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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. Source

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. Source

Benziane H.,Laboratoire Of Chimie Therapeutique | Karfo R.,Service de Pharmacie Hospitaliere | Siah S.,Service des Brules et Chirurgie Plastique | Taoufik J.,Laboratoire Of Chimie Therapeutique
Annals of Burns and Fire Disasters | Year: 2011

Infection has long been the main cause of mortality in severely burned patients. The aim of this work is to assess the prescription of antibiotics in our Burns and Plastic Surgery Department in relation to the recommendations of the manufacturers. A summary is provided of the specific features of these products. Patients hospitalized in the Mohammed V Military Teaching Hospital, Rabat, Morocco, during the period January 2008/May 2009 and treated with antibiotics were considered. This retrospective study concerned 227 nominal medical prescriptions of antibiotics to 41 patients: 70% of the prescriptions were nondocumented. The commonest method of administration was by injection (89%). Various groups of therapeutic drugs were used: betalactamines (65%), glycopeptides (10.5%), aminosides (9%), quinolones (7%), and colistin (4.3%), plus 4.2% from other groups (metronidazole 500 mg, perfusion; fluconazol 100 mg/50 ml, injection; rifampicin 600 mg, perfusion; silver sulphadiazine, 2% fusidic acid cream). A total of 227 nominal medical prescriptions were analysed: the dosages and counter-indications were correctly respected. Three drug interactions were recorded (fluconazol-rifampicin, fluconazol-Saccharomyces boulardii, amikacin-vancomycin). This study shows the importance of the pharmaceutical analysis of prescriptions for antibiotics used in a burns unit, which are active but therefore very toxic. Source

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. Source

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. Source

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