Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and...

A new series of bis((5-aryl-1,3,4-oxadiazol-2-yl)thio)alkanes 4–14 have been synthesized via nucleophilic substitution reaction of dihaloalkanes with respective 1,3,4-oxadiazole-2-thiols 3a-f, and characterized by spectroscopic techniques. The structures of 4 and 12 were unambiguously confirmed...

A series of novel 3-{[(substituted phenyl)methyl]thio}-4-alkyl/aryl-5-(4-aminophenyl)-4H-1,2,4-triazoles 11–20 and several related Schiff's bases, 3-{[(substituted phenyl)-methyl]thio}-4-alkyl/aryl-5-{[[(substituted phenyl/5-nitro-2-furyl)methylene]amino]-phenyl}-4H-1,2,4-triazoles 21–31 ...

An alternative and fast method for the purification of an exo-β-d-galactofuranosidase has been developed using a 4-aminophenyl 1-thio-β-d-galactofuranoside affinity chromatography system and specific elution with 10 mM d-galactono-1,4-lactone in a salt gradient. A concentrated culture medium f...

Previous studies from our laboratories have reported the synthesis and pharmacological characteristics of a series of symmetrical opiate azines: naloxonazine, oxymorphonazine and naltrexonazine. We have now synthesized and characterized in binding assays and in vivo two asymmetrical azines: oxym...

(2E,3Z)-2-(1-Methyl-2,5-dioxoimidazolidin-4-ylidene)-3-[(arylamino- or heteroarylamino)methylene]succinate 5 obtained by [2+2] cycloaddition of (5Z)-5-[(dimethylamino)methylene]-3-methylimidazolidine-2,4-dione (1) and dimethyl acetylenedicarboxylate (2) followed by substitution of the dimethylam...

The preparation of new methyl 4-(het)aryl-3-amino-1H-pyrrole-2-carboxylates was achieved starting from commercial arylacetonitriles. This four steps synthesis afforded with good yields interesting building-blocks useful in the access to many nitrogen heterocycles with potential therapeutic interest.

In this study, a novel ligand, 7-(2,3-dicyanophenoxy)-3-(2-chloro-4-fluorophenyl)coumarin was synthesized by the reaction of 3-(2-chloro-4-fluorophenyl)-7-hydroxycoumarin with 1,2-dicyano-3-nitrobenzen in dry DMF as the solvent in the presence of K2CO3 as the base. The preparation of the corresp...

A series of novel N-pyrrolyl-, N-(2,5-dimethyl)pyrrolyl- and N-(2,5-dithiophen-2-yl)pyrrolyl- partially fluorinated and/or fully substituted benzenes have been prepared by the nucleophilic substitution of fluorine (SNAr) in hexafluorobenzene, 1-pentafluorophenyl-1H-pyrrole; 2,5-dimethyl-1-pentaf...

The flash vacuum pyrolysis of new 1,1-dimethyl- and 1-methyl-1H,3H-pyrrolo[1,2-c]thiazole-2,2-dioxides gave penta-substituted 2-vinyl-1H-pyrroles via sigmatropic [1,8]-H shift of the corresponding azafulvenium methide intermediates. In some cases these 1H-pyrroles underwent rearrangement to 2-al...

1-(4-Fluorophenyl)-2,5-di(thiophen-2-yl)-1H-pyrrole (FPTP) was synthesized and polymerized both chemically and electrochemically. Spectroelectrochemistry experiments reflected a π to π* transition with a band gap energy of 1.94 eV for the polymer. A dual type electrochromic device (ECD) of P(F...

Human urinary metabolites of the oral anti-rheumatic drug RS-2(4-isobutylphenyl)propionic acid (“ibuprofen”) have been further characterised by gas chromatograph-mass spectrometry of appropriate derivatives. Gas-phase analytical resoltion of diasteromeric amides formed with R-(−)-α-phenylethy...

A new derivative of polyamine, N,N-bis-(1,8-naphthalenedicarboximidopropyl)-N-propylamine has been synthesized and its structure studied by X-ray diffraction, FTIR, 1H and 13 C NMR spectroscopy. The B3LYP and DFT calculations have been carried out. The molecular conformation is folded and stabil...

We here show the first identified ligand 2,7-diamino-1,8-naphthyridine (DANP) that strongly and specifically binds to the single cytosine and thymine bulges with exclusively 1:1 stoichiometry.

X-ray structural analyses have been made on single crystals of mer(N)-[Co(5-dptma)(NO2)2] (A), mer(N)-[CoCl(5-dptma)(H2O)] Br (B), mer(N)-[CoCl(5-dptma)(H2O)]ClO4 (C) and mer(N)-[CoCl(5-dptma)(H2O)] NO3 (D), where H(5-dptma) is N,N-bis(3-aminopropyl)glycine. Complex A crystallizes in the monocli...

IntroductionIn locations that lack nearby cyclotron facilities for radionuclide production, generator-based 68Ga radiopharmaceuticals might have clinical utility for positron emission tomography (PET) studies of myocardial perfusion and other physiological processes.

The Pd(II) bis(benzonitrile) complex [Pd(PhCN)2Cl2] reacted with a mixture of 2-hydroxy-3-methoxybenzaldehyde, 1,3-diaminopropane, and triethylamine in acetonitrile to produce [Pd(L1)Cl] (HL1 = (E)-2-(((3-aminopropyl)imino)methyl)-6-methoxyphenol) (1), which contains an imine–amine-type macrocy...

Besides putrescine, cadaverine, spermidine, spermine and thermospermine, three novel polyamines were detected in a slightly halophilic eubacterium Halococcus acetoinfaciens (IAM 12094, ATCC 25861). These novel polyamines were found to be N-3-aminopropylcadaverine [NH2(CH2)3NH(CH2)5NH2] and its a...

Blue crystals of {[Cu(bapa)]3[Cr(CN)6]2}n·6nH2O (bapa = bis(3-aminopropyl)amine) have been prepared, characterized and investigated by IR spectroscopy, X-ray structural analysis and measurement of magnetic response. Its unusual 3D crystal structure is formed by infinite Cu(II)–Cr(III) antipara...

Green crystals of Co(III)/Co(II) mixed valence compound [Co(bapen)Br2]2[CoBr4] (bapen = N,N′-bis(3-aminopropyl)ethane-1,2-diamine) were isolated from the aqueous system CoBr2 – bapen – HBr, crystallographically studied and characterized by elemental analysis and IR spectroscopy. Its ionic cry...