Laboratoire Of Chimie Therapeutique

Witry-lès-Reims, France

Laboratoire Of Chimie Therapeutique

Witry-lès-Reims, France
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Ghinet A.,University of Lille Nord de France | Ghinet A.,Heilongjiang University | Farce A.,University of Lille Nord de France | Farce A.,Laboratoire Of Chimie Therapeutique | And 11 more authors.
Medicinal Chemistry | Year: 2012

In order to predict the antioxidant activity of 7 polycyclic lactams, a two dimensional quantitative-structure activity relationships (2D-QSAR) study based on a 5-descriptor model was performed. The synthetic compounds built from a condensed lactam scaffold were screened for their abilities to inhibit the autoxidation of pyrogallol, a superoxide anion radical-dependent process. The ketone 2 (8,9-dihydro-7H-benzo[de]pyrrolo[1,2-a]quinoline-7,10(7aH)-dione) exhibited the most potent antioxidant activity in vitro. The oxidation mechanism was proved by the isolation and characterization of alcohol 5 formed in the reaction of ketone 2 with dissolved oxygen in methanol. © 2012 Bentham Science Publishers.


Ait El Cadi M.,Laboratoire Of Pharmacologie Et Of Toxicologie | Makram S.,Laboratoire Of Pharmacologie Et Of Toxicologie | Ansar M.,Laboratoire Of Chimie Therapeutique | Khabbal Y.,Laboratoire Of Pharmacologie Et Of Toxicologie | And 4 more authors.
Annales Pharmaceutiques Francaises | Year: 2012

Zygophylle or . Zygophyllum gaetulum Emberger and. Maire is a Moroccan medicinal plant which has been used as an anti-inflammatory, antidiabetic, antispasmodic and antidiarrheic. The present study was carried out to study and compare the anti-inflammatory effect of ethanolic extract with aqueous extract of . Z. . gaetulum. Organic extract of . Z. . gaetulum was obtained in soxhlet apparatus. Aqueous extract was obtained by infusion. The Wistar albinos rats of either sex weighing 200-300. g aged 2-3 months were used for this experiment. The rats were housed under standard environmental conditions. The anti-inflammatory activity was estimated by measuring the oedema induced by carragenin according to the method of Winter and al. Ethanolic extract of . Z. . gaetulum reduced the increase of the paw volume with a percentage of inhibition of 46% (. p<. 0.01), this percentage was 47.48% (. p<. 0.01) with aqueous extract. The inhibition decrease in time, it arrived to 39% (. p<. 0.01) at the sixth hour while the activity of aqueous extract decrease a lot. In conclusion, . Z. . gaetulum is an interesting plant which the aqueous and éthanolic extracts could be used scientifically in the treatment of inflammation. © 2011 Elsevier Masson SAS.


Montanha J.A.,Federal University of Rio Grande do Sul | Schenkel E.P.,Federal University of Santa Catarina | Moellerke P.,Federal University of Rio Grande do Sul | Roehe P.M.,Federal University of Rio Grande do Sul | And 2 more authors.
Latin American Journal of Pharmacy | Year: 2013

A clerodane diterpene was isolated from the aerial parts of Baccharis patens Baker, which was identified as 2〈-hidroxy-hardwickiic acid by spectroscopic methods. Using the Yield reduction assay, this compound was active against herpes simplex virus type 1 (HSV-1) at 0.94, 0.47, and 0.23 mM, but did not show any virucidal activity.


Harhar H.,Mohammed V University | Gharby S.,Mohammed V University | Monfalouti H.E.,Mohammed V University | Monfalouti H.E.,Laboratoire Of Chimie Therapeutique | And 2 more authors.
Natural Product Communications | Year: 2010

The composition of the essential oil from the fresh and dried pulp of the fruit of Argania spinosa (Skeels) L. has been studied. Camphor was the major component in both oil types, but in addition, the fresh fruit oil had significant amounts of 1,8-cineole, endo-borneol, and 2-(4-methylcyclohex-3- enyl)-propan-2-ol., and the dried pulp oil 3,5-dimethyl-4-ethylidene-cyclohex-2- ene-1-one, 1,8-cineole, and 2-methylbutanoic acid. The presence of camphor and 1,8-cineole in argan fruit essential oil suggests that it could be used locally as an insect repellent, offering an output for argan fruit pulp that is at present a waste product.


Samadi A.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Soriano E.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Revuelta J.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Valderas C.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | And 11 more authors.
Bioorganic and Medicinal Chemistry | Year: 2011

The synthesis, structure, theoretical and experimental in vitro antioxidant properties using the DPPH, ORAC, and benzoic acid, as well as preliminary in vitro pharmacological activities of (Z)-α-aryl and heteroaryl N-alkyl-nitrones 6-15, 18, 19, 21, and 23, is reported. In the in vitro antioxidant activity, for the DPPH radical test, only nitrones bearing free phenol groups gave the best RSA (%) values, nitrones 13 and 14 showing the highest values in this assay. In the ORAC analysis, the most potent radical scavenger was nitrone indole 21, followed by the N-benzyl benzene-type nitrones 10 and 15. Interestingly enough, the archetypal nitrone 7 (PBN) gave a low RSA value (1.4%) in the DPPH test, or was inactive in the ORAC assay. Concerning the ability to scavenge the hydroxyl radical, all the nitrones studied proved active in this experiment, showing high values in the 94-97% range, the most potent being nitrone 14. The theoretical calculations for the prediction of the antioxidant power, and the potential of ionization confirm that nitrones 9 and 10 are among the best compounds in electron transfer processes, a result that is also in good agreement with the experimental values in the DPPH assay. The calculated energy values for the reaction of ROS (hydroxyl, peroxyl) with the nitrones predict that the most favourable adduct-spin will take place between nitrones 9, 10, and 21, a fact that would be in agreement with their experimentally observed scavenger ability. The in vitro pharmacological analysis showed that the neuroprotective profile of the target molecules was in general low, with values ranging from 0% to 18.7%, in human neuroblastoma cells stressed with a mixture of rotenone/oligomycin-A, being nitrones 18, and 6-8 the most potent, as they show values in the range 24-18.4%. © 2010 Elsevier Ltd. All rights reserved.


Harhar H.,University Mohammeddal | Gharby S.,University Mohammeddal | Gharby S.,Laboratoire Controle Qualite | Kartah B.,University Mohammeddal | And 4 more authors.
Plant Foods for Human Nutrition | Year: 2011

Virgin argan oil, which is harvested from argan fruit kernels, constitutes an alimentary source of substances of nutraceutical value. Chemical composition and oxidative stability of argan oil prepared from argan kernels roasted for different times were evaluated and compared with those of beauty argan oil that is prepared from unroasted kernels. Prolonged roasting time induced colour development and increased phosphorous content whereas fatty acid composition and tocopherol levels did not change. Oxidative stability data indicate that kernel roasting for 15 to 30min at 110°C is optimum to preserve virgin argan oil nutritive properties. © 2011 Springer Science+Business Media, LLC.


Verones V.,Laboratoire Of Chimie Therapeutique | Flouquet N.,Laboratoire Of Chimie Therapeutique | Farce A.,Laboratoire Of Chimie Therapeutique | Carato P.,Laboratoire Of Chimie Therapeutique | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase. © 2010 Elsevier Masson SAS. All rights reserved.


PubMed | University of Yaounde I, Laboratoire Of Chimie Therapeutique and CNRS Laboratory for Therapeutic Innovation
Type: | Journal: Fitoterapia | Year: 2016

As part of our search of new bioactive saponins from Cameroonian medicinal plants, phytochemical investigation of the roots of Albizia glaberrima led to the isolation of three new oleanane-type saponins, named glaberrimosides A-C (1-3). Their structures were established by direct interpretation of their spectral data, mainly HRESIMS, 1D NMR (1H, 13C NMR, and DEPT) and 2D NMR (COSY, ROESY, HSQC and HMBC) as 3-O-[-L-arabinopyranosyl-(1 6)-[-D-glucopyranosyl-(1 2)]--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)-[-d-glucopyranosyl-(1 2)]--D-glucopyranosyl]-oleanolic acid (1), 3-O-[-L-arabinopyranosyl-(1 6)-[-D-glucopyranosyl-(1 2)]--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)--D-glucopyranosyl]-oleanolic acid (2), and 3-O-[-D-glucopyranosyl-(12)--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)-[-D-fucopyranosyl-(1 2)]--D-glucopyranosyl]-oleanolic acid (3). The pro-apoptotic effect of the three saponins was evaluated on three human cell lines (pancreatic carcinoma AsPC-1, hematopoietic monocytic THP-1, and human fibroblast cell line BJ). Saponins 1-3 specifically induced apoptosis of pancreatic carcinoma cell (AsPC-1) in a dose-dependent manner. More interestingly, there were inactive on monocytic (THP-1) and normal human fibroblast (BJ) cell lines.


Garofalo A.,University of Lille Nord de France | Goossens L.,University of Lille Nord de France | Six P.,University of Lille Nord de France | Lemoine A.,University of Lille Nord de France | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

Three series of 6,7-dimethoxyquinazoline derivatives substituted in the 4-position by aniline, N-methylaniline and aryloxy entities, targeting EGFR and VEGFR-2 tyrosine kinases, were designed and synthesized. Pharmacological activities of these compounds have been evaluated for their enzymatic inhibition of VEGFR-2 and EGFR and for their antiproliferative activities on various cancer cell lines. We have studied the impact of the variation in the 4-position substitution of the quinazoline core. Substitution by aryloxy groups led to new compounds which are selective inhibitors of VEGFR-2 enzyme with IC50 values in the nanomolar range in vitro. © 2011 Elsevier Ltd. All rights reserved.


PubMed | Laboratoire Of Chimie Therapeutique
Type: Journal Article | Journal: European journal of medicinal chemistry | Year: 2010

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase.

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