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261por Valle-Casuso, José-Carlos, Gaudaire, Delphine, Martin-Faivre, Lydie, Madeline, Anthony, Dallemagne, Patrick, Pronost, Stéphane, Munier-Lehmann, Hélène, Zientara, Stephan, Vidalain, Pierre-Olivier, Hans, Aymeric“…Using this assay, we identified three molecules that impair EAV infection in equine cells: the broad-spectrum antiviral and nucleoside analog ribavirin, and two compounds previously described as inhibitors of dihydroorotate dehydrogenase (DHODH), the fourth enzyme of the pyrimidine biosynthesis pathway. These molecules effectively suppressed cytopathic effects associated to EAV infection, and strongly inhibited viral replication and production of infectious particles. …”
Publicado 2020
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262por Wu, Wenneng, Chen, Meihang, Fei, Qiang, Ge, Yonghui, Zhu, Yingying, Chen, Haijiang, Yang, Maofa, Ouyang, Guiping“…In this study, thirteen new pyridylpyrazolamide derivatives containing pyrimidine motifs were synthesized via six-step reactions. …”
Publicado 2020
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263por Kokorekin, Vladimir A., Neverov, Sergey V., Kuzina, Vera N., Petrosyan, Vladimir A.“…This method is equally effective for the synthesis of 3-thiocyanatopyrazolo[1,5-a]pyrimidines, both without substituents and with various donor (acceptor) substituents in the pyrimidine ring.…”
Publicado 2020
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264por Robinson, William J., Taylor, Annie E., Lauga-Cami, Solange, Weaver, George W., Arroo, Randolph R.J., Kaiser, Marcel, Gul, Sheraz, Kuzikov, Maria, Ellinger, Bernhard, Singh, Kuldip, Schirmeister, Tanja, Botana, Adolfo, Eurtivong, Chatchakorn, Bhambra, Avninder S.“…Our work herein describes the design and syntheses of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines, with compound 13, the 4-(2-methoxyphenyl)-6-(pyridine-3-yl)pyrimidin-2-amine demonstrating an IC(50) value of 0.38 μM and a promising off-target ADME-Tox profile in vitro. …”
Publicado 2021
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265por Provenzani, Riccardo, San-Martin-Galindo, Paola, Hassan, Ghada, Legehar, Ashenafi, Kallio, Aleksi, Xhaard, Henri, Fallarero, Adyary, Yli-Kauhaluoma, Jari“…Taken together, our study highlights the value of multisubstituted pyrimidines to develop novel anti-biofilm agents.…”
Publicado 2021
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266por Chmiel-Szukiewicz, Elżbieta“…This work presents the results of research related to the determination of application possibilities of new oligoetherols with 1,3-pyrimidine rings and boron atoms in rigid polyurethane foam production. …”
Publicado 2021
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267“…Herein, we report that the pyrimidine nucleoside phosphorylase from Thermus thermophilus is active over an exceptionally broad pH (4–10), temperature (up to 100 °C) and cosolvent space (up to 80 % (v/v) nonaqueous medium), and displays tremendous stability under harsh reaction conditions with predicted total turnover numbers of more than 10(6) for various pyrimidine nucleosides. …”
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268por Gabryel-Skrodzka, Malwina, Nowak, Martyna, Stachowiak, Klaudia, Zabiszak, Michal, Ogawa, Kazuma, Jastrzab, Renata“…The influence of pH on the complex formation of phosphoethanolamine and pyrimidine nucleosides (uridine, cytidine and thymidine) with copper(II) ions was studied. …”
Publicado 2021
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269por Lauritsen, Ida, Frendorf, Pernille Ott, Capucci, Silvia, Heyde, Sophia A. H., Blomquist, Sarah D., Wendel, Sofie, Fischer, Emil C., Sekowska, Agnieszka, Danchin, Antoine, Nørholm, Morten H. H.“…Here, we study the sequential generation of hotspot mutations in those genes, and uncover a regulatory role of pyrimidine nucleosides in carbon catabolism. Cytidine binds to the cytidine regulator CytR, modifies the expression of sigma factor 32 (RpoH), and thereby impacts global gene expression. …”
Publicado 2021
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270por Johansson, Niklas G., Dreano, Loïc, Vidilaseris, Keni, Khattab, Ayman, Liu, Jianing, Lasbleiz, Arthur, Ribeiro, Orquidea, Kiriazis, Alexandros, Boije af Gennäs, Gustav, Meri, Seppo, Goldman, Adrian, Yli‐Kauhaluoma, Jari, Xhaard, Henri“…We furthermore provide early structure‐activity relationships around a new scaffold having a pyrazolo[1,5‐a]pyrimidine core. The most promising pyrazolo[1,5‐a]pyrimidine congener was further investigated and found to inhibit Plasmodium falciparum mPPase in membranes as well as the growth of P. falciparum in an ex vivo survival assay.…”
Publicado 2021
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271por Rashid, Haroon ur, Martines, Marco Antonio Utrera, Duarte, Adriana Pereira, Jorge, Juliana, Rasool, Shagufta, Muhammad, Riaz, Ahmad, Nasir, Umar, Muhammad Naveed“…Pyrimidines are aromatic heterocyclic compounds that contain two nitrogen atoms at positions 1 and 3 of the six-membered ring. …”
Publicado 2021
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272“…We report a prebiotically relevant solution to the N1-ribosylation of pyrimidine nucleobases, a well-known challenge to the RNA world hypothesis. …”
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273por Drewry, David H., Annor-Gyamfi, Joel K., Wells, Carrow I., Pickett, Julie E., Dederer, Verena, Preuss, Franziska, Mathea, Sebastian, Axtman, Alison D.“…[Image: see text] The pyrimidine core has been utilized extensively to construct kinase inhibitors, including eight FDA-approved drugs. …”
Publicado 2021
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274por Xiong, Yinghui, Wu, Li, Shao, Li, Wang, Yang, Huang, Zebing, Huang, Xun, Li, Chunhui, Wu, Anhua, Liu, Zhenguo, Fan, Xuegong, Zhou, Pengcheng“…Interestingly, the disorders of pyrimidine and purine metabolites like the known microbial metabolites thymidine and 2′-deoxyuridine had already occurred in liver fibrosis and continued in cirrhosis. …”
Publicado 2022
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275“…Early detection of BRCA will increase the probability of cure. Pyrimidine metabolism (PyM) stands for an essential metabolic pathway related to DNA replication of cancer cells, which may also serve as a diagnostic marker and therapeutic target. …”
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276por Nguyen, Oanh T. K., Ha, Pha T., Dang, Ha V., Vo, Yen H., Nguyen, Tung T., Le, Nhan T. H., Phan, Nam T. S.“…An aerobic coupling of 2-aminopyrimidines or 2-aminopyridines with trans-chalcones to afford aroylimidazo[1,2-a]pyrimidines and aroylimidazo[1,2-a]pyridines is reported. …”
Publicado 2019
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277por Yadav, Tanuja T., Moin Shaikh, Gulam, Kumar, Maushmi S., Chintamaneni, Meena, YC, Mayur“…From the literature, it shows that pyrimidine is one of the most commonly studied heterocycles for its antiproliferative activity against EGFR inhibition. …”
Publicado 2022
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278“…In this issue of EMBO Molecular Medicine, So and colleagues investigate the mechanism of action of AG636, a new potent inhibitor of de novo pyrimidine synthesis, and discovered an unexpected link to AML protein translation essential for LSC function.…”
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279“…A battery of novel pyrimidine-quinolone hybrids was designed by docking scaffold replacement as lactate dehydrogenase A (hLDHA) inhibitors. …”
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280“…Twenty-three novel trifluoromethyl pyrimidine derivatives containing an amide moiety were designed and synthesized through four-step reactions and evaluated for their antifungal, insecticidal, and anticancer properties. …”
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