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1.
Data Brief ; 30: 105577, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32577438

RESUMO

[This corrects the article DOI: 10.1016/j.dib.2019.103828.].

2.
Data Brief ; 23: 103828, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31372464

RESUMO

In this data article, we will present the data coming from 3D Inertial Measurement Unit (3-accelerometers and 3-gyroscopes sensors) mounted on the motorcycle collected during a motorcycle's falls experiments. Developing a motorcycle's fall events detection algorithms is a very challenging task because the motorcycle falling is multi-factorial and is strongly influenced by many unknown factors. To solve this issue, one solution can be to use a data-set collected during controlled experiments, knowing that the real motorcycle falls cannot be replicated, a stuntman can be chosen to be as close to reality as possible. The experiments have been conducted based on predefined scenarios such as: fall in a curve, fall on a slippery straight road section, fall with leaning of the motorcycle ''intentional manoeuvre'' and fall in a roundabout. These scenarios have been designed based on realistic falls. Other experiments have been conducted under different extreme driving situations. These extreme manoeuvres were carried out on track by professional riders. The purpose of performing these manoeuvres was to obtain a dataset describing the limit handling behaviour.

3.
J Pharm Biomed Anal ; 74: 273-83, 2013 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-23245261

RESUMO

This paper focuses on implementing a design space approach and on the critical process parameters (CPPs) to consider when applying the Quality by Design (QbD) concepts outlined in ICH Q8(R2), Q9 and Q10 to analytical method development and optimization for three chiral compounds developed as modulators of small conductance calcium-activated potassium (SK) channels. In this sense, an HPLC method using a polysaccharide-based stationary phase containing a cellulose tris (4-chloro-3-methylphenylcarbamate) chiral selector in polar organic solvent chromatography mode was considered. The effects of trifluoroacetic acid (TFA) and n-hexane concentration in an acetonitrile (MeCN) mobile phase were investigated under a wide range of column temperatures. Good correlations were found between the observed data obtained after using a central composite design and the expected chromatographic behaviours predicted by applying the design of experiments-design space (DoE-DS) methodology. The critical quality attribute represented here by the separation criterion (S(crit)) allowed assessing the quality of the enantioseparation. Baseline separation for the compounds of interest in an analysis time of less than 20 min was possible due to the original and powerful tools applied which facilitated an enhanced method comprehension. Finally, the advantage of the DoE-DS approach resides in granting the possibility to concurrently assess robustness and identify the optimal conditions which are compound dependent.


Assuntos
Desenho de Equipamento/métodos , Solventes/análise , Solventes/química , Acetonitrilas/análise , Acetonitrilas/química , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida de Alta Pressão/normas , Dietilaminas/análise , Dietilaminas/química , Desenho de Equipamento/normas , Estereoisomerismo , Ácido Trifluoracético/análise , Ácido Trifluoracético/química
4.
Bioorg Med Chem Lett ; 21(22): 6756-9, 2011 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-21978678

RESUMO

A structure-activity relationship study of N-methyl-laudanosine, a SK channel blocker, has indicated that the 6,7-dimethoxy group could be successfully replaced by a hydrophobic moiety such as an isopropyl substituent in position 8 of the isoquinoline ring. In the present study, bis-(8-isopropyl-isoquinolinium) derivatives (2a-e) were synthesized and tested for their affinity for cloned SK2 and SK3 channels in comparison with their 6,7-dimethoxy analogues (4a-f). Several ligands were investigated, both in flexible (propyl, butyl and pentyl) and rigid (m- or p-xylyl) series, the m-xylyl derivative (2d) having the best profile in terms of affinity and selectivity for SK3/SK2 channels. Molecular studies showed that the optimal conformation of compound 2d fits well with our SK pharmacophore model.


Assuntos
2-Propanol/química , 2-Propanol/farmacologia , Apamina/metabolismo , Isoquinolinas/química , Isoquinolinas/farmacologia , Canais de Potássio Ativados por Cálcio de Condutância Baixa/metabolismo , 2-Propanol/síntese química , Sítios de Ligação , Células HEK293 , Humanos , Isoquinolinas/síntese química , Ligantes , Modelos Moleculares , Ligação Proteica , Ensaio Radioligante , Canais de Potássio Ativados por Cálcio de Condutância Baixa/química , Relação Estrutura-Atividade
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