Search results for "44"

In Vitro Modulation of P-Glycoprotein Activity by Euphorbia intisy Essential Oil on Acute Myeloid Leukemia Cell Line HL-60R

2021

Euphorbia species have a large spectrum of traditional medicinal uses. We tested the biological activities of the essential oil (EO) of Euphorbia intisy Drake in an acquired multidrug resistance leukemia model to assess whether the EO obtained by hydrodistillation of stems was able to reverse the resistant phenotype. HL-60R cell lines are characterized by the overexpression of P-glycoprotein (P-gp), inhibitors of apoptosis proteins (IAPs) and constitutive expression of NF-κB. EO chemical composition was determined by GC/MS analysis

Spectral characteristics of 5-hydroxymethylfurfural as a related substance in medicinal products containing glucose

2019

Objectives: To study 5-hydroxymethylfurfural (5-HMF) spectral characteristics aiming at their future application in analytical procedures and their validation for the determination of 5-HMF in liquid products containing glucose after sterilization.Method: Direct spectrophotometric method for the determination of 5-HMF using the molar absorption coefficient at the absorption maximum (284 nm).Results and discussion: aqueous 5-HMF solutions have strong absorption in the ultraviolet range below 310 nm and give two absorption maxima at wavelengths of 229–230 nm and 284 nm. An excellent linear relationship between absorbance and 5-HMF concentration was observed in the concentration range of 2.0–1…

Analytical Research Based on the Use of Low Cost Instrumentation

2019

Erratum: Mangas-Sanjuán, V.; et al. Assessment of the Inter-Batch Variability of Microstructure Parameters in Topical Semisolids and Impact on the De…

2020

Demonstration of similar microstructure is essential for demonstrating the equivalence of generic topical products since the microstructure of semisolids may affect the drug release. The objective of this study was to compare the microstructure-defining physical parameters of different batches of a reference ointment containing calcipotriol and betamethasone (Daivobet 50 µg/0.5 mg/g) in order to define the acceptance range that allows concluding equivalence between these batches. Being batches of the same reference product, they are expected to be clinically equivalent and possess similar microstructure. The 90% confidence intervals for the test/reference ratio of these physical parameters …

X-Ray characterization of 3-methyl-6,8-di(2-pyridyl)-[1,2,3]triazolo[5',1':6,1]pyrido[2,3-d]pyrimidine

2005

Abarca Gonzalez, Belen. Belen.Abarca@uv.es ; Ballesteros Campos, Rafael, Rafael.Ballesteros@uv.es ; Chadlaoui, Mimoun, michad@alumni.uv.es ; Ramirez de Arellano Sanchez, Maria del Carmen, Ramirezdearellano@uv.es

From Overstoichiometric to Substoichiometric Enantioselective Protonation with 2-Sulfinyl Alcohols: A View in Perspective

2005

A general study of the enantioselective protonation of prochiral enolates with 2-sulfinyl alcohols is reported. The modification of reaction conditions to reduce drastically the amount of chiral proton source needed to obtain a good enantiomeric excess is reported. The effects of the different factors controlling the stereoselectivity are clearly established. Different protocols for enolate generation are compared.

Synthesis of alkyl-5,8-dimethyl-6-phenyl-5,6-dihydropyrazolo[3,4-f] [1,2,3,5]tetrazepin-4(3H)-ones of pharmaceutical interest

2006

The multistep synthesis of two pyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one derivatives, a new class of fused 1,2,3,5-tetrazepinones with potential antiproliferative activity, has been carried out. Owing to the instability of the above compounds, the last step of the synthesis was performed at -5/0 degrees C. The obtained tetrazepinones, when allowed to stand at r.t. for 24 h, afforded quantitatively 1-phenyl-3,6-dimethylpyrazolo [3,4-d][1,2,3] triazole.

Triazolopyridines 23. Synthesis of 5,5'-bi[1,2,3]triazolo[5,1-a]isoquinoline

2003

5,5'-Bi[1,2,3]triazolo[5,1-a]isoquinoline 6 has been synthesised from [1,2,3]triazolo[5,1-a] isoquinoline 5 by four procedures, dimerisation by LDA, Stille and Suzuki self-coupling reactions, and Suzuki cross-coupling reaction. The last is the best. Compound 6 gives 1,1'bi(acetoxymethyl)-3,3'-biisoquinoline 10 by triazolo ring opening by acetic acid.

Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor

2012

Derivatives of the new ring system 1,4-dihydropyrazolo[4,3-c][1,2,6] benzothiadiazocin-11(10H)one 5,5-dioxide were synthesized in five or six steps in 57-66% overall yields and tested as COX inhibitors.

Synthesis of substituted isoindolo[2,1-a]quinoxalin-6-yl–amino and 6-imino-5-yl thiourea derivatives

2014

A series of substituted 1-(5-bromopyridin-2-yl)-3-[2-(isoindolo[2,1-a]quinoxalin-6- ylamino)ethyl]thiourea and 1-(5-bromopyridin-2-yl)-3-[2-(6-iminoisoindolo[2,1-a]quinoxalin- 5(6H)-yl)ethyl]thiourea derivatives were prepared in good yields (63-85%) by reaction between the corresponding amino compounds with 5-bromo-2-isothiocyanatopyridine. All thiourea derivatives, tested for inhibition of HIV-1 RT, showed no significant antiviral activity.