Relevant bibliographies by topics / 4-dihydropyrimidines

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  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic '4-dihydropyrimidines'

Author: Grafiati
Published: 4 June 2021
Last updated: 11 February 2022

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Journal articles on the topic "4-dihydropyrimidines"

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C. Heda, L. C., Rashmi Sharma, C. Pareek, and P. B. Chaudhari. "Synthesis and Antimicrobial Activity of Some Derivatives of 5-Substituted Indole Dihydropyrimidines." E-Journal of Chemistry 6, no. 3 (2009): 770–74. http://dx.doi.org/10.1155/2009/893812.

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P. Biginelli reported the synthesis of functionalized 3, 4 dihydropyrimidine-2 (1H)-ones via three component condensation of an aromatic aldehyde, urea and ethylacetoacetate. This multicomponent reaction is of much importance due to excellent pharmacological properties of dihydropyrimidines. In this account, we synthesized some halo substituted indole dihydropyrimidines and evaluated their antimicrobial activity. The minimum inhibitory concentration (MIC) was determined by micro dilution technique in Mueller-Hinton broth. The MICs were recorded after 24 hours of incubation at 37 °C. These results are promising, showing these compounds are biologically active.
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Cho, Hidetsura, Yoshio Nishimura, Yoshizumi Yasui, Satoshi Kobayashi, Shin-ichiro Yoshida, Eunsang Kwon, and Masahiko Yamaguchi. "Synthesis of 4-unsubstituted dihydropyrimidines. Nucleophilic substitution at position-2 of dihydropyrimidines." Tetrahedron 67, no. 14 (April 2011): 2661–69. http://dx.doi.org/10.1016/j.tet.2011.01.092.

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Vedernikova, Irina V., Achiel Haemers, and Yuryi I. Ryabukhin. "Synthesis of 4-oxopyrimidinium and 4-oxo-1,4-dihydropyrimidines." Journal of Heterocyclic Chemistry 36, no. 1 (January 1999): 97–104. http://dx.doi.org/10.1002/jhet.5570360115.

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Povstyanoy, V. M., T. A. Yuyrova, A. N. Retchitskiy, and A. A. Krysko. "ALTERNATIVE METHODS OF SYNTHESIS OF NOVEL HETEROSYNTHONES – FUNCTIONALIZED HYPOXANTHINE PYRIMIDINES." Odesa National University Herald. Chemistry 26, no. 2(78) (July 31, 2021): 32–39. http://dx.doi.org/10.18524/2304-0947.2021.2(78).233823.

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It has been known that derivatives of dihydropyrimidine and xanthine possess the physiological activity of the wide spectrum of action. The combination of the specified heterocyclic fragments within one molecule can lead to the increase of its known types of biological activity as well as to the discovery of novel types of activity. We have previously reported the synthesis of intermediates, which consist of functionalized dihydropyrimidines, connected via a methylene bridge with the halogen substituted derivatives of the ophylline, 3-methylxanthine and imidazole. It was also observed that these compounds would react with N‑nucleophiles with the formation of various branched and cyclic products. The aim of this work was to determine the optimal conditions for obtaining heterocyclic products as a result of conjugation of bromomethyldihydropyrimidine and hypoxanthine at the positions C6 and C1 via a methylene bridge. It is important to note, that the latter can be widely modified by using structurally diverse aromatic aldehydes during the synthesis of dihydropyrimidine core by using Biginelli reaction, which explains structural diversity of the reaction products. After having tried various reaction conditions, we have concluded that the optimal method for obtaining the products entailed keeping equimolar ratios of bromomethyl substituted dihydropyrimidines and 1-potassium‑2-chloro‑7-methylhypoxanthine in dry ethanol for 4 hours. The ester group at the C5 of dihydropyrimidine ring and a chlorine leaving group at C2 of hypoxanthine fragments of the molecule allow to consider these structures as pro missing synthons for farther synthesis of condensed pyrimidine and xanthine systems. The structures of novel compounds have been confirmed with the methods such as HPLC/MS, 1H, and 13C NMR spectroscopy.
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Cho, Hidetsura, Yoshio Nishimura, Yoshizumi Yasui, Satoshi Kobayashi, Shin-ichiro Yoshida, Eunsang Kwon, and Masahiko Yamaguchi. "ChemInform Abstract: Synthesis of 4-Unsubstituted Dihydropyrimidines. Nucleophilic Substitution at Position-2 of Dihydropyrimidines." ChemInform 42, no. 33 (July 22, 2011): no. http://dx.doi.org/10.1002/chin.201133157.

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Lin, Yun, Jin-Tao Liu, and Xian-Jin Yang. "One-pot Synthesis of 4-Trifluoromethyl-1,2-dihydropyrimidines." Chinese Journal of Chemistry 25, no. 1 (January 2007): 113–15. http://dx.doi.org/10.1002/cjoc.200790003.

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Vedernikova, Irina V., Achiel Haemers, and Yuryi I. Ryabukhin. "ChemInform Abstract: Synthesis of 4-Oxopyrimidinium and 4-Oxo-1,4-dihydropyrimidines." ChemInform 30, no. 32 (June 14, 2010): no. http://dx.doi.org/10.1002/chin.199932155.

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Khan, M. Wahab, and Nitya G. Kundu. "An Expeditious Synthesis of 4-Acyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidines (6-acyl uracils) and 4-Acyl-6-aryl-2-oxo-2,3-dihydropyrimidines." Journal of Chemical Research 23, no. 1 (January 1999): 20–21. http://dx.doi.org/10.1177/174751989902300116.

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A facile synthesis of 4-acyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidines (6-acyl uracils) and 4-acyl-6-aryl-2-oxo-2,3-dihydropyrimidines is described where the Friedel–Crafts reaction on 2,6-dichloropyrimidine-4-carbonyl chloride plays a crucial role.
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Mehrabi, Hossein, Tayebeh Yarahmadi, and Farzaneh Alizadeh Bami. "Synthesis of 4-aryl-2-Thioxo-3,4-Dihydropyrimidines Using a Three-Component Reaction of Meldrum's Acid with Arylaldehydes and Acetylthiourea." Journal of Chemical Research 42, no. 6 (June 2018): 326–28. http://dx.doi.org/10.3184/174751918x15293155829494.

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A one-pot method for the preparation of new 4-aryl-2-thioxo-3,4-dihydropyrimidines via a three-component reaction of Meldrum's acid with arylaldehydes and acetylthiourea in the presence of p-toluenesulfonic acid as catalyst in CH3CN under reflux is reported.
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Yavari, Issa, Asiyeh Amirahmadi, and Mohammad Halvagar. "A Synthesis of Functionalized Thiazoles and Pyrimidine-4(3H)-thiones from 1,1,3,3-Tetramethylguanidine, Acetylenic Esters, and Aryl Isothiocyanates." Synlett 28, no. 19 (August 25, 2017): 2629–32. http://dx.doi.org/10.1055/s-0036-1590862.

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Aryl isothiocyanates react with dialkyl 2-{[bis(dimethylamino)methylene]amino}maleates, generated from 1,1,3,3-tetramethylguanidine and acetylenic esters, to afford 2-(dimethylamino)-1,3-thiazole derivatives, functionalized 2-(dimethylamino)-6-thioxo-1,6-dihydropyrimidines, and ethyl 2-(dimethylamino)-6-[(4-nitrophenyl)im­ino]-4-phenyl-6H-1,3-thiazine-5-carboxylate, in moderate to good yields.
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Dissertations / Theses on the topic "4-dihydropyrimidines"

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Sullivan, Shannon M. "Synthesis of 2,4-disubstituted pyrimidine derivatives as potential 5-HT7 receptor antagonist." unrestricted, 2008. http://etd.gsu.edu/theses/available/etd-05052008-153400/.

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Thesis (M.S.)--Georgia State University, 2008.
Title from file title page. Lucjan Strekowski, committee chair; A.L. Baumstark, Gabor Patonay, Doyle Barrow , committee members. Electronic text (68 p. : ill.) : digital, PDF file. Description based on contents viewed June 23, 2008. Includes bibliographical references (p. 42-430.
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Govender, Reshme. "Pharmacological Screening of Substituted 1, 4 Dihydropyrimidines." Thesis, 2016. http://hdl.handle.net/10321/1712.

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Submitted in partial fulfillment for the Degree of Master of Applied Sciences in Biotechnology, Durban University of Technology, Durban, South Africa, 2016.
Pharmacological research is essential for the advancement of treatment therapies to combat diseases that plague mankind. Pyrimidines have been a subject under investigation by medicinal chemists for many years due to their interesting pharmacological properties. In previous studies, pyrimidines and their derivatives have been reported to have antimicrobial, anti-inflammatory, antimalarial, analgesic, and antitumour activities amongst other biological activities. Although there has been a significant amount of research carried out on these heterocycles, there will always be a continuous need for the discovery of novel synthetic drugs which have a higher degree of potency and fewer side effects. Hence, this study was undertaken to determine the pharmacological activities of eight novel 1, 4 dihydropyrimidine analogues (DHPM 1 – 8), that have been synthesized in our laboratory. The dihydropyrimidines were synthesized and characterized and thereafter evaluated for in vitro antimicrobial, antioxidant, anti-inflammatory, cytotoxicity and apoptotic activities. The compounds also underwent a safety study. Antimicrobial activity was evaluated using the disk diffusion assay; compounds displaying superior activity were subjected to further analysis to establish the minimum inhibitory concentration. Overall compounds DHPM 7 and 8 showed the best antibacterial activity against Gram positive bacteria. The minimum inhibitory concentration (MIC) for DHPM 7 against the Gram positive organisms (B.cereus, S.aureus and B.coagulans) was 0.75 µg/mL; however DHPM 7 had a MIC of 0.37 µg/mL against M. luteus. DHPM 8 displayed an MIC of 0.75 µg/mL against B.cereus, S.aureus, M.luteus, S.faecalis and B.coagulans. Antioxidant activity was assessed using the DPPH method. DHPM 2 showed outstanding free radical scavenging capacity of 90.63% at a concentration of 1 mg/mL. The DHPM 1 - 8 were analysed for their lipoxygenase inhibitory activity. Excellent inhibition ranging from 59.37 ± 0.6 to 81.19 ± 0.94% was demonstrated. The inhibitory activity was elucidated by a molecular docking study against the lipoxygenase enzyme (PDB code = 3V99) using the MOE 2013.08 and Leadit 2.1.2 software and high affinities were demonstrated. DHPM 1 - 8 were tested for cytotoxic activity against two human cancer cell lines, MCF-7 and UACC-62 by means of the MTT assay. It was observed for the MCF-7 cell line, DHPM 1, 4, 6, 7 and 8 displayed cytotoxicity above 89% at 50 µg/mL. The DHPMs at 50 µg/mL were noted to be very effective against the Melanoma cell line with DHPM 2 having a cytotoxicity value of 82.62% and DHPM 1, 4, 5, 6, 7 and 8 exhibiting cytotoxicity greater than 96%. Only slight inhibition of the proliferation of PBMC’s was noted. IC50 values of DHPM 1-8 were determined and the best activity overall was displayed by DHPM 8. The IC50 of DHPM 8 was 0.92 ± 0.09 and 1.97 ± 0.08 µM against MCF - 7 and UACC - 62 cell lines, respectively. The compounds that displayed toxicity towards the UACC - 62 cell line were investigated for their apoptotic inducing potential. The apoptotic studies were performed by flow cytometry using the following assays; Annexin V, JC-1 and Caspase -3 assays. The effect of these compounds was compared to a known anti-cancer drug, Camptothecin. On evaluation of the mechanism of action of the compounds, it was found that most compounds are using apoptotic pathways for cell death. Our studies have identified antimicrobial activity (DHPM 1-8) against Gram positive organisms, high antioxidant activity (DHPM 2), anti-inflammatory activity (DHPM 1-8) and anticancer activity (DHPM 1-8) against UACC-62 and MCF-7 cells. DHPM 1-8 were found to have no toxicity at 100 µg/mL in the brine shrimp assay and hence are probably safe as therapeutic agents. Furthermore molecular docking studies confirmed the activity of DHPM 1-8 as potential lipoxygenase inhibitors. DHPM 1-8 are novel compounds with great potential to be developed into chemotherapeutic agents.
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Book chapters on the topic "4-dihydropyrimidines"

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Curtis, A. D. M. "From 4-Imino-3,4-dihydropyrimidines." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00895.

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Kikelj, D. "From 4-Methyl-6-thioxo-1,6-dihydropyrimidine-5-carbonitriles and 2-Ylidenemalononitriles." In Six-Membered Hetarenes with Two Identical Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-016-00851.

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Conference papers on the topic "4-dihydropyrimidines"

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Gama, Fernando H. de Souza, and Simon J. Garden. "The use of 2,2,6-trimethyl-4H-1,3-dioxin-4-one (TMD) in multicomponent reactions. Synthesis of acetoacetanilides, pyridones and dihydropyrimidines." In 14th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0273-1.

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Duburs, Gunars, Brigita Vigante, Egils Bisenieks, Aivars Krauze, Aiva Plotniece, Arkady Sobolev, Ilona Domracheva, and Karlis Pajuste. "Pleiotropic focused anticancer approach by dihydropyridines, dihydropyrimidines and heteroaromatic compounds." In 4th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2018. http://dx.doi.org/10.3390/ecmc-4-05778.

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Соломийчук, М., О. Панимарчук, В. Кушнир, and М. Никорюк. "Сочетание биологического препарата на основе бактерий Pseudomonas Fluorescens и стимулирующих веществ." In International Scientific Symposium "Plant Protection – Achievements and Prospects". Institute of Genetics, Physiology and Plant Protection, Republic of Moldova, 2020. http://dx.doi.org/10.53040/9789975347204.34.

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Derivatives of ammonium salts of dihydropyrimidine did not show a toxic effect on reducing the concentration of viable cells of the bacterium strain AR-33 Pseudomonas fluorescens. The best indicators of the weight of 100 seeds and the number of formed beans in soybeans were shown by the combination Planriz - 5 l / ha + 0.1% solution of xymedon + 0.2% solution of succinic acid + 2 ml of DMAE + 2 ml of DMSO. The use of all combinations of biocomplexes showed the effectiveness of drugs against diseases in the range of 59.31-69.63%. As a result of the use of biocomplexes, their fungicidal, immunoprotective and stimulating action, an increase in yield of 1.15 - 1.7 times relative to control was recorded. The best yield on potatoes showed a combination of Planriz, v.s. (bacteria of strain AP-33 Pseudomonas fluorescens, 3x109 CFU / cm3) - 5 l / ha + 0.1% solution of ximedon + 0.2% solution of succinic acid + 2 ml of DMAE + 2 ml of DMSO, which was 3 , 4 t / ha. The effectiveness of the drug against late blight was 79.1%.
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