A new series of compounds possessing 5-(2-aminothiazol-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol skeleton was designed, synthesized, and evaluated for their in vitro DHFR inhibition, antimicrobial, antitumor and schistosomicidal activities. Four active compounds were allocated, the antibacterial ...

We report the Wittig reactions of 2-methoxy-5-(2′-ethylhexyloxy)-1,4-xylylenebis(triphenylphosphonium bromide) with terephthalaldehyde, 1,4-naphthalenedicarbaldehyde and 9,10-anthracenedicarbaldehyde. Two sets of model compounds were synthesized. The first consisted of a central fragment of 2-m...

RésuméLa synthèse et les résultats de l'étude des propriétés sérotoninergiques et/ou anti-dopaminergiques d'une série de (tétrahydro-1,2,3,6 pyridinyl-4)-3 1H-indoles substitués ou non sur le noyau indolique sont présentés. La plupart des composés ont été obtenus par co...

Although several tritiated agonists have been used for radiolabelling serotonin (5-hydroxytryptamine, 5-HT)1B receptors in rats, data with a selective, radiolabelled antagonist have not been presented. Inasmuch as [3H]GR125,743 specifically labels cloned, human and native guinea pig 5-HT1B recep...

A series of pyrazolo[1′,5′:1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones was synthesized and tested in radioligand binding assays to determine their affinities for the human adenosine A1, A2A, A2B and A3 receptors. Results indicated that this scaffold is appropriate for adenosine receptor subtype A1...

Here we report a structure–activity relationship (SAR) study of analogues of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol. Our SAR is focused on introduction of various substitutions in the piperazine ring of the hybrid template. The goal behind this s...

The synthesis of covalently cross-linked bis-lexitropsins 14, 15 and 16 designed to bind to specific nucleotide sequences in the minor groove of double-helical DNA is described.

The binding behaviour toward DNA of some minor groove binders related to distamycin was studied by means of circular dichroism. In addition their influence on the activity of topoisomerases isolated from Streptomyces noursei has been investigated. The monocationic imidazole containing ligands (l...

The coupling of a sterically hindered acridinyl isoxazole ester directly to the amine group of a lexitropsin is significantly improved by double activation, using trimethylaluminum to activate the amine portion and samarium (III) chloride to enhance the carboxylate reactivity.

The syntheses of 1–4, pyrroloiminoquinone chromophore and its lexitropsin carrier linked derivative designed to improved cellular uptake are described.

Carbocyclic oligopeptides containing of two, three or four aromatic rings with N,N-dimethylpropyl-1,3-diamine group as C-terminus fragment of compounds and 5-[bis(2-chloroethyl)amino]-2,4-dinitrobenzamide as N-terminal were synthesized. These lexitropsins present antitumour activity on the neopl...

We have constructed hybrid drugs where mitomycin C is linked to the N-methylpyrrole carboxamide framework present in lexitropsins. The coupling reactions leading to these products are efficient and the yields are very high. An interesting spectroscopic feature of these hybrids is the red shift o...

Novel strong hydrogen-bond donor hydroxylated-poly(2,3,4,5,6-pentafluorostyrene) (PPFSOH) copolymers were synthesized via a versatile and chemoselective thiol-para-fluoro coupling using an unprotected bis(trifluoromethyl)mercaptoalcohol as modifier. Their ability to form miscible blends or inter...

Methanol crossover through the Nafion membrane is a perennial problem in the operation of direct methanol fuel cells (DMFCs) and therefore justifies the search for a Nafion substitute. This study reports a new methanol-blocking polymer matrix which consists of a methanol barrier phase and an emb...

This paper explores the different methods currently available to obtain the partial solubility parameters of polymers in order to apply them for the prediction of miscibility in polymer/polymer blends. Blends based on poly(ethylene oxide) (PEO) have been chosen because its miscibility has been r...

A better understanding of controlling factors in the control of bio-events on polymer surfaces is the first benchmark toward realization of life innovation. Although it has been accepted that a family of poly(vinyl ether) (PVE) with various side chain structures is a good candidate for a blood c...

Solid electrolytes based on poly(ethylene oxide)/poly(4-vinyl phenol-co-2-hydroxyethyl methacrylate) (PVPh-HEM) blends and LiClO4 were obtained and characterized by differential scanning calorimetry (DSC), infrared vibrational spectroscopy (FTIR) and electrochemical impedance spectroscopy (EIS)....

In the present work, blends of poly(ethylene oxide) (PEO), poly(acrylonitrile-co-methyl acrylate) (PANMA) and poly(4-vinylphenol-co-2-hydroxyethyl methacrylate) (PVPh-HEM) were studied by DSC, FTIR and electrochemical impedance spectroscopy (EIS). PEO/PANMA blends were found to be immiscible, wh...

Blends of poly(ethylene oxide) (PEO) and poly(4-vinylphenol-co-2-hydroxyethyl methacrylate) (PVPh-HEM) were studied by means of synchrotron small and wide angle X-ray scattering (SAXS and WAXS, respectively) and by differential scanning calorimetry (DSC). The DSC measurements were used in the de...

DSC and optical microscopy were used to determine the miscibility and crystallinity of blends of poly(ethylene oxide) (PEO) with poly(4-vinylphenol-co-2-hydroxyethyl methacrylate) (PVPh-HEM). A single glass transition temperature was observed for all blends, indicating miscibility. A progressive...