This work reports the synthesis, radiolabelling and preliminary in vivo evaluation of [123I]-(4-fluorophenyl){1-[2-(4-iodophenyl)ethyl]piperidin-4-yl}methanone. The tributylstannylprecursor was synthesized with a yield of 30%. Radiolabelling was performed using an electrophilic iododestannylatio...

Human African trypanosomiasis (HAT), also known as sleeping sickness is a parasitic disease transmitted by the bite of the 'Glossina' insect, commonly known as the tsetse fly. This disease affects mostly poor populations living in remote rural areas of Africa. Untreated, it is usually ...

A series of diketo esters and their pertinent bioisosteres were designed and synthesized as potent antibacterial agents by targeting methionine amino peptidases (MetAPs). In the biochemical assay against purified MetAPs from Streptococcus pneumoniae (SpMetAP1a), Mycobacterium tuberculosis (MtMet...

The synthesis and antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids 8–58 is described. Trifluoromethylpyridine derivatives 8–58 were evaluated for their anticancer activity toward human tumoral cell lines by the National Cancer Inst...

A new method for the solid phase synthesis of benzothiazoles and 2-arylamino-3-carboxyl-4-hydroxy-5-arylthiophenes is described. Resin bound cyclic malonic acid ester was reacted with aryl isothiocyanates and then with bromine or α-bromoketones, followed by treatment with perchloric acid or sod...

The synthesis of 2-pyridone derivatives from different substituted amines and various 3-(E)-methyl 3-(4-oxo-4H-chromen-3-yl)acrylate derivatives was proposed and described. The optimized reaction conditions and the generality of the reaction were investigated, respectively. Moreover, less side p...

We have carried out the optimization of substituents at the C-3 or the C-5 position on the pyrrolidine ring of VLA-4 antagonist 3 with 2-(phenylamino)-7-fluorobenzoxazolyl moiety for the purpose of improving in vivo efficacy while maintaining good aqueous solubility. As a result, we successfully...

Fabricartion of a redox-active electrode by modification of a glassy carbon electrode (GCE) with a unique ionic liquid derived fibrillated mesoporous carbon (IFMC) following the electrografting of 4-phenylurazole via electrochemical reduction of 4-(4-nitrophenyl)urazole in the presence of sodium...

An unexpected reaction between 4-phenylurazole and fumaric esters which led to the formation of 5-alkylidene derivatives of hydantoin is described in this paper. The reaction takes place in the presence of tetrabutylammonium bromide (TBAB), and 1,4-diaza-bicyclo[2,2,2]octane (DABCO) at 70 °C un...

The validation of a pre-column derivatization procedure with 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate (AQC) to the determination of the amino acid content by RP-HPLC with fluorescence detection (λ excitation 250 nm, λ emission 395 nm) in milk-cereal based infant foods was carried out. T...

Described herein is the preparation of new aminoacylated derivatives of the dinucleotide pdCpA, and of transfer RNAs. The focus of the present work is the synthesis of amino acid analogs related to aspartic acid and cysteine species that have important functional roles in many proteins. The acti...

An improved method for the synthesis and isolation of large amounts of crystalline sodium cysteine-S-sulfate is described. The final product has been characterized as the monohydrate, monosodium salt by elemental analysis and various equivalent weight determinations. The equilibrium constant for...

This work deals with hydrolysis curves for 15 amino acids (aspartic acid, threonine, serine, glutamic acid, proline, glycine, alanine, valine, isoleucine, leucine, phenylalanine, tyrosine, histidine, lysine and arginine) in bovine casein and in model-processed cheeses with 30, 45 and 60% (w/w) f...

Quinone–hydroquinone analogues have been proven to be efficient promoters of Fenton reactions by accelerating the Fe(III)/Fe(II) redox cycle along with self-destruction. However, so far there is little information on non-quinone–hydroquinone cocatalyst for Fenton reactions. This study found th...

This paper studies the synthesis of l-cysteic acid from 1-cystine by oxidation with electrochemically generated bromine in aqueous-HBr solution. High current efficiency and material yield were obtained. A very interesting process of paired synthesis has been proposed to obtain l-cysteic acid and...

The complexation of triphenylantimony(V) catecholates (3,6-DBCat)SbPh3 (1), (4,5-pip-3,6-DBCat)SbPh3 (2) and (4,5-Cl2-3,6-DBCat)SbPh3 (3) with neutral 4-(2,6-dimethylphenyliminomethyl)pyridine (Py-CHN–Ar) leads to the formation of hexacoordinated complexes (3,6-DBCat)SbPh3·(Py-CHN–Ar) (4), (4...

A new process for the direct chlorination of 3-methyl-pyridine with special catalyst to yield 2-chloro-5-methyl-pyridine in the airlift loop reactor has been considered. The effects of reaction temperature, the molar ratio of palladium chloride to 3-methyl-pyridine, concentration of 3-methyl-pyr...

To further explore the chemical space around the entrance channel of HIV-1 reverse transcriptase (RT), a series of novel indolylarylsulfones (IASs) bearing N-substituted piperidine at indole-2-carboxamide were identified as potent HIV NNRTIs by structure-guided scaffold morphing and fragment rea...

A highly efficient, simple and rapid method for the preparation of various 2-aminobenzoxazoles and other benzoxazole derivatives using a catalytic amount of poly (ethylene glycol)-bound sulfonic acid (PEG-SO3H) is described. PEG-SO3H is found to be an economical and reusable catalyst with low ca...

Methods for the construction of C3-amino substituted 2H-indazole motifs are scarce. While the Davis-Beirut reaction proved useful and versatile in the construction of alkoxy- and thia- C3-substituted 2H-indazoles under mild basic conditions, the same success was not enjoyed when confronted with ...