title: Design and synthesis of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives as neuraminidase inhibitors.
abstract: A series of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives were prepared to evaluate their ability of inhibiting neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from aldehyde by using a suitable synthetic strategy, which showed moderate inhibitory activity against influenza A NA. Compound 6g exhibited the strongest inhibitory activity against influenza virus A NA (IC50 = 17.64 μM), which indicated pyrimidine ring could be used as a core structure to design novel influenza NA inhibitors.
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Lou
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Rao
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Wenwen
authors.initials: W
authors.lastname: Qi
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Jinhui
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Haiyu
authors.initials: H
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Yuxi
authors.initials: Y
authors.lastname: Li
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Jinping
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Zhiming
authors.initials: Z
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Xianming
authors.initials: X
authors.lastname: Hu
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China. Electronic address: liupengwhu@whu.edu.cn.
authors.forename: Peng
authors.initials: P
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Virology, Ministry of Education, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, 185# Donghu Rd, Wuhan 430071, China.
authors.forename: Xuechuan
authors.initials: X
authors.lastname: Hong
mesh_terms: D020134:Catalytic Domain; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009980:Influenza A virus / Q000201:enzymology*; D008958:Models, Molecular; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C000596337:6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D009439:Neuraminidase
keywords: 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives; Anti-influenza; Neuraminidase inhibitors; SAR