): 237. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17343.

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Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted al

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Sowmya, P. T., A. S. Paniraj, K. M. Lokanatha Rai, and Anitha Sudhir. "Synthesis and biological activity of some new podophyllotoxin bearing pyrimidine moiety." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 03 (2024): 267. http://dx.doi.org/10.59467/ijhc.2024.34.267.

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Podophyllotoxin (PPT), a naturally occurring aryltetralin-type lignan obtained from Podophyllin, an ethanolic extract of Podophyllum peltatum L. (syn. P. hexandnum Royle), exhibits marked biological activity as strong antineoplastic drugs and antiviral agents. Chemical transformations performed on PPT resulted in analogs which also display potent cytotoxic, antiviral, and immunosuppressive activities. In the present research, ten new compounds of PPTs 2a-l bearing pyrimidine moiety were synthesized by the reaction of PPT (1) with 2-methyl sulphonyl pyrimidines in the presence of tetrahydrofura

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Lakes, Jourdan E., Brittany E. Davis, and Michael D. Flythe. "Activity of Cannabidiol on Ex Vivo Amino Acid Fermentation by Bovine Rumen Microbiota." Fermentation 10, no. 6 (2024): 267. http://dx.doi.org/10.3390/fermentation10060267.

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Amino-acid-fermenting bacteria are wasteful organisms within the rumens of beef cattle that remove dietary amino nitrogen by producing ammonia, which is then excreted renally. There are currently no on-label uses for the control of this microbial guild, but off-label use of broad-spectrum antimicrobials has shown efficacy, which contributes to antimicrobial resistance. Plant-derived antimicrobials supplemented into the diets of cattle may offer worthwhile alternatives. This study sought to investigate the role of cannabidiol (CBD) as a terpenophenolic antimicrobial. Ex vivo cell suspensions we

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A., V. Dobaria, R. Patel J., and H. Parekh H. "Synthesis and antimicrobial screening of cyanopyridines." Journal of Indian Chemical Society Vol. 79, Sep 2002 (2002): 772–73. https://doi.org/10.5281/zenodo.5844555.

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Department of Chemistry, Saurashtra University, Rajkot-360 005, India <em>Fax : </em>91-0281-78512 <em>Manuscript received 3 May 2001, revised 5 November 2001, accepted 11 April 2002</em> 2-Amino-3-cyano-4-(2'-chloro-7'-methylquinolin-3'-y1)-6-arylpyridines (3a-n) have been synthesized by the condensation of chalcones (2a-n) with malononitrile and ammonium acetate. All the compounds have been screened for their antimicrobial activity.

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35

M. Madawali, Indira, Navanath V. Kalyane, Gaviraj E. N, and Shivakumar B. "Synthesis and Antimicrobial activity of some new Pyrimidines of 6-chlorobenzimidazoles." Oriental Journal of Chemistry 34, no. 3 (2018): 1633–37. http://dx.doi.org/10.13005/ojc/340358.

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Naresh, Kondapally. "Synthesis and antimicrobial activity of some new Thieno[2,3-d]pyrimidines." International Journal of Pharmacy Education and Research 1, no. 1 (2014): 49–52. http://dx.doi.org/10.17812/ijper/2014;1(1):49-52.

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Verma, Mohan, and Prabhakar Kumar Verma. "Synthesis, characterization, antimicrobial and anticancer evaluation of pyrimidines Clubbed with thiazolidinone." Journal of medical pharmaceutical and allied sciences 11, no. 2 (2022): 4582–87. http://dx.doi.org/10.55522/jmpas.v11i2.2527.

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A series of novel derivatives of pyrimidine clubbed with thiazolidinone was synthesized in good yield and characterized by physiochemical and spectral means. All the synthesized derivatives were evaluated for their antimicrobial and anticancer activity. Antimicrobial properties of the title compounds were investigated against Gram positive (Bacillus subtilis and Staphylococcus aureus) and Gram negative bacterial (Escherichia coli) as well fungal strains (Candida albicans and Aspergillus niger). The anticancer evaluation of synthesized compounds against HeLa Cervical cancer cell Line indicated

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Amatur, Roquia, and tam Tilak. "Design and Synthesis of Novel Chromeno Pyrimidine analogs of potential Antimicrobial properties." International Journal of Applied Sciences and Management 1, no. 2 (2016): 105–16. https://doi.org/10.5281/zenodo.5172238.

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The aim of the study is to design and synthesize the new bioactive heterocyclic compounds. Pyrimidine is an important class of heterocyclic compound that are known to possess important pharmacological and antimicrobial properties. 2H-chromenes are also known to possess antimicrobial properties. Chromeno pyrimidines are compounds having both pyrimidines and 2H-chromenes in their structures. Hence, the synthesis of novel chromeno pyrimidine containing chloro, fluoro, trifluoromethyl groups have been carried out by multi-step organic synthesis, in order to study their interesting antimicrobial pr

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Osolоdchenko, T., I. Andreieva, N. Zavada, I. Ryabova, and A. Volyansky. "Spectrum and levels of antimicrobial activity of modified amino acids." Annals of Mechnikov Institute, no. 4 (December 12, 2019): 62–65. https://doi.org/10.5281/zenodo.3572576.

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<strong>Introduction</strong><strong>. </strong>Antimicrobial resistance  threatens the effective prevention and treatment of an ever-increasing range of infections and  is rising to dangerously high levels in all parts of the world. The search among the natural and synthetic biologically active compounds that influence the development of resistance in against antibacterial agents in the clinically relevant strains acquires increasingly greater significance. <strong>Material & methods</strong><strong>. </strong>Were studied the spectrum and levels of antimicrobial activity of 10

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Osolоdchenko, T. P., I. D. Andreieva, M. A. Komisarenko, I. S. Ryabova, and N. P. Zavada. "Results of primary microbiological screening of modified quercetin derivatives." Annals of Mechnikov Institute, no. 4 (December 6, 2021): 21–26. https://doi.org/10.5281/zenodo.5761159.

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<strong>Introduction. </strong>The development of new effective and low-toxic drugs based on herbal raw materials is an urgent task of modern science. Quercetin is one of the most well-known and well-studied flavonoids. Attempts to enhance the medicinal properties of quercetin by its chemical modifications are promising. The aim of the work is to search for modified quercetin derivatives with high antimicrobial properties by their primary microbiological screening. <strong>Materials & methods. </strong>Primary microbiological screening of antimicrobial activity of 315 quercetin derivatives

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Osolоdchenko, T. P., I. D. Andreieva, S. V. Ponomarenko, et al. "PRIMARY MICROBIOLOGICAL SCREENING OF AMINO ACIDS AND THEIR MODIFIED VARIANTS." Annals of Mechnikov Institute, no. 1 (April 14, 2019): 40–46. https://doi.org/10.5281/zenodo.2639502.

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<strong>Introduction</strong><strong>.  </strong>The Fight against infectious diseases is still the most relevant problem in medicine [1]. Antimicrobial chemical agents have the leading role in prophylaxis and treatment of diseases of microbial genesis [2]. The main negative consequence of antibiotic therapy is the progressive resistance of the microorganisms [3-5]. With increasing frequency, the specialists turn to the natural treatment approaches, especially towards plants that possess antibacterial activity and towards the compounds that compose the biological structure of the organism

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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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Patel, Sanjay K. S., Jung-Hoe Kim, Vipin C. Kalia, and Jung-Kul Lee. "Antimicrobial Activity of Amino-Derivatized Cationic Polysaccharides." Indian Journal of Microbiology 59, no. 1 (2018): 96–99. http://dx.doi.org/10.1007/s12088-018-0764-7.

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45

Takada, Mayu, Takahito Ito, Megumi Kurashima, Natsumi Matsunaga, Yosuke Demizu, and Takashi Misawa. "Structure–Activity Relationship Studies of Substitutions of Cationic Amino Acid Residues on Antimicrobial Peptides." Antibiotics 12, no. 1 (2022): 19. http://dx.doi.org/10.3390/antibiotics12010019.

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Antimicrobial peptides (AMPs) have received considerable attention as next-generation drugs for infectious diseases. Amphipathicity and the formation of a stabilized secondary structure are required to exert their antimicrobial activity by insertion into the microbial membrane, resulting in lysis of the bacteria. We previously reported the development of a novel antimicrobial peptide, 17KKV, based on the Magainin 2 sequence. The peptide was obtained by increasing the amphipathicity due to the replacement of amino acid residues. Moreover, we studied the structural development of 17KKV and revea

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Liu, Bin, and Eric Wilson. "Dissecting the antimicrobial activity of CCL28 through protein mutagenesis (98.9)." Journal of Immunology 182, no. 1_Supplement (2009): 98.9. http://dx.doi.org/10.4049/jimmunol.182.supp.98.9.

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Abstract Some chemokines have been shown act as antimicrobial proteins in vitro, suggesting that they may contribute directly to innate immune protection. Based on the study of defensins and other antimicrobial peptides (AMPs), it has been proposed that the characteristics of cationicity, hydrophobicity and amphipathicity of the AMPs determine the killing activity of these peptides. However, amino acid characteristics necessary for the antimicrobial activity of chemokines have not been elucidated. Using mouse CCL28 we have determined the primary sequence features required for antimicrobial act

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Anjani, Solankee, and Tailor Riki. "An efficient synthesis of some new chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus as potential antimicrobial and antitubercular agent." Chemistry International 2, no. 4 (2016): 189–200. https://doi.org/10.5281/zenodo.1471239.

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In an attempt to find a new class of antimicrobial and antitubercular agent, a new series of chalcone, acetyl pyrazoline and amino pyrimidine bearing 1,3,5- triazine nucleus were synthesized with appropriate chemical reagent. Chalcones (D1-D5) were synthesized by the classical Claisen-Schmidt condensation of substituted ketone (C) with variously substituted aldehydes via conventional method. Now treatment of chalcones with hydrazine hydrate/glacial acetic acid and guanidine hydrochloride/Alkali afforded the corresponding acetyl pyrazoline (E1-E5) and amino pyrimidine (F1-F5) derivatives respec

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48

Abdel-Gawad, Soad M., M. M. Ghorab, A. M. Sh El-Sharief, F. A. El-Telbany, and M. Abdel-Alla. "Design, synthesis, and antimicrobial activity of some new pyrazolo[3,4-d]pyrimidines." Heteroatom Chemistry 14, no. 6 (2003): 530–34. http://dx.doi.org/10.1002/hc.10187.

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49

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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50

RENUKA, JAIN, and SHIPRA. "Synthesis, Spectral Studies and Antimicrobial Activity of some Fluorinecontaining 2-Amino-4-arylthiazoles." Journal of Indian Chemical Society Vol. 74, Jan 1997 (1997): 54–55. https://doi.org/10.5281/zenodo.5877755.

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Department of Chemistry. University of Rajasthan, Jaipur-302 004 <em>Manuscript </em><em>received 13 August 1993, revised 22 February 1995, accepted 15 June 1995</em> Synthesis, Spectral Studies and Antimicrobial Activity of some Fluorinecontaining 2-Amino-4-arylthiazoles

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