BIOMAT Database Logo BIOMAT Database Logo

Design, synthesis and biological evaluation of honokiol derivatives as influenza neuraminidase inhibitors. 2019

Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
College of Chemistry and Chemical Engineering, Hunan University , Changsha 410082 , China.

Honokiol, a natural polyphenol, which was reported to have satisfactory influenza neuraminidase (NA) inhibitory activity, was structurally modified. Twenty-three compounds were synthesized and the ortho-effects in the epoxidation and hydrolyzation reactions were studied. The derivatives were evaluated for NA inhibitory activity and the benzoylhydrazone derivatives showed much better anti-NA activity than honokiol. Structure-activity relationship analysis suggested that the polyphenols exhibited better anti-NA activity than monophenols and biphenols. Furthermore, probable binding mode of drug with target revealed that the most active compound had much stronger interactions with the active site of NA than honokiol suggesting the potent anti-influenza virus activity.

UI MeSH Term Description Entries
D007251 Influenza, Human An acute viral infection in humans involving the respiratory tract. It is marked by inflammation of the NASAL MUCOSA; the PHARYNX; and conjunctiva, and by headache and severe, often generalized, myalgia. Grippe,Human Flu,Human Influenza,Influenza in Humans,Influenza,Flu, Human,Human Influenzas,Influenza in Human,Influenzas,Influenzas, Human
D009439 Neuraminidase An enzyme that catalyzes the hydrolysis of alpha-2,3, alpha-2,6-, and alpha-2,8-glycosidic linkages (at a decreasing rate, respectively) of terminal sialic residues in oligosaccharides, glycoproteins, glycolipids, colominic acid, and synthetic substrate. (From Enzyme Nomenclature, 1992) Sialidase,Exo-alpha-Sialidase,N-Acylneuraminate Glycohydrolases,Oligosaccharide Sialidase,Exo alpha Sialidase,Glycohydrolases, N-Acylneuraminate,N Acylneuraminate Glycohydrolases,Sialidase, Oligosaccharide
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000998 Antiviral Agents Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly. Antiviral,Antiviral Agent,Antiviral Drug,Antivirals,Antiviral Drugs,Agent, Antiviral,Agents, Antiviral,Drug, Antiviral,Drugs, Antiviral
D001713 Biphenyl Compounds Whitish aromatic crystalline organic compounds made up of two conjoined BENZENE rings. Compounds, Biphenyl
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D017705 Lignans A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed) Lignan,Neolignan,Neolignans

Related Publications

Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.
August 2011, Journal of enzyme inhibition and medicinal chemistry,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis and biological evaluation of dihydrofurocoumarin derivatives as potent neuraminidase inhibitors.
April 2021, Bioorganic & medicinal chemistry letters,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis, and biological evaluation of crenatoside analogues as novel influenza neuraminidase inhibitors.
February 2016, European journal of medicinal chemistry,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis and biological evaluation of novel zanamivir derivatives as potent neuraminidase inhibitors.
December 2018, Bioorganic & medicinal chemistry letters,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, Synthesis, and Biological Evaluation of Novel Acylhydrazone Derivatives as Potent Neuraminidase Inhibitors.
September 2020, ACS medicinal chemistry letters,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors.
December 2017, Bioorganic & medicinal chemistry letters,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.
January 2020, European journal of medicinal chemistry,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis, and bioassay of 4-thiazolinone derivatives as influenza neuraminidase inhibitors.
March 2021, European journal of medicinal chemistry,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Design, synthesis and biological activity of thiazolidine-4-carboxylic acid derivatives as novel influenza neuraminidase inhibitors.
April 2011, Bioorganic & medicinal chemistry,
Ding Lin, and Yang-Jie Yi, and Meng-Wu Xiao, and Jia Chen, and Jiao Ye, and Ai-Xi Hu, and Wen-Wen Lian, and Ai-Lin Liu, and Guan-Hua Du
Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors.
July 1999, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!