The Experts below are selected from a list of 17742 Experts worldwide ranked by ideXlab platform
Shin-ichiro Nishimura - One of the best experts on this subject based on the ideXlab platform.
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Novel trivalent Anti-Influenza reagent
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Fei Feng, Nobuaki Miura, Masatoshi Okamatsu, Yoshihiro Sakoda, Hiroshi Kida, Norikazu Isoda, Shin-ichiro NishimuraAbstract:Abstract We designed and synthesized novel trivalent Anti-Influenza reagents. Sialyllactose was located at the terminal of each valence which aimed to block each receptor-binding site of the hemagglutinin (HA) trimer on the surface of the virus. Structural analyses were carried out with a model which was constructed with a computer simulation. A previously reported cyclic glycopeptide blocker [Ohta, T.; Miura, N.; Fujitani, N.; Nakajima, F.; Niikura, K.; Sadamoto, R.; Guo, C.-T.; Suzuki, T.; Suzuki, Y.; Monde, K.; Nishimura, S.-I. Angew. Chem. Int. Ed. , 2003 , 42 , 5186] bound to the HA in the model. The analyses suggest that the glutamine residue in the cyclic peptide bearing Neu5Acα2,3Galβ1,4Glc trisaccharide via a linker interacts with the Gln189 in HA through hydrogen bonding. The present Anti-Influenza reagents likely interact with a glutamine residue included in the vicinity of Gln189. A plague reduction assay of the Influenza virus, A/PR/8/1934 (H1N1), was performed in MDCK cells to evaluate for the synthesized compounds to inhibit viral replication. One of the compounds showed approximately 85% inhibition at the concentration of 400 μM at 4 °C.
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Novel trivalent Anti-Influenza reagent
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Fei Feng, Nobuaki Miura, Masatoshi Okamatsu, Yoshihiro Sakoda, Hiroshi Kida, Norikazu Isoda, Shin-ichiro NishimuraAbstract:Abstract We designed and synthesized novel trivalent Anti-Influenza reagents. Sialyllactose was located at the terminal of each valence which aimed to block each receptor-binding site of the hemagglutinin (HA) trimer on the surface of the virus. Structural analyses were carried out with a model which was constructed with a computer simulation. A previously reported cyclic glycopeptide blocker [Ohta, T.; Miura, N.; Fujitani, N.; Nakajima, F.; Niikura, K.; Sadamoto, R.; Guo, C.-T.; Suzuki, T.; Suzuki, Y.; Monde, K.; Nishimura, S.-I. Angew. Chem. Int. Ed. , 2003 , 42 , 5186] bound to the HA in the model. The analyses suggest that the glutamine residue in the cyclic peptide bearing Neu5Acα2,3Galβ1,4Glc trisaccharide via a linker interacts with the Gln189 in HA through hydrogen bonding. The present Anti-Influenza reagents likely interact with a glutamine residue included in the vicinity of Gln189. A plague reduction assay of the Influenza virus, A/PR/8/1934 (H1N1), was performed in MDCK cells to evaluate for the synthesized compounds to inhibit viral replication. One of the compounds showed approximately 85% inhibition at the concentration of 400 μM at 4 °C.
Fei Feng - One of the best experts on this subject based on the ideXlab platform.
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Novel trivalent Anti-Influenza reagent
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Fei Feng, Nobuaki Miura, Masatoshi Okamatsu, Yoshihiro Sakoda, Hiroshi Kida, Norikazu Isoda, Shin-ichiro NishimuraAbstract:Abstract We designed and synthesized novel trivalent Anti-Influenza reagents. Sialyllactose was located at the terminal of each valence which aimed to block each receptor-binding site of the hemagglutinin (HA) trimer on the surface of the virus. Structural analyses were carried out with a model which was constructed with a computer simulation. A previously reported cyclic glycopeptide blocker [Ohta, T.; Miura, N.; Fujitani, N.; Nakajima, F.; Niikura, K.; Sadamoto, R.; Guo, C.-T.; Suzuki, T.; Suzuki, Y.; Monde, K.; Nishimura, S.-I. Angew. Chem. Int. Ed. , 2003 , 42 , 5186] bound to the HA in the model. The analyses suggest that the glutamine residue in the cyclic peptide bearing Neu5Acα2,3Galβ1,4Glc trisaccharide via a linker interacts with the Gln189 in HA through hydrogen bonding. The present Anti-Influenza reagents likely interact with a glutamine residue included in the vicinity of Gln189. A plague reduction assay of the Influenza virus, A/PR/8/1934 (H1N1), was performed in MDCK cells to evaluate for the synthesized compounds to inhibit viral replication. One of the compounds showed approximately 85% inhibition at the concentration of 400 μM at 4 °C.
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Novel trivalent Anti-Influenza reagent
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Fei Feng, Nobuaki Miura, Masatoshi Okamatsu, Yoshihiro Sakoda, Hiroshi Kida, Norikazu Isoda, Shin-ichiro NishimuraAbstract:Abstract We designed and synthesized novel trivalent Anti-Influenza reagents. Sialyllactose was located at the terminal of each valence which aimed to block each receptor-binding site of the hemagglutinin (HA) trimer on the surface of the virus. Structural analyses were carried out with a model which was constructed with a computer simulation. A previously reported cyclic glycopeptide blocker [Ohta, T.; Miura, N.; Fujitani, N.; Nakajima, F.; Niikura, K.; Sadamoto, R.; Guo, C.-T.; Suzuki, T.; Suzuki, Y.; Monde, K.; Nishimura, S.-I. Angew. Chem. Int. Ed. , 2003 , 42 , 5186] bound to the HA in the model. The analyses suggest that the glutamine residue in the cyclic peptide bearing Neu5Acα2,3Galβ1,4Glc trisaccharide via a linker interacts with the Gln189 in HA through hydrogen bonding. The present Anti-Influenza reagents likely interact with a glutamine residue included in the vicinity of Gln189. A plague reduction assay of the Influenza virus, A/PR/8/1934 (H1N1), was performed in MDCK cells to evaluate for the synthesized compounds to inhibit viral replication. One of the compounds showed approximately 85% inhibition at the concentration of 400 μM at 4 °C.
Xiaorong Wang - One of the best experts on this subject based on the ideXlab platform.
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Anti-Influenza agents from plants and traditional Chinese medicine.
Phytotherapy research : PTR, 2006Co-Authors: Xiaoyan Wang, Wei Jia, Aihua Zhao, Xiaorong WangAbstract:Influenza is a serious threat to health in all parts of the world. The control and treatment of Influenza depends mainly on chemical or biochemical agents and, to date, some Anti-Influenza agents have been isolated from plants as a result of chemical and pharmacological studies. These agents include a variety of polyphenols, flavonoids, saponins, glucosides and alkaloids. Traditional medicine focuses on the use of herbs and traditional Chinese medicine has performed well in clinical practice and shows a potential in the therapy of Influenza and its symptoms. The present paper reviews some constituents and extracts from plants and traditional Chinese medicine with Anti-Influenza activity.
Mark Von Itzstein - One of the best experts on this subject based on the ideXlab platform.
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Recent progress in the discovery of neuraminidase inhibitors as Anti-Influenza agents
Annual Reports in Medicinal Chemistry, 2013Co-Authors: Aisyah Saad Abdul Rahim, Mark Von ItzsteinAbstract:Abstract Influenza continues to pose imminent threat to mankind, at times in epic proportions. However, Anti-Influenza therapeutic options are limited. The recent emergence of flu viruses, of varying virulence and infectivity, underscores the urgency for new neuraminidase (NA) inhibitors. This review aims to highlight the progress in NA inhibitors (NAIs) that have emerged in the last 6 years including the exciting discovery of sialic acid analogues that lock open the 150-loop of group 1 NAs. The review begins with a brief account of the flexible 150-loop in group 1 NAs and recent viral mutations before it continues onto the recent progress in the discovery of NAIs—grouped according to flexible and rigid scaffolds. A short discussion on the potential of natural products as Anti-Influenza drug leads is also included. This review concludes with an outlook on the future direction for the next generation of Anti-Influenza therapeutics.
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Anti-Influenza drugs: the development of sialidase inhibitors.
Handbook of experimental pharmacology, 2009Co-Authors: Mark Von Itzstein, Robin J. ThomsonAbstract:Viruses, particularly those that are harmful to humans, are the 'silent terrorists' of the twenty-first century. Well over four million humans die per annum as a result of viral infections alone. The scourge of Influenza virus has plagued mankind throughout the ages. The fact that new viral strains emerge on a regular basis, particularly out of Asia, establishes a continual socio-economic threat to mankind. The arrival of the highly pathogenic avian Influenza H5N1 heightened the threat of a potential human pandemic to the point where many countries have put in place 'preparedness plans' to defend against such an outcome. The discovery of the first designer Influenza virus sialidase inhibitor and Anti-Influenza drug Relenza™, and subsequently Tamiflu™, has now inspired a number of continuing efforts towards the discovery of next generation Anti-Influenza drugs. Such drugs may act as 'first-line-of-defence' against the spread of Influenza infection and buy time for necessary vaccine development particularly in a human pandemic setting. Furthermore, the fact that Influenza virus can develop resistance to therapeutics makes these continuing efforts extremely important. An overview of the role of the virus-associated glycoprotein sialidase (neuraminidase) and some of the most recent developments towards the discovery of Anti-Influenza drugs based on the inhibition of Influenza virus sialidase is provided in this chapter.
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Anti-Influenza virus drug design: Sialidase inhibitors
Australian Journal of Chemistry, 2001Co-Authors: Jeffrey Clifford Dyason, Mark Von ItzsteinAbstract:This review will give an overview of the design process behind the development of sialidase inhibitors, which can be used as Anti-Influenza drugs. Two drugs (Relenza™ and Tamiflu™) are already available as prescription drugs and a third (BCX-1812) is currently undergoing third-phase clinical trials. Also, the use of molecular-modelling techniques in the understanding of the mechanism and the prediction of inhibition of this enzyme is reviewed.
Kuo Hsiung Lee - One of the best experts on this subject based on the ideXlab platform.
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Development of Anti‐Influenza agents from natural products
Medicinal research reviews, 2020Co-Authors: Zhi‐jun Zhang, Susan L. Morris-natschke, Yung-yi Cheng, Kuo Hsiung LeeAbstract:The Influenza pandemic continues to threaten public health due to its high morbidity and mortality rates, despite some successes in Antiviral research. Natural drugs are important alternative therapies in the treatment of and recovery from Influenza and have been the subjects of intense investigation during the last few decades. Many reports have shown that the development of novel bioactive chemicals extracted from natural drugs has significant advantages. Oseltamivir is a successful case of an Anti-Influenza drug synthesized using two natural products, quinic acid, and shikimic acid, as starting materials. In China, traditional Chinese medicine (TCM) plays an important role in the treatment of Influenza. TCM herbal extracts and prescriptions or their isolated bioactive constituents have shown significant therapeutic and preventive effects against Influenza. For example, the roots of Isatis indigotica (Banlangen) fight viral infection by targeting both the virus and the host and have significantly different effects than those of synthetic chemicals. Lianhuaqingwen capsule exerts its Anti-Influenza activity by regulating the immune response to interfere with both viral and host reactions and might well be an alternative therapeutic option to treat Influenza virus infection. This paper reviews the chemical ingredients, crude extracts, and TCM prescriptions with Anti-Influenza activity reported during the period of 2010-September 2019. We hope that this comprehensive review will not only fuel research on Anti-Influenza active natural products and TCM research but also provide a promising alternative candidate for further Anti-Influenza drug development.
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Phenolic diterpenoid derivatives as Anti-Influenza a virus agents.
ACS medicinal chemistry letters, 2015Co-Authors: Zhao Dang, Kuo Hsiung Lee, Katherine Jung, Lei Zhu, Hua Xie, Chin Ho Chen, Li HuangAbstract:A series of diterpenoid derivatives based on podocarpic acid were synthesized and evaluated as Anti-Influenza A virus agents. Several of the novel podocarpic acid derivatives exhibited nanomolar activities against an H1N1 Influenza A virus (A/Puerto Rico/8/34) that was resistant to two Anti-Influenza drugs, oseltamivir and amantadine. This class of compounds inhibits the Influenza virus by targeting the viral hemagglutinin-mediated membrane fusion. These results indicated that podocarpic acid derivatives may serve as potential drug candidates to fight drug-resistant Influenza A virus infections.
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Identification and Synthesis of Quinolizidines with Anti-Influenza A Virus Activity
ACS medicinal chemistry letters, 2014Co-Authors: Zhao Dang, Kuo Hsiung Lee, Katherine Jung, Lei Zhu, Hua Xie, Li Huang, Weihong Lai, Chin Ho ChenAbstract:Influenza A virus infection causes a contagious respiratory illness that poses a threat to human health. However, there are limited Anti-Influenza A therapeutics available, which is further compounded by the emergence of drug resistant viruses. In this study, Sophora quinolizidine alkaloids were identified as a new class of Anti-Influenza A virus agents. Among the tested Sophora alkaloids, dihydroaloperine exhibited the most potent activity with an EC50 of 11.2 μM. The potency of the quinolizidine alkaloids was improved by approximately 5-fold with chemical modifications on the aloperine molecule. These compounds were effective against an H1N1 Influenza A virus that was resistant to the two Antiflu drugs oseltamivir and amantadine. The identification of the quinolizidine alkaloids as effective and novel Anti-Influenza A agents may aid in the development of new therapeutics.