scholarly journals In vivo screening of modified siRNAs for non-specific antiviral effect in a small fish model: number and localization in the strands are important

2012 ◽  
Vol 40 (10) ◽  
pp. 4653-4665 ◽  
Author(s):  
Brian Dall Schyth ◽  
Jesper Bertram Bramsen ◽  
Malgorzata Maria Pakula ◽  
Sekar Larashati ◽  
Jørgen Kjems ◽  
...  
Keyword(s):  
Antiviral Effect ◽  
Small Fish ◽  
In Vivo Screening ◽  
Fish Model

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

1-Acyl-3-cyclooctylguanidines

1980 ◽  
Vol 45 (5) ◽  
pp. 1595-1600 ◽  
Author(s):  
Jaroslav Sluka ◽  
František Šmejkal ◽  
Zdeněk Buděšínský
Keyword(s):  
Influenza Virus ◽  
Herpes Simplex ◽  
Methyl Esters ◽  
Antiviral Effect ◽  
Influenza Virus A

On recation of cyclooctylamine with the sulfate of S-methylisothiourea cyclooctylguanidine was formed which was acylated with the methyl esters of 5-halogeno- and 3,5-dihalogeno-2-alkoxybenzoic acids. The 1-acyl-3-cyclooctylguanidine I-XVII formed were tested for their antiviral effect against the influenza virus A/NWS, A-PR8 and A2 Singapore, and further against the viruses NDV, herpes 2, vaccinia and WEE. In the in vivo test against the influenza virus A2 Singapore and herpes simplex 1-(5-bromo-2-dodecyloxybenzoyl)-3-cyclooctylguanidine is more active and less toxic than cyclooctylamine and 1-cyclooctylguanidine.

Synthesis and In Vivo Screening of Isosteviol Derivatives as New Cardioprotective Agents

2021 ◽  
pp. 113396
Author(s):  
Hanyuan Zhang ◽  
Bo Liu ◽  
Geng Xu ◽  
Chao Xu ◽  
E. Ou ◽  
...  
Keyword(s):  
In Vivo Screening

scholarly journals Internal exposure dynamics drive the Adverse Outcome Pathways of synthetic glucocorticoids in fish

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Luigi Margiotta-Casaluci ◽  
Stewart F. Owen ◽  
Belinda Huerta ◽  
Sara Rodríguez-Mozaz ◽  
Subramanian Kugathas ◽  
...  
Keyword(s):  
Predictive Power ◽  
Adverse Outcome ◽  
Plasma Concentrations ◽  
Internal Exposure ◽  
Adverse Outcome Pathway ◽  
Conceptual Tool ◽  
Fish Model ◽  
Species Specific

Abstract The Adverse Outcome Pathway (AOP) framework represents a valuable conceptual tool to systematically integrate existing toxicological knowledge from a mechanistic perspective to facilitate predictions of chemical-induced effects across species. However, its application for decision-making requires the transition from qualitative to quantitative AOP (qAOP). Here we used a fish model and the synthetic glucocorticoid beclomethasone dipropionate (BDP) to investigate the role of chemical-specific properties, pharmacokinetics, and internal exposure dynamics in the development of qAOPs. We generated a qAOP network based on drug plasma concentrations and focused on immunodepression, skin androgenisation, disruption of gluconeogenesis and reproductive performance. We showed that internal exposure dynamics and chemical-specific properties influence the development of qAOPs and their predictive power. Comparing the effects of two different glucocorticoids, we highlight how relatively similar in vitro hazard-based indicators can lead to different in vivo risk. This discrepancy can be predicted by their different uptake potential, pharmacokinetic (PK) and pharmacodynamic (PD) profiles. We recommend that the development phase of qAOPs should include the application of species-specific uptake and physiologically-based PK/PD models. This integration will significantly enhance the predictive power, enabling a more accurate assessment of the risk and the reliable transferability of qAOPs across chemicals.

scholarly journals Biological activity from indigenous medicinal plants of Mauritius

2005 ◽  
Vol 77 (1) ◽  
pp. 41-51 ◽  
Author(s):  
A. Gurib-Fakim ◽  
H. Subratty ◽  
F. Narod ◽  
J. Govinden-Soulange ◽  
F. Mahomoodally
Keyword(s):  
Medicinal Plant ◽  
Plant Extracts ◽  
Biological Properties ◽  
Pharmacological Properties ◽  
Plant Materials ◽  
In Vivo Screening ◽  
Medicinal Plant Extracts ◽  
Minor Ailments

The Mauritian population has a long tradition in the use of ethno-medicine, and the practice is still strong, especially in the treatment of minor ailments. Such interest stems from an existing culture, and many “tisanes” are still prepared from plant materials and sold in several markets around the island.This paper will focus on the various chemical/biological screening techniques currently being used to evaluate the biological properties of medicinal plant extracts. Particular emphasis will be put on extraction and various screening for biological/pharmacological properties. Due consideration will be given to the pharmacological approaches that utilize different animal models for the in vitro and in vivo screening of medicinal plant extracts.

scholarly journals Comparison of In Vitro and In Vivo Screening Models for Androgenic and Estrogenic Activities

2005 ◽  
Vol 89 (1) ◽  
pp. 173-187 ◽  
Author(s):  
Edwin Sonneveld ◽  
Jacoba A. C. Riteco ◽  
Hendrina J. Jansen ◽  
Bart Pieterse ◽  
Abraham Brouwer ◽  
...  
Keyword(s):  
In Vivo Screening

scholarly journals In Vivo Screening of Hepatocellular Carcinoma Using AC Susceptibility of Anti-Alpha Fetoprotein-Activated Magnetic Nanoparticles

PLoS ONE ◽  
2012 ◽  
Vol 7 (10) ◽  
pp. e46756 ◽  
Author(s):  
Jen-Jie Chieh ◽  
Kai-Wen Huang ◽  
Yang-De Lee ◽  
Herng-Er Horng ◽  
Hong-Chang Yang ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Magnetic Nanoparticles ◽  
Ac Susceptibility ◽  
Alpha Fetoprotein ◽  
In Vivo Screening
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