Some N-[(N-benzoyldehydrophenylalalnyl)glycinyl/cysteinyl]-N,N′-dicyclohexylurea analogs (3a–3o) were synthesized by conjugating different substituted N-benzoyldehydrophenylalanyl glycines/cysteines (differing substitutions on benzylidene ring) and dicyclohexyl carbodiimide (DCC) using base as...

A synthetic procedure has been developed to enable the sequential regio-selective Suzuki-Miyaura cross-coupling of 1,4-dibromo-2-nitrobenzene with a variety of arylboronic acids. The first Suzuki coupling step, using a phosphine-free palladium catalyst at room temperature, gave selective couplin...

The success of chemotherapeutics in easing the burden of malaria is under continuous threat from ever-evolving parasite resistance, including resistance to artemisinin combination therapies. Therefore, the discovery of new classes of antimalarials which inhibit new biological targets is imperati...

The new of 1-(2-hydroxyethoxy)methylindole derivatives 3a-i were prepared in good yields. None of them showed any significant anti-HIV activity and therefore the benzocondensation between the 2 and 3 positions of the pyrrole ring definitely reduced the weak activity found in the analogues 1a-c.

Azo dyes derived from 2-amino-6-(2-chloroethoxy)benzothiazole and 2-amino 4-(2-hydroxyethoxy)-benzothiazole were prepared by diazotization and coupling with different N,N-disubstituted anilines. The dyes were then quaternized with various alkylating agents, re. dimethyl sulphate, benzene-sulfoni...

Sulfonic acid esters are considered as potentially alkylating agents that may exert genotoxic effects in bacterial and mammalian cell systems. One possible source of human exposure stems from drug synthesis when the salt-forming agents methanesulfonic acid, benzenesulfonic acid or p-toluenesulfo...

The development, optimization and validation of an extraction method for methyl and ethyl esters of various sulfonic acids is presented. The extraction and determination of these esters in active pharmaceutical ingredients (APIs) was accomplished using solid-phase microextraction coupled to GC/M...

Oligodeoxynucleotides containing 4-thiothymidine residues were obtained using the phosphoramidites of 2 and 3. Treatment with CH3COSK in EtOH was used to introduce the 4-thioketo function at the oligodeoxynucleotide level.

4-Thiofuranoid glycals substituted at the 1-position with methyl (5), (t-butyldimethylsilyloxy)methyl (7), and acetoxymethyl (8) groups were prepared from the 3,5-O-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl) (TIPDS)-4-thiofuranoid glycal (3) by way of LDA-lithiation. N-Iodosuccimide-initiated e...

An investigation, based on the synergy between UV–Vis and FTIR-ATR spectroscopies and ElectroSpray Ionization Mass Spectrometry (ESI-MS), on the reactivity of 4-thiothymidine (S4-TdR) with H2O2, selected as a Reactive Oxygen Species (ROS) potentially related to Photo Dynamic Therapy (PDT), was ...

A 5′-O-monomethoxytritylthymidine-3′-S-thiophosphoramidite (3) has been used to prepare oligodeoxynucleotides containing 3′-thiothymidine on a solid phase support. The intermediate thiophosphites are most efficiently oxidised using tetrabutylammonium periodate.

The TAM kinase family arises as a new effective and attractive therapeutic target for cancer therapy, autoimmune and viral diseases. A series of 2,6-disubstituted imidazo[4,5-b]pyridines were designed, synthesized and identified as highly potent TAM inhibitors. Despite remarkable structural simi...

(Z)-13-hexadecen-11-yn-1-yl acetate (2), the sex pheromone of Thaumetopoea pytyocampa, and (5Z,7E)-5,7-dodecadien-1-ol (3), a sex pheromone component of Malacosoma disstria, have been prepared in high chemical and stereoisomeric purity by synthetic schemes involving the stereospeific coupling of...

The first stereospecific synthesis of 11S,12S-oxido 5Z, 7E, 9E, 14Z-eicosatetraenoic acid has been achieved from 2-deoxy-D-ribose using either a Horner-Emmons or Wittig condensation to form the 9,10-trans or the 5,6-cis-double bond respectively.

Phase-transfer-catalyzed esterification of various carboxylic acids has been carried out on a microanalytical scale with a new reagent, N-(9-acridinyl)-bromoacetamide, in aqueous/organic two-phase systems. The procedure gives esters showing very high fluorescence intensity in acid solution. The ...

The thermodynamic parameters for the dissociation in acetonitrile of the tris-trifluoromethanesulfonates of the heavier lanthanides according to the equilibrium Ln(tri)2 ++tri−⇌Ln(tri)3 (Ln=Tb–Lu; tri−=CF3SO3 −) are reported. Potentiometric, calorimetric, conductometric and FT-IR measurements s...

Anhydrous solutions of lanthanide(III) trifluoromethanesulfonates (triflates) in acetonitrile have been prepared and studied. Solubility measurements revealed that among the salts considered (Ln(SO3CF3)3; LnLaLu) only the heavier ones (LnDyLu) are soluble (S>150 mmol dm−3) in strictly an...

The concentration and temperature dependencies of density of lanthanum, gadolinium, lutetium and sodium trifluoromethanesulfonates in N,N-dimethylformamide (DMF) and N,N-dimethylacetamide (DMA) have been determined. From density data the apparent molar volumes and partial molar volumes of the sa...

The relationship between treatment efficacy and the pharmacokinetics (PK) and pharmacodynamics (PD) of anticancer drugs is poorly defined. 1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU) is an alkylating agent used in the treatment of brain and other forms of cancer. It is postulated that BCNU kills...

The 2-haloethylnitrosoureas have been shown to form the cross-linked structure 1-(3-cytosinyl),2-(1-guanyl)ethane in DNA. This cross-link has now been synthesized by the reaction of O6-(2-fluoroethyl)guanosine with deoxycytidine in dimethyl sulfoxide followed by removal of the sugars by acid hyd...