The Experts below are selected from a list of 7518 Experts worldwide ranked by ideXlab platform
Akira Naito - One of the best experts on this subject based on the ideXlab platform.
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synergistic antiviral activity of s 033188 s 033447 a novel inhibitor of influenza virus cap dependent endonuclease in combination with Neuraminidase Inhibitors in vitro
Open Forum Infectious Diseases, 2017Co-Authors: Mitsutaka Kitano, Atsuko Yamamoto, Takeshi Noshi, Makoto Kawai, Ryu Yoshida, Akihiko Sato, Takao Shishido, Akira NaitoAbstract:Background S-033447, an active form of orally available prodrug S-033188, is a novel small molecule inhibitor of cap-dependent endonuclease that is essential for influenza virus transcription and replication. In this study, we evaluated the inhibitory effect of S-033188 in combination with Neuraminidase Inhibitors on the replication of influenza A/H1N1 virus in cultured cells.
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Synergistic Antiviral Activity of S-033188/S-033447, a Novel Inhibitor of Influenza Virus Cap-Dependent Endonuclease, in Combination with Neuraminidase Inhibitors In Vitro.
Open Forum Infectious Diseases, 2017Co-Authors: Mitsutaka Kitano, Atsuko Yamamoto, Takeshi Noshi, Makoto Kawai, Ryu Yoshida, Akihiko Sato, Takao Shishido, Akira NaitoAbstract:Background S-033447, an active form of orally available prodrug S-033188, is a novel small molecule inhibitor of cap-dependent endonuclease that is essential for influenza virus transcription and replication. In this study, we evaluated the inhibitory effect of S-033188 in combination with Neuraminidase Inhibitors on the replication of influenza A/H1N1 virus in cultured cells.
Hideo Yasunaga - One of the best experts on this subject based on the ideXlab platform.
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trends of Neuraminidase Inhibitors use in children with influenza related respiratory infections
Pediatric Pulmonology, 2018Co-Authors: Kazuhiro Uda, Naho Morisaki, Yusuke Okubo, Nobuaki Michihata, Kensuke Shoji, Isao Miyairi, Hiroki Matsui, Kiyohide Fushimi, Hideo YasunagaAbstract:BACKGROUND Neuraminidase Inhibitors are recommended for children hospitalized with influenza-related respiratory infections, and oseltamivir is the first choice of treatment in most situations. However, little is known regarding the recent trend in using Neuraminidase Inhibitors and their difference in health economy. The aim of this study was to reveal recent trends in Neuraminidase inhibitor use and compare hospitalization costs across different treatment regimens. METHODS We retrospectively obtained the hospital discharge records of inpatients under 18 years of age with a diagnosis of influenza-related respiratory infections using a national inpatient database in Japan. We excluded patients with chronic medical conditions from the analyses. Multivariable mixed effects regression models were used to investigate the recent treatment trends and healthcare costs. RESULTS We identified 27 771 inpatients with influenza-related respiratory infections. The proportions of Neuraminidase inhibitor use increased from 62.6% in 2010 to 71.8% in2014 (Ptrend < 0.001). Correspondingly, the proportions of peramivir use showed an upward trend, ranging from 31.4% to 57.4% (Ptrend < 0.001). In contrast, proportions of oseltamivir and zanamivir use decreased from 26.1% to 12.1% and from 4.9% to 1.5%, respectively (Ptrend < 0.001). Laninamivir use did not change over the period. Total hospitalization costs were higher in the peramivir group than in the oseltamivir group (adjusted difference, $84.3; 95%CI, $70.7-$98.4). CONCLUSIONS We observed an increasing trend in peramivir use and decreasing trends in use of oseltamivir and zanamivir. Treatment with peramivir required higher hospitalization costs.
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Trends of Neuraminidase Inhibitors use in children with influenza related respiratory infections.
Pediatric Pulmonology, 2018Co-Authors: Yusuke Okubo, Naho Morisaki, Nobuaki Michihata, Kensuke Shoji, Isao Miyairi, Hiroki Matsui, Kiyohide Fushimi, Hideo YasunagaAbstract:BACKGROUND:Neuraminidase Inhibitors are recommended for children hospitalized with influenza-related respiratory infections, and oseltamivir is the first choice of treatment in most situations. However, little is known regarding the recent trend in using Neuraminidase Inhibitors and their difference in health economy. The aim of this study was to reveal recent trends in Neuraminidase inhibitor use and compare hospitalization costs across different treatment regimens. METHODS:We retrospectively obtained the hospital discharge records of inpatients under 18 years of age with a diagnosis of influenza-related respiratory infections using a national inpatient database in Japan. We excluded patients with chronic medical conditions from the analyses. Multivariable mixed effects regression models were used to investigate the recent treatment trends and healthcare costs. RESULTS:We identified 27 771 inpatients with influenza-related respiratory infections. The proportions of Neuraminidase inhibitor use increased from 62.6% in 2010 to 71.8% in2014 (Ptrend
Yusuke Okubo - One of the best experts on this subject based on the ideXlab platform.
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trends of Neuraminidase Inhibitors use in children with influenza related respiratory infections
Pediatric Pulmonology, 2018Co-Authors: Kazuhiro Uda, Naho Morisaki, Yusuke Okubo, Nobuaki Michihata, Kensuke Shoji, Isao Miyairi, Hiroki Matsui, Kiyohide Fushimi, Hideo YasunagaAbstract:BACKGROUND Neuraminidase Inhibitors are recommended for children hospitalized with influenza-related respiratory infections, and oseltamivir is the first choice of treatment in most situations. However, little is known regarding the recent trend in using Neuraminidase Inhibitors and their difference in health economy. The aim of this study was to reveal recent trends in Neuraminidase inhibitor use and compare hospitalization costs across different treatment regimens. METHODS We retrospectively obtained the hospital discharge records of inpatients under 18 years of age with a diagnosis of influenza-related respiratory infections using a national inpatient database in Japan. We excluded patients with chronic medical conditions from the analyses. Multivariable mixed effects regression models were used to investigate the recent treatment trends and healthcare costs. RESULTS We identified 27 771 inpatients with influenza-related respiratory infections. The proportions of Neuraminidase inhibitor use increased from 62.6% in 2010 to 71.8% in2014 (Ptrend < 0.001). Correspondingly, the proportions of peramivir use showed an upward trend, ranging from 31.4% to 57.4% (Ptrend < 0.001). In contrast, proportions of oseltamivir and zanamivir use decreased from 26.1% to 12.1% and from 4.9% to 1.5%, respectively (Ptrend < 0.001). Laninamivir use did not change over the period. Total hospitalization costs were higher in the peramivir group than in the oseltamivir group (adjusted difference, $84.3; 95%CI, $70.7-$98.4). CONCLUSIONS We observed an increasing trend in peramivir use and decreasing trends in use of oseltamivir and zanamivir. Treatment with peramivir required higher hospitalization costs.
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Trends of Neuraminidase Inhibitors use in children with influenza related respiratory infections.
Pediatric Pulmonology, 2018Co-Authors: Yusuke Okubo, Naho Morisaki, Nobuaki Michihata, Kensuke Shoji, Isao Miyairi, Hiroki Matsui, Kiyohide Fushimi, Hideo YasunagaAbstract:BACKGROUND:Neuraminidase Inhibitors are recommended for children hospitalized with influenza-related respiratory infections, and oseltamivir is the first choice of treatment in most situations. However, little is known regarding the recent trend in using Neuraminidase Inhibitors and their difference in health economy. The aim of this study was to reveal recent trends in Neuraminidase inhibitor use and compare hospitalization costs across different treatment regimens. METHODS:We retrospectively obtained the hospital discharge records of inpatients under 18 years of age with a diagnosis of influenza-related respiratory infections using a national inpatient database in Japan. We excluded patients with chronic medical conditions from the analyses. Multivariable mixed effects regression models were used to investigate the recent treatment trends and healthcare costs. RESULTS:We identified 27 771 inpatients with influenza-related respiratory infections. The proportions of Neuraminidase inhibitor use increased from 62.6% in 2010 to 71.8% in2014 (Ptrend
Mitsutaka Kitano - One of the best experts on this subject based on the ideXlab platform.
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synergistic antiviral activity of s 033188 s 033447 a novel inhibitor of influenza virus cap dependent endonuclease in combination with Neuraminidase Inhibitors in vitro
Open Forum Infectious Diseases, 2017Co-Authors: Mitsutaka Kitano, Atsuko Yamamoto, Takeshi Noshi, Makoto Kawai, Ryu Yoshida, Akihiko Sato, Takao Shishido, Akira NaitoAbstract:Background S-033447, an active form of orally available prodrug S-033188, is a novel small molecule inhibitor of cap-dependent endonuclease that is essential for influenza virus transcription and replication. In this study, we evaluated the inhibitory effect of S-033188 in combination with Neuraminidase Inhibitors on the replication of influenza A/H1N1 virus in cultured cells.
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Synergistic Antiviral Activity of S-033188/S-033447, a Novel Inhibitor of Influenza Virus Cap-Dependent Endonuclease, in Combination with Neuraminidase Inhibitors In Vitro.
Open Forum Infectious Diseases, 2017Co-Authors: Mitsutaka Kitano, Atsuko Yamamoto, Takeshi Noshi, Makoto Kawai, Ryu Yoshida, Akihiko Sato, Takao Shishido, Akira NaitoAbstract:Background S-033447, an active form of orally available prodrug S-033188, is a novel small molecule inhibitor of cap-dependent endonuclease that is essential for influenza virus transcription and replication. In this study, we evaluated the inhibitory effect of S-033188 in combination with Neuraminidase Inhibitors on the replication of influenza A/H1N1 virus in cultured cells.
Dirk B Mendel - One of the best experts on this subject based on the ideXlab platform.
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carbocyclic influenza Neuraminidase Inhibitors possessing a c3 cyclic amine side chain synthesis and inhibitory activity
Bioorganic & Medicinal Chemistry Letters, 2000Co-Authors: H. Wu, Bradford Graves, Paul A Escarpe, Holly L Macarthur, X. Chen, Dirk B MendelAbstract:As part of our continuing work in the area of influenza Neuraminidase Inhibitors, a series of C3-aza Inhibitors possessing a cyclic amine side chain was synthesized and evaluated for influenza Neuraminidase inhibitory activity. Analogues possessing a six-, seven- and eight-membered ring, 4c–e, respectively, at the C3 position exhibited excellent influenza B Neuraminidase inhibition.
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Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza Neuraminidase Inhibitors
Bioorganic & medicinal chemistry letters, 1999Co-Authors: Lijun Zhang, Bradford Graves, Paul A Escarpe, Dirk B Mendel, X. Chen, Matthew A. Williams, Ke-yu Wang, Geoff Lawton, Choung U. KimAbstract:1,4,5,6-Tetrahydropyridazine derivative 15 and its C-5 epimer 19, which possessed side chains similar to GS4071, were synthesized via a hetero Diels-Alder reaction, and evaluated as influenza Neuraminidase Inhibitors. Compounds 15 and 19 exhibited a μM range of influenza Neuraminidase inhibitory activity.
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Structure−Activity Relationship Studies of Novel Carbocyclic Influenza Neuraminidase Inhibitors
Journal of medicinal chemistry, 1998Co-Authors: Choung U. Kim, W G Laver, Paul A Escarpe, Dirk B Mendel, X. Chen, Lijun Zhang, Matthew A. Williams, Willard Lew, Raymond C. StevensAbstract:A series of influenza Neuraminidase Inhibitors with the cyclohexene scaffold containing lipophilic side chains have been synthesized and evaluated for influenza A and B Neuraminidase inhibitory activity. The size and geometry of side chains have been modified systematically in order to investigate structure-activity relationships of this class of compounds. The X-ray crystal structures of several analogues complexed with Neuraminidase revealed that the lipophilic side chains bound to the hydrophobic pocket consisted of Glu276, Ala246, Arg224, and Ile222 of the enzyme active site. The structure-activity relationship studies of this series have also demonstrated remarkably different inhibitory potency between influenza A and B Neuraminidase. This indicated that the lipophilic side chains had quite different hydrophobic interactions with influenza A and B Neuraminidase despite their complete homology in the active site. Influenza B Neuraminidase appeared to be much more sensitive toward the increased steric bulkiness of Inhibitors compared to influenza A Neuraminidase. From the extensive structure-activity relationship investigation reported in this article, GS 4071 emerged as one of the most potent influenza Neuraminidase Inhibitors against both influenza A and B strains.
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structure activity relationship studies of novel carbocyclic influenza Neuraminidase Inhibitors
Journal of Medicinal Chemistry, 1998Co-Authors: Choung U. Kim, W G Laver, Paul A Escarpe, Dirk B Mendel, X. Chen, Lijun Zhang, Matthew A. Williams, Willard Lew, Raymond C. StevensAbstract:A series of influenza Neuraminidase Inhibitors with the cyclohexene scaffold containing lipophilic side chains have been synthesized and evaluated for influenza A and B Neuraminidase inhibitory activity. The size and geometry of side chains have been modified systematically in order to investigate structure-activity relationships of this class of compounds. The X-ray crystal structures of several analogues complexed with Neuraminidase revealed that the lipophilic side chains bound to the hydrophobic pocket consisted of Glu276, Ala246, Arg224, and Ile222 of the enzyme active site. The structure-activity relationship studies of this series have also demonstrated remarkably different inhibitory potency between influenza A and B Neuraminidase. This indicated that the lipophilic side chains had quite different hydrophobic interactions with influenza A and B Neuraminidase despite their complete homology in the active site. Influenza B Neuraminidase appeared to be much more sensitive toward the increased steric bulkiness of Inhibitors compared to influenza A Neuraminidase. From the extensive structure-activity relationship investigation reported in this article, GS 4071 emerged as one of the most potent influenza Neuraminidase Inhibitors against both influenza A and B strains.
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A new series of C3-aza carbocyclic influenza Neuraminidase Inhibitors: synthesis and inhibitory activity
Bioorg Med Chem Lett, 1998Co-Authors: Wilbur Lew, B J Graves, W G Laver, H. Wu, Paul A Escarpe, Dirk B Mendel, X. Chen, C. U. KimAbstract:The synthesis and influenza Neuraminidase inhibitory activity of a new series of C3-aza carbocyclic Neuraminidase Inhibitors are described. Analogues 3c and 3j, bearing a 3-pentyl group, exhibit influenza A inhibitory activities comparable to that of 1.