La douleur physique chez le sujet âgé dément

LILLE2-BU Santé-Recherche (593502101) / SudocPARIS-BIUM (751062103) / SudocSudocFranceF

Lipid-lowering properties of 6-benzoyl-2(3H)-benzothiazolone and structurally related compounds

Fifteen compounds derived from the 2( 3H)-benzothiazolone template with an acyl side-chain in position-6 were evaluated for their lipid-lowering action in mice. Among these compounds, 6-benzoyl-2( 3H)-benzothiazolone was found to be the most potent one both in mice models receiving a hypercholesterolemic diet ( for 15 days) or a standard diet ( for 21 days). 6-Benzoyl-2( 3H)-benzothiazolone compares favorably with fenofibrate, the standard drug, both in terms of HDL-C/Chol ( High Density Lipoprotein-Cholesterol/Total Cholesterol) ratio and absence of liver hepatomegaly

Efficient and selective deprotection method for N-protected 2(3H)-benzoxazolones and 2(3H)-benzothiazolones

Cyclic carbamate flanked with heterocyclic or aliphatic moieties are frequently used in medicinal chemistry. The synthesis of derivatives bearing a free NH often requires the use of a protection method. A literature search reveals very few protection/deprotection methods for cyclic carbamates. In this paper, we described different methods applicable to 2(3H)-benzoxazolone and 2(3H)-benzothiazolone. (C) 2004 Elsevier Ltd. All rights reserved

(5Z)-3-(2-Oxopropyl)-5-(3,4,5-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione

In the crystal of the title molecule, C16H17NO6S, there are three sets of intermolecular C—H...O hydrogen bonds, as well as two sets of intermolecular C—H...π(ring) interactions. In addition, the thiazolidene rings participate in offset π–π stacking interactions [centroid–centroid distance = 3.685 (1) Å]. These generate small channels running parallel to the a axis with approximate cross-sections of 3.7 × 8.1 Å

Antioxydant activity of β-carboline derivatives in the LDL oxidation model

A series of b-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO4 or 2,20-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R = 1.6 for 5 mM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R = 1.9 to 2.8 for 1 mM CuSO4. These substances have protective actions and increase significantly the cell viability

MUC4-ErbB2 Oncogenic Complex: Binding studies using Microscale Thermophoresis

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A top−down approach of potentially complicating factors for using carbonyl sulfide (COS) to assess region−scale GPP in western France.

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Effect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists

A series of nitrogen heterocycles containing α–ethoxyphenylpropionic acid derivatives were designed as dual PPARα/γ agonist ligands for the treatment of type 2 diabetes (T2D) and its complications. 6-Benzoyl-benzothiazol-2-one was the most tolerant of the tested heterocycles in which incorporation of O-methyl oxime ether and trifluoroethoxy group followed by enantiomeric resolution led to the (S)-stereoisomer 44 b displaying the best in vitro pharmacological profile. Compound 44 b acted as a very potent full PPARγ agonist and a weak partial agonist on the PPARα receptor subtype. Compound 44 b showed high efficacy in an ob/ob mice model with significant decreases in serum triglyceride, glucose and insulin levels but mostly with limited body-weight gain and could be considered as a selective PPARγ modulator (SPPARγM)

Synthesis and Biological Evaluation of <i>N</i>‑[2-(4-Hydroxyphenylamino)-pyridin-3-yl]-4-methoxy-benzenesulfonamide (ABT-751) Tricyclic Analogues as Antimitotic and Antivascular Agents with Potent in Vivo Antitumor Activity

Benzopyridothiadiazepine (<b>2a</b>) and benzopyridooxathiazepine (<b>2b</b>) were modified to produce tricyclic quinazolinone <b>15</b>–<b>18</b> or benzothiadiazine <b>26</b>–<b>27</b> derivatives. These compounds were evaluated in cytotoxicity and tubulin inhibition assays and led to potent inhibitors of tubulin polymerization. <i>N</i>-[2­(4-Methoxyphenyl)­ethyl]-1,2-dihydro-pyrimidino­[2,1-<i>b</i>]­quinazolin-6-one (<b>16a</b>) exhibited the best <i>in vitro</i> cytotoxic activity (GI₅₀ 10–66.9 nM) against the NCI 60 human tumor cell line and significant potency against tubulin assembly (IC₅₀ 0.812 μM). In mechanism studies, <b>16a</b> was shown to block cell cycle in G2/M phase and to disrupt microtubule formation and displayed good antivascular properties as inhibition of cell migration, invasion, and endothelial tube formation. Compound <b>16a</b> was evaluated in C57BL/6 mouse melanoma B16F10 xenograft model to validate its antitumor activity, in comparison with reference ABT-751 (<b>1</b>). Compound <b>16a</b> displayed strong <i>in vivo</i> antitumor and antivascular activities at a dose of 5 mg/kg without obvious toxicity, whereas <b>1</b> needed a 10-fold higher concentration to reach similar effects

Antimicrobial Properties of Compounds Isolated from Syzygium malaccense (L.) Merr. and L.M. Perry and Medicinal Plants Used in French Polynesia

A preliminary ethnopharmacological survey, achieved in French Polynesia, led to the collection of the most cited plants among 63 species used to treat “infectious” diseases, with a description of their medicinal uses. Bibliographical investigations and antimicrobial screening permitted the selection of the botanical species Syzygium malaccense (Myrtaceae) for phytochemical analysis. Leaves of Syzygium malaccense were usually used in mixture with rhizomes of Curcuma longa to treat infectious diseases such as cystitis. The methanolic plant extracts were tested in vitro with an agar microdilution method on 33 bacteria strains and 1 yeast to obtain their Minimal Inhibitory Concentration (MIC), and cytotoxicity against HepG2 cells were evaluated. Antimicrobial synergistic effects of methanolic plant extracts from leaves of Syzygium malaccense and rhizomes from Curcuma longa were also evaluated. The bio-guided isolation of leaf extract from Syzygium malaccense led to the identification of seven alkyl-salicylic acids (anacardic acids or ginkgolic acids C15:0, C15:1, C17:0, C17:1, C17:2, C17:3 and C19:1) described for the first time in this species. All compounds were tested against Staphylococcus aureus (18.75 < MIC < 75.0 µg/mL), Streptococcus pyogenes (2.34 < MIC < 18.75 µg/mL) and Pseudomonas aeruginosa (MIC = 150 µg/mL), and their structure–activity relationships were discussed. The methanolic extract and salicylic derivatives from S. malaccense showed an interesting antimicrobial activity against Gram+ bacteria, without toxicity on hepG2 cells at 400 μg/mL. Moreover, these antibacterial compounds have already been studied for their anti-inflammatory activity, which supports the therapeutic interest of S. malaccense against infectious disease