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Oseltamivir

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https://www.readbyqxmd.com/read/28433777/design-and-expeditious-synthesis-of-organosilanes-as-potent-antivirals-targeting-multidrug-resistant-influenza-a-viruses
#1
Yanmei Hu, Yuanxiang Wang, Fang Li, Chunlong Ma, Jun Wang
The efficacy of current influenza vaccines and small molecule antiviral drugs is curtailed by the emerging of multidrug-resistant influenza viruses. As resistance to the only FDA-approved oral influenza antiviral, oseltamivir (Tamiflu), continues to rise, there is a clear need to develop the next-generation of antiviral drugs. Since more than 95% of current circulating influenza A viruses carry the S31N mutation in their M2 genes, the AM2-S31N mutant proton channel represents an attractive target for the development of broad-spectrum antivirals...
April 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28417640/combinations-of-l-n-g-monomethyl-arginine-and-oseltamivir-against-pandemic-influenza-a-virus-infections-in-mice
#2
Donald F Smee, Ashley Dagley, E B Tarbet
L-N(G)-monomethyl-arginine (L-NMMA) is an experimental compound that suppresses nitric oxide production in animals. The compound was combined with oseltamivir to treat lethal influenza A/California/04/2009 (H1N1) pandemic virus infections in mice. Treatments were given twice a day for five days starting 4 h (oseltamivir, by oral gavage) or three days (L-NMMA, by intraperitoneal route; corresponding to the time previously reported for nitric oxide induction in the animals) after infection. Low doses of oseltamivir were used in order to demonstrate synergy or antagonism...
April 2017: Antiviral Chemistry & Chemotherapy
https://www.readbyqxmd.com/read/28410396/evolution-of-the-neuraminidase-gene-of-seasonal-influenza-a-and-b-viruses-in-thailand-between-2010-and-2015
#3
Nipaporn Tewawong, Preeyaporn Vichiwattana, Sumeth Korkong, Sirapa Klinfueng, Nungruthai Suntronwong, Thanunrat Thongmee, Apiradee Theamboonlers, Sompong Vongpunsawad, Yong Poovorawan
The neuraminidase inhibitors (NAIs) oseltamivir and zanamivir are commonly used for the treatment and control of influenza A and B virus infection. However, the emergence of new influenza virus strains with reduced susceptibility to NAIs may appear with the use of these antivirals or even naturally. We therefore screened the neuraminidase (NA) sequences of seasonal influenza virus A(H1N1), A(H1N1)pdm09, A(H3N2), and influenza B virus strains identified in Thailand for the presence of substitutions previously reported to reduce susceptibility to NAIs...
2017: PloS One
https://www.readbyqxmd.com/read/28401407/molecular-analysis-of-amantadine-resistant-influenza-a-h1n1-pdm09-virus-isolated-from-slum-dwellers-of-dhaka-bangladesh
#4
Mozibur Rahman, Sheikh Ariful Hoque, Mohammad Ariful Islam, Sabita Rezwana Rahman
Influenza is a highly contagious viral infection associated with excessive hospitalizations and deaths throughout the world. Continuous antigenic shift and drift is not only responsible for this devastating effect of influenza but also causes ineffectiveness of antiviral drugs and vaccines. In this study, we investigated the effectiveness of ribavirin, oseltamivir, and amantadine drugs in vitro against nine influenza A isolates collected during June 2012-August 2013 from different slums in Dhaka city. The effectiveness of these drugs was determined by measuring the inhibition of virus-induced cytopathic effect on MDCK cells through MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)...
April 11, 2017: Virus Genes
https://www.readbyqxmd.com/read/28393840/antiviral-activity-of-chlorogenic-acid-against-influenza-a-h1n1-h3n2-virus-and-its-inhibition-of-neuraminidase
#5
Yue Ding, Zeyu Cao, Liang Cao, Gang Ding, Zhenzhong Wang, Wei Xiao
Lonicera japonica Thunb, rich in chlorogenic acid (CHA), is used for viral upper respiratory tract infection treatment caused by influenza virus, parainfluenza virus, and respiratory syncytial virus, ect in China. It was reported that CHA reduced serum hepatitis B virus level and death rate of influenza virus-infected mice. However, the underlying mechanisms of CHA against the influenza A virus have not been fully elucidated. Here, the antiviral effects and potential mechanisms of CHA against influenza A virus were investigated...
April 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28385598/discovery-of-acylguanidine-oseltamivir-carboxylate-derivatives-as-potent-neuraminidase-inhibitors
#6
Zhaoliang Li, Yanchun Meng, Shengtao Xu, Wang Shen, Zhaoqing Meng, Zhenzhong Wang, Gang Ding, Wenzhe Huang, Wei Xiao, Jinyi Xu
In search of novel anti-influenza agents with higher potency, a series of acylguanidine oseltamivir carboxylate analogues were synthesized and evaluated against influenza viruses (H1N1 and H3N2) in vitro. The representative compounds with strong inhibitory activities (IC50 <40nM) against neuraminidase (NA) were further tested against the NA from oseltamivir-resistant strain (H259Y). Among them, compounds 9 and 17 were potent NA inhibitors that exhibited a 5 and 11-fold increase in activity comparing with oseltamivir carboxylate (2, OC) against the H259Y mutant, respectively...
May 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28356526/chimeric-hemagglutinin-constructs-induce-broad-protection-against-influenza-b-virus-challenge-in-the-mouse-model
#7
Megan Ermler, Ericka Kirkpatrick, Weina Sun, Rong Hai, Fatima Amanat, Veronika Chromikova, Peter Palese, Florian Krammer
Seasonal influenza virus epidemics represent a significant public health burden. Approximately 25% of all influenza virus infections are caused by type B viruses and these infections can be severe, especially in children. Current influenza virus vaccines are an effective prophylaxis against infection but are impacted by rapid antigenic drift which can lead to mismatches between vaccine strains and circulating strains. Here, we describe a broadly protective vaccine candidate based on chimeric hemagglutinins consisting of globular head domains from exotic influenza A viruses and stalk domains from influenza B viruses...
March 29, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28346272/influenza-in-children
#8
Janienne Kondrich, Michele Rosenthal
PURPOSE OF REVIEW: We review the current information and evidence available on the global burden of disease in the pediatric population, clinical presentation and complications, testing, treatment, and immunization. RECENT FINDINGS: In addition to multiple other risk factors for influenza complications, children with neurologic and neuromuscular disorders are significantly higher risk for serious complications. In practice, there is no lower age limit for children with influenza who can be treated with oseltamivir...
March 24, 2017: Current Opinion in Pediatrics
https://www.readbyqxmd.com/read/28337082/pharmacokinetics-of-peramivir-in-an-adolescent-patient-receiving-continuous-venovenous-hemodiafiltration
#9
Ryan C Dillon, Robert Witcher, Jeffrey J Cies, Wayne S Moore, Arun Chopra
Critically ill patients requiring renal replacement therapy commonly experience pharmacokinetic alterations. This case report describes the pharmacokinetics of peramivir (Rapivab, BioCryst Pharmaceuticals, Inc, Durham, NC), the first US Food and Drug Administration-approved intravenous neuraminidase inhibitor for the treatment of influenza, in an adolescent patient receiving continuous renal replacement therapy (CRRT). A 49.5-kg, 17-year-old Caucasian female presented with fever, cough, and persistent hypoxia...
January 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#10
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28331290/effects-of-dexamethasone-coadministered-with-oseltamivir-on-the-pharmacokinetics-of-oseltamivir-in-healthy-volunteers
#11
Kyungho Jang, Min-Kyoung Kim, Jaeseong Oh, SeungHwan Lee, Joo-Youn Cho, Kyung-Sang Yu, Tai Kiu Choi, Sang-Hyuk Lee, Kyoung Soo Lim
PURPOSE: Oseltamivir is widely used in the treatment and prophylaxis of influenza A and B viral infections. It is ingested as an oral prodrug that is rapidly metabolized by carboxylesterase 1 (CES1) to its active form, oseltamivir carboxylate. Dexamethasone is also used in the treatment of acute respiratory distress syndrome, a severe complication of influenza; however, its influence on the pharmacokinetics (PK) of oseltamivir is controversial. The aim of this study was to investigate the effects of coadministering oseltamivir and dexamethasone on the PK of oseltamivir in healthy volunteers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28327126/characterization-and-mechanisms-of-anti-influenza-virus-metabolites-isolated-from-the-vietnamese-medicinal-plant-polygonum-chinense
#12
Thu Thi Tran, Meehyein Kim, Yejin Jang, Hye Won Lee, Hoa Thi Nguyen, Thanh Ngoc Nguyen, Hae Woong Park, Quang Le Dang, Jin-Cheol Kim
BACKGROUND: Polygonum chinense Linn. is a common medicinal plant in Southeast Asia and has been used in traditional medicine in Vietnam. The plant contains phytochemicals with various biological properties; however, its antiviral effect has not yet been demonstrated. This study was aimed to evaluate the anti-influenza virus activity of crude extracts of P. chinense, to characterize antiviral metabolites therefrom and to investigate their mechanisms of antiviral action. METHODS: The methanol (MeOH) extract and organic solvent layers of P...
March 21, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28315686/crystal-structure-of-the-catalytic-domain-of-clostridium-perfringens-neuraminidase-in-complex-with-a-non-carbohydrate-based-inhibitor-2-cyclohexylamino-ethanesulfonic-acid
#13
Youngjin Lee, Hyung-Seop Youn, Jung-Gyu Lee, Jun Yop An, Kyoung Ryoung Park, Jung Youn Kang, Young Bae Ryu, Mi Sun Jin, Ki Hun Park, Soo Hyun Eom
Anti-bacterial and anti-viral neuraminidase agents inhibit neuraminidase activity catalyzing the hydrolysis of terminal N-acetylneuraminic acid (Neu5Ac) from glycoconjugates and help to prevent the host pathogenesis that lead to fatal infectious diseases including influenza, bacteremia, sepsis, and cholera. Emerging antibiotic and drug resistances to commonly used anti-neuraminidase agents such as oseltamivir (Tamiflu) and zanamivir (Relenza) have highlighted the need to develop new anti-neuraminidase drugs...
March 15, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28315128/rapid-influenza-diagnostic-tests-improve-suitability-of-antiviral-treatment-in-hospitalized-children
#14
Aneta Nitsch-Osuch, Ernest Kuchar, Izabela Gołębiak, Krzysztof Kanecki, Patryk Tarka, Lidia Brydak
Influenza may have a complicated course in young children. The aim of the study was to analyze the suitability of influenza treatment among children younger than 5 years hospitalized due to an influenza-like illness. We conducted a comparison of the treatment among children hospitalized in two consecutive years: 2015, when no rapid influenza diagnostic tests (RIDT) were in use, and 2016, when RIDT were implemented into a routine practice in the pediatric ward. In both seasons, nasopharyngeal swabs were collected and examined with real time qRT-PCR...
March 18, 2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28298229/a-novel-benzo-heterocyclic-amine-derivative-n30-inhibits-influenza-virus-replication-by-depression-of-inosine-5-monophospate-dehydrogenase-activity
#15
Jin Hu, Linlin Ma, Huiqiang Wang, Haiyan Yan, Dajun Zhang, Zhuorong Li, Jiandong Jiang, Yuhuan Li
BACKGROUD: Influenza virus is still a huge threat to the world-wide public health. Host inosine-5'- monophosphate dehydrogenase (IMPDH) involved in the synthesis of guanine nucleotides, is known to be a potential target to inhibit the replication of viruses. Herein, we evaluated antiviral activity of a benzo-heterocyclic amine derivative N30, which was designed to inhibit IMPDH. RESULTS: The results demonstrated that N30 inhibited the replication of H1N1, H3N2, influenza B viruses, including oseltamivir and amantadine resistant strains in vitro...
March 15, 2017: Virology Journal
https://www.readbyqxmd.com/read/28293815/selectivity-improvement-for-spectrofluorimetric-determination-of-oseltamivir-phosphate-in-human-plasma-and-in-the-presence-of-its-degradation-product
#16
Mahmoud A Omar, Sayed M Derayea, Islam M Mostafa
A simple and sensitive spectrofluorimetric method has been developed and validated for determination of oseltamivir phosphate (OSP). The proposed method is based on condensation reaction of the primary amino group of OSP with ninhydrin and phenylacetaldehyde in buffered medium (pH 6.5). The formed yellow fluorescent product exhibits excitation and emission maxima at 390 and 460 nm, respectively. The selectivity improvement of our proposed method is based on the water insolubility of the oseltamivir carboxylic acid (OSC) the active metabolite of OSP, which contains the same primary amino group as OSP but cannot, condensed with ninhydrin and phenylacetaldehyde reagents...
March 14, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28286235/aerosol-administration-increases-the-efficacy-of-oseltamivir-for-the-treatment-of-mice-infected-with-influenza-viruses
#17
Victor H Leyva-Grado, Peter Palese
Oseltamivir is an influenza neuraminidase inhibitor that along with supportive therapy has shown to help critically ill patients infected with H7N9 and H1N1pdm influenza virus strains to recover from disease. The standard of care recommends the administration of oseltamivir via oral route which represents difficulties in patients with gastrointestinal complications. Here we tested the use of aerosol administration of oseltamivir to treat mice infected with influenza A/H7N9 virus or influenza A/H1N1pdm virus and directly compared this approach to the standard of care, oral administration...
June 2017: Antiviral Research
https://www.readbyqxmd.com/read/28279127/in-silico-prediction-of-drug-resistance-due-to-s247r-mutation-of-influenza-h1n1-neuraminidase-protein
#18
Rahul Shubhra Mandal, Samiran Panda, Santasabuj Das
We present here in silico studies on antiviral drug resistance due to a novel mutation of influenza A/H1N1 neuraminidase (NA) protein. Influenza A/H1N1 virus was responsible for a recent pandemic and is currently circulating among the seasonal influenza strains. M2 and NA are the two major viral proteins related to pathogenesis in humans and have been targeted for drug designing. Among them, NA is preferred because the ligand-binding site of NA is highly conserved between different strains of influenza virus...
March 9, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28267329/boronic-acid-modifications-enhance-the-anti-influenza-a-virus-activities-of-novel-quindoline-derivatives
#19
Wei Wang, Ruijuan Yin, Meng Zhang, Rilei Yu, Cui Hao, Lijuan Zhang, Tao Jiang
The unique glycan-binding ability of chemically synthesized boronic acid derivatives makes them emerging candidates for developing anti-influenza A virus (IAV) drugs. Herein we report the synthesis and the anti-IAV activities of three series of novel boronic acid-modified quindoline derivatives both in vitro and in vivo. Boronic acid-modified compounds 6a and 7a effectively prevented the entry of virus RNP into the nucleus, reduced virus titers in IAV infected cells, and also inhibited the activity of viral neuraminidase...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28246106/neuraminidase-inhibitors-during-pregnancy-and-risk-of-adverse-neonatal-outcomes-and-congenital-malformations-population-based-european-register-study
#20
Sophie Graner, Tobias Svensson, Anna-Belle Beau, Christine Damase-Michel, Anders Engeland, Kari Furu, Anders Hviid, Siri Eldevik Håberg, Ditte Mølgaard-Nielsen, Björn Pasternak, Helle Kieler
Objective To evaluate the possible effects of exposure to neuraminidase inhibitors during embryo-fetal life with respect to adverse neonatal outcomes and congenital malformations.Design Population based multinational observational cohort study and meta-analysis.Setting National registers covering information on maternal healthcare, births, and prescriptions in Denmark, Norway, and Sweden and the EFEMERIS database from the Haute-Garonne district in France.Participants All women together with their singleton infants born between 1 January 2008 and 31 December 2010...
February 28, 2017: BMJ: British Medical Journal
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