variable susceptibility
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Author(s):  
Daniela Visaggio ◽  
Emanuela Frangipani ◽  
Sarah Hijazi ◽  
Mattia Pirolo ◽  
Livia Leoni ◽  
...  

Acta Tropica ◽  
2021 ◽  
Vol 224 ◽  
pp. 106129
Author(s):  
Nilton Barnabé Rodrigues ◽  
Luís Eduardo Martinez Villegas ◽  
Ana Paula Marques Duarte ◽  
Alessandra Silva Orfanó ◽  
Breno dos Anjos Costa ◽  
...  

2021 ◽  
Author(s):  
Christina Tzitzoglaki ◽  
Anja Hoffmann ◽  
Andreea Turcu ◽  
Christos Liolios ◽  
Patrick Schmerer ◽  
...  

One challenge facing anti-influenza drug development is the heterogeneity of the circulating influenza A viruses, which comprise several strains with variable susceptibility to antiviral drugs. Viruses bearing the S31N mutant of the M2, such as the pandemic 2009 H1N1 and seasonal H3N2, as well as other mutants (L26F, V27A, A30T, G34E) are resistant to amantadine class of drugs. Here, we synthesized and tested many of the second generation amantadine - aryl conjugates, against the WT M2 and all the M2 amantadine resistant strains, i.e. L26F, V27A, S31N, A30T, G34E generated from WSN/33 (S31N) virus. We identified many compounds that are dual in vitro M2 WT and L26F virus inhibitors. Furthermore, few of them (21, 32, 33), having a rimantadine or diamantadine or 4-(1-adamantyl)aniline instead of amantadine in the conjugate, were in vitro inhibitors against M2 WT, L26F and S31N while one of them inhibited also the A30T virus. The electrophysiology (EP) experiments showed that these compounds blocked significantly M2 WT, L26F or even M2 V27A channels but not the M2 S31N. The observation that adamantane variants and derivatives inhibit multiple M2 mutant virus replication in cell culture, without blocking M2 channel-mediated proton current in EP is not uncommon, underlying a mechanism of antiviral activity that has not been identified.


2021 ◽  
Author(s):  
Margaret Kandel ◽  
Colin Phillips

Although reflexive–antecedent agreement shows little susceptibility to number attraction in comprehension, prior production research using the preamble-completion paradigm has demonstrated attraction for both verbs and anaphora. In four production experiments, we compared number attraction effects on subject–verb and reflexive–antecedent agreement using a novel scene-description task in addition to a more traditional preamble elicitation paradigm. While the results from the preamble task align with prior findings, the more naturalistic scene description task produced the same contrast observed in comprehension, with robust verb attraction but minimal anaphor attraction. In addition to analyzing agreement error distributions, we also analyzed the production time-course of participant responses, finding timing effects that pattern with error distributions, even when no error is present. The results suggest that production agreement processes show similar profiles to comprehension processes. We discuss potential sources of variable susceptibility to agreement attraction, suggesting that differences may arise from the time-course of information processing across tasks and linguistic dependencies.


2020 ◽  
Vol 11 ◽  
Author(s):  
Margot Paulin ◽  
Cécile Miot-Sertier ◽  
Lucie Dutilh ◽  
Clément Brasselet ◽  
Cédric Delattre ◽  
...  

2019 ◽  
Vol 184 (6) ◽  
pp. 759-773 ◽  
Author(s):  
Limin Yao ◽  
Hong Wang ◽  
Zhe Wan ◽  
Ruoyu Li ◽  
Jin Yu

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (01) ◽  
pp. 25-31
Author(s):  
B. V. Dhokchawle ◽  
S. Asirvatham ◽  
S. J. Tauro ◽  
B. A. Bhandari ◽  
S. S. Babu ◽  
...  

The present works deals with simple and efficient method of improving therapeutic efficacy of naproxen by retarding gastrointestinal side effects through masking of carboxylic group chemically. This is achieved by synthesis of ester prodrugs of naproxen with various naturally available antioxidants; menthol, thymol, eugenol, guiacol, vanillin and sesamol by the dicyclohexyl carbodiimide (DCC) coupling method. The title compounds are purified and characterized by spectral data. Further, their partition coefficients have been determined and hydrolytic studies have been performed. The synthesized compounds are more lipophilic compared to the parent moieties and are stable in acidic environment, which is a prerequisite for their oral absorption. Under gastric as well as intestinal pH conditions, these prodrugs showed variable susceptibility towards hydrolysis. The title compounds when evaluated for anti-inflammatory and analgesic activities showed improvement over the parent drug. Prodrugs were also found to be significantly less ulcerogenic then parent drugs.


2018 ◽  
Vol 24 (7) ◽  
pp. 1031-1039 ◽  
Author(s):  
Natalia Gómez-Casanova ◽  
Alberto Bellido ◽  
Alejandra Espinosa-Texis ◽  
Rosario Cueva ◽  
Toni Ciudad ◽  
...  

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