The methyl glycoside of a tetrasaccharide isolated from heparin, methyl O-(α-l-idopyranosyluronic acid)-(1 → 4)-O-(2-acetamido-2-deoxy-α-d-glucopyranosyl)-(1 → 4)-O-(β-d-glucopyranosyluronic acid)-(1 → 3)-O-β-d-galactopyranoside disodium salt and a trisaccharide derivative thereof, methyl...

Acid-catalyzed cyclization of N-(3-methylbut-3-enyl)-N-styrylformamides 1–3 in the presence of 9-BBN triflate gave access to 2-benzyl-1-formyl-4-methyl-1,2,5,6-tetrahydropyridines 4a–6a and minor amounts of the isomeric 1,2,3,6-tetrahydropyridines 4b–6b. Triflic acid catalyzed cyclization of ...

Poly(p-chloromethylstyrene-ethyleneglycoldimethacrylate) polymeric microbeads, poly(p-CMS-EGDMA), were synthesized and 1,5,9,13-tetrathiacyclohexadecane-3,11-diol (S4HD) was attached chemically onto the polymeric microbeads. Characterization of all microbeads was done by Fourier transform-infrar...

Poly(p-chloromethylstyrene-divinylbenzene) polymeric microbeads, poly(p-CMS-DVB), were synthesized and 1,5,9,13-tetrathiacyclohexadecane-3,11-diol was attached chemically to the polymeric microbeads. Characterizations of all microbeads were carried out using FT-IR, TGA, DSC and an elemental anal...

The fabrication of a fully bio-sourced adsorbent of Cd(II) by covalent immobilization of quinine on cellulose paper is described. The double bond of commercially available quinine was converted to a terminal alkyne function which was reacted with cellulose paper, chemically modified with azide f...

A novel voltammetric assay for quinine (QN) determination using an electrochemically pretreated pencil graphite electrode is described. The detection limit of QN was 2 × 10−7 M. The method possesses some obvious advantages including extreme simplicity, rapid response, and low cost.

A series of hybrid antiprotozoal compounds with quinine-triazolyl scaffold were prepared by copper catalyzed Huisgen 1,3-dipolar cycloaddition via O-mesylation with mesyl chloride followed by azide displacement. The synthesized azide derivative was made to react with various aromatic and aliphat...

A convenient and facile method for the direct synthesis of α,α-difluorobenzoyl lactones or cyclic ethers via the radical cyclization reaction of 2-iodo-2,2-difluoroacetophenone with unsaturated acids or alcohols was reported.

The present study described design, preparation and characterization of a new magnetic nanocomposite based on polyvinyl alcohol (PVA) as a non-toxic, water-soluble, high mechanical stable and low-cost polymer. Fourier transform infrared (FT-IR) spectroscopy, field-emission scanning electron micr...

Herein, we described the ultrasound-assisted synthesis of thioesters via the Ag-catalyzed radical oxidative decarboxylation of α-keto acids, in the presence of disulfides. This protocol takes advantage of the sonication to prepare the title compounds in moderate to very good yields, in only 20 ...

A sensitive, selective, and rapid ultra-high performance liquid chromatography–tandem mass spectrometry (uHPLC–MS/MS) was developed for the simultaneous quantification of clopidogrel (Plavix®) and its derivatized active metabolite (CAMD) in human plasma. Derivatization of the active metabolite...

IntroductionThe clopidogrel active metabolite (CAM) is unstable and challenging to quantitate. The objective was to validate a new method for stabilization and quantitation of CAM, clopidogrel, and the inactive metabolites clopidogrel carboxylic acid and 2-oxo-clopiodgrel in feline plasma.

In order to obtain 4-C-alkylated pyridin-2(1H)-ones, two strategies were studied: nucleophilic substitution of 4-chloro-3-nitropyridinone derivatives which essentially failed and lithiations of 2-methoxy-3-pivaloylaminopyridines which gave the expected products.

The acute effect of an antimycotic drug, bifonazole, on hepatic peroxisomes of rats was studied in comparison with that of clotrimazole, which has a similar structure. By feeding 0.5% bifonazole in the diet for 5 days, the activities of camitine acyltransferase, carnitine palmitoyltransferase an...

Acyl-Coenzyme A thioesters of the hypolipidaemic and cancerinogenic peroxisome proliferators clofibric acid, nafenopin, ciprofibrate, bezafibrate and tibric acid were found to greatly increase the activity of rat brain protein kinase C. Maximal activation required the simultaneous presence of Ca...

2,6-Diaminopurine (DAP) and 2,6-diaminopurine 2′-deoxyriboside (DAPdR) are analogs of adenine and deoxyadenosine, respectively. It was the purpose of this study to compare these analogs under identical conditions in order to define their inhibitory properties and the underlying mechanism in L12...

2,6-Diaminopurine nucleosides are used as pharmaceutical drugs or prodrugs against cancer and viral diseases.The synthesis of 2,6-diaminopurine riboside, -2′-deoxyriboside, -2′,3′-dideoxyriboside and -arabinofuranoside was efficiently carried out by transglycosylation using bacterial whole ce...

The 2′,3′-dideoxyriboside of 2,6-diaminopurine (ddDAPR) and its 2′,3′-didehydro derivative (ddeDAPR) are poor substrates for adenosine deaminase (ADA) but potent inhibitors of the enzyme. Their Km values for ADA are of the same order of magnitude as those of the natural adenosine (Ado) and 2...

The 2′,3′-dideoxyriboside (ddDAPR), 2′,3′-didehydro-2′,3′-dideoxyriboside (ddeDAPR) and 3′-azido-2′,3′-dideoxyriboside (AzddDAPR) of 2,6-diaminopurine have been previously recognized as potent inhibitors of human immunodeficiency virus replication. These compounds are also potent inhibi...

New thiophene and annulated thiophene pyrazole hybrids were synthesized and screened for their in vitro COX-1/COX-2 enzymatic inhibition and in vivo anti-inflammatory activities. All compounds were more COX-2 selective inhibitors than COX-1 with compound 13 exhibiting the highest COX-2 selectivi...