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https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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...
March 7, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28279127/in-silico-prediction-of-drug-resistance-due-to-s247r-mutation-of-influenza-h1n1-neuraminidase-protein
#9
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
#10
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 3 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...
March 7, 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
#11
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
https://www.readbyqxmd.com/read/28240183/influenza-a-virus-nucleoprotein-a-highly-conserved-multi-functional-viral-protein-as-a-hot-antiviral-drug-target
#12
Yanmei Hu, Hannah Sneyd, Raphael Dekant, Jun Wang
Prevention and treatment of influenza virus infection is an ongoing unmet medical need. Each year, thousands of deaths and millions of hospitalizations are attributed to influenza virus infection, which poses a tremendous health and economic burden to the society. Aside from the annual influenza season, influenza viruses also lead to occasional influenza pandemics as a result of emerging or re-emerging influenza strains. Influenza viruses are RNA viruses that exist in quasispecies, meaning that they have a very diverse genetic background...
February 24, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28214542/several-hpept1-transported-drugs-are-substrates-of-the-escherichia-coli-proton-coupled-oligopeptide-transporter-ydgr
#13
Bala K Prabhala, Nanda G Aduri, Mazhar Iqbal, Moazur Rahman, Michael Gajhede, Paul R Hansen, Osman Mirza
Proton-dependent oligopeptide transporters (POTs) are secondary active transporters found in all kingdoms of life. POTs utilize the proton electrochemical gradient for the uptake of nutrient dipeptides and tripeptides. The human POT hPepT1 is known to transport a number of drugs. As part of ongoing studies on substrate specificities of POTs from Escherichia coli, our aim in this study was to investigate whether bacterial POTs could also transport these drugs. For this, we selected the common orally administered drugs sulpiride, bestatin, valacyclovir, ampicillin and oseltamivir, that are all transported by hPepT1...
February 16, 2017: Research in Microbiology
https://www.readbyqxmd.com/read/28205506/prospective-surveillance-of-antiviral-resistance-in-hospitalized-infants-less-than-12-months-of-age-with-a-h3n2-influenza-infection-and-treated-with-oseltamivir
#14
Barbara Rath, Xi Chen, Vera Spies, Susann Muehlhans, Patrick Obermeier, Franziska Tief, Lea Seeber, Katharina Karsch, Jeanette Milde, Heino Skopnik, Brunhilde Schweiger, Susanne C Duwe
BACKGROUND: Infants exhibit elevated influenza virus loads and prolonged viral shedding, which may increase the risk for resistance development, especially in cases of suboptimal exposure to antiviral therapy. METHODS: We performed a prospective surveillance of hospitalized infants undergoing oseltamivir therapy during the 2008-2009 and 2011-2012 influenza seasons at two paediatric hospitals in Germany. A total of 37 infants less than one year of age with laboratory confirmed influenza A(H3N2) infection received oseltamivir as per physician's order for 5 days (2008-2009 season: 2mg/kg BID; 2011-2012 season: 2...
February 16, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28195559/selection-of-multi-drug-resistant-influenza-a-and-b-viruses-under-zanamivir-pressure-and-their-replication-fitness-in-ferrets
#15
Ding Yuan Oh, Jacqueline Panozzo, Sophie Vitesnik, Rubaiyea Farrukee, David Piedrafita, Jennifer Mosse, Aeron C Hurt
BACKGROUND: Intravenous zanamivir has been used to treat patients with severe influenza. Because the majority of cases (including immunocompromised patients) require the drug for an extended period of treatment, there is a higher risk that the virus will develop resistance. Therefore, knowing the possible amino acid substitutions that may arise in recently circulating influenza strains under prolonged zanamivir exposure and their impact on antiviral susceptibility is important. METHODS: Influenza A(H1N1)pdm09, A(H3N2) and B virus were serially passaged under increasing zanamivir pressure in vitro...
February 14, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28188897/survival-biases-lead-to-flawed-conclusions-in-observational-treatment-studies-of-influenza-patients
#16
Martin Wolkewitz, Martin Schumacher
BACKGROUND AND OBJECTIVE: Several observational studies reported that Oseltamivir (Tamiflu) reduced mortality in infected and hospitalized patients. Because of the restriction of observation to hospital stay and time-dependent treatment assignment, such findings were prone to common types of survival bias (length, time-dependent and competing risk bias). METHODS: British hospital data from the Influenza Clinical Information Network (FLU-CIN) study group were used which included 1,391 patients with confirmed pandemic influenza A/H1N1 2009 infection...
February 7, 2017: Journal of Clinical Epidemiology
https://www.readbyqxmd.com/read/28182988/design-in-silico-studies-synthesis-and-in%C3%A2-vitro-evaluation-of-oseltamivir-derivatives-as-inhibitors-of-neuraminidase-from-influenza-a-virus-h1n1
#17
Rocío M Neri-Bazán, Jazmín García-Machorro, David Méndez-Luna, Luis E Tolentino-López, Federico Martínez-Ramos, Itzia I Padilla-Martínez, Leopoldo Aguilar-Faisal, Marvin A Soriano-Ursúa, José G Trujillo-Ferrara, M Jonathan Fragoso-Vázquez, Blanca L Barrón, José Correa-Basurto
Since the neuraminidase (NA) enzyme of the influenza A virus plays a key role in the process of release of new viral particles from a host cell, it is often a target for new drug design. The emergence of NA mutations, such as H275Y, has led to great resistance against neuraminidase inhibitors, including oseltamivir and zanamivir. Hence, we herein designed a set of derivatives by modifying the amine and/or carboxylic groups of oseltamivir. After being screened for their physicochemical (Lipinski's rule) and toxicological properties, the remaining compounds were submitted to molecular and theoretical studies...
January 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28182419/expeditious-lead-optimization-of-isoxazole-containing-influenza-a-virus-m2-s31n-inhibitors-using-the-suzuki-miyaura-cross-coupling-reaction
#18
Fang Li, Yanmei Hu, Yuanxiang Wang, Chunlong Ma, Jun Wang
The existence of multidrug-resistant influenza viruses, coupled with the continuously antigenic shift and antigenic drift of influenza viruses, necessitates the development of the next-generation of influenza antivirals. As the AM2-S31N mutant persists in more than 95% of current circulating influenza A viruses, targeting the AM2-S31N proton channel appears to be a logical and valid approach to combating drug resistance. Starting from compound 1, an isoxazole compound with potent AM2-S31N channel blockage and antiviral activity, in this study we report an expeditious synthetic strategy that allows us to promptly explore the structure-activity relationships of isoxazole-containing AM2-S31N inhibitors...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28179375/quantitative-prediction-of-human-renal-clearance-and-drug-drug-interactions-of-organic-anion-transporter-substrates-using-in-vitro-transport-data
#19
Sumathy Mathialagan, Mary A Piotrowski, David A Tess, Bo Feng, John Litchfiled, Manthena V Varma
Organic anion transporters (OATs) play an important role in the renal secretion of drugs, and their functional change can result in pharmacokinetic variability. In this study, we applied transport rates measured using OAT-transfected human embryonic kidney cells to predict human renal secretory and total renal clearance of 31 diverse drugs. Selective substrates to OAT1 (tenofovir), OAT2 (acyclovir and ganciclovir) and OAT3 (benzylpenicillin, oseltamivir acid) were used to obtain relative activity factors (RAFs) for these individual transporters by relating in vitro transport clearance to in vivo secretory clearance...
February 8, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28176519/-favipiravir-a-new-concept-of-antiviral-drug-against-influenza-viruses
#20
REVIEW
J Reina, N Reina
Favipiravir (T-705) is a new antiviral drug with strong inhibitory activity on RNA-dependent RNA polymerase of most RNA virus genome. All the influenza viruses have been shown fully sensitive to this new antiviral, including genetic strains to neuraminidase inhibitors (oseltamivir) resistance. Its mechanism of action lies in blocking viral replication and induction of lethal mutagenesis which determines the loss of infective activity of influenza viruses. Its activity is particularly intense in the respiratory tract, decreasing the viral load to non-infectious levels...
February 8, 2017: Revista Española de Quimioterapia: Publicación Oficial de la Sociedad Española de Quimioterapia
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