Synthesis and anti-CVB3 activity of 4-amino acid derivative substituted pyrimidine nucleoside analogues |
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| Institution: | 1. High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou, Henan Province 450002, PR China;2. College of Chemistry, Zhengzhou University, Zhengzhou, Henan Province 450001, PR China;3. Henan Key Laboratory of Organic Functional Molecules and Drug Innovation, Henan Normal University, Xinxiang 453007, PR China;1. Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK;2. Division of Biosciences, Institute of Structural and Molecular Biology, University College London, London WC1E 6BT, UK;3. Wolfson Institute of Biomedical Research, University College London, Gower Street, London WC1E 6BT, UK;1. Department of Chemistry, Faculty of Science, Ain Shams University, Abbassia, Cairo, Egypt;2. Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Cairo, Egypt;3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Heliopolis University for Sustainable Development, Cairo, Egypt;4. Division of Biochemistry, Department of Pharmacology, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia;5. Department of Biochemistry, Faculty of Science, Ain Shams University, Abbassia, Cairo, Egypt;1. Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukaramah 21514, Saudi Arabia;2. Department of Chemistry, Collage of Science, Taif University, P. O. Box 11099, Taif 21944, Saudi Arabia;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt;4. Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt;1. Department of Chemistry, RTM Nagpur University, Nagpur 440033, India;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia;3. Laboratory of Applied Organic Chemistry LCOA, Synthesis of Biomolecules and Molecular Modelling Group, Badji-Mokhtar - Annaba University, Box 12, 23000 Annaba, Algeria;4. University Mohamed Premier, Faculty of Science, Department of Chemistry, Laboratory of Applied and Environmental Chemistry, BV Mohammed VI, BP 524, 60000 Oujda, Morocco;5. Department of Chemistry, College of Science, University of Bahrain, Sakhir 32038, Bahrain;1. Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University, School of Medicine, Atlanta, GA 30322, United States;2. Cocrystal Pharma, Inc., Tucker, GA 30084, United States |
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| Abstract: | Seven novel 4-amino acid derivative substituted pyrimidine nucleoside analogues were designed, synthesized, and tested for their anti-CVB3 activity. Initial biological studies indicated that among these 4-amino acid derivative substituted pyrimidine nucleoside analogues, 4-N-(2′-amino-glutaric acid-1′-methylester)-1-(2′- deoxy-2′-β-fluoro-4′-azido)-furanosyl-cytosine 2 exhibited the most potent anti-CVB activity (IC50 = 9.3 μM). The cytotoxicity of these compounds has also been assessed. The toxicity of compound 2 was similar to that of ribavirin. |
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| Keywords: | Pyrimidine nucleoside Amino acid Anti-CVB3 activity Synthesis |
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