In spite of great progress in understanding cancer biology, current therapeutic procedures remain unsatisfactory. Chemotherapy is often followed by secondary effects with cellular toxicity negatively affecting the results. The discovery and development of new safe and efficient antitumor agents ...

Previous high throughput virtual screening of 10 million-compound and following cell based validation led to the discovery of a novel, nonlipopeptide-like chemotype ZINC 6662436, as toll-like receptor 2 (TLR2) agonists. In this report, compounds belonging to four areas of structural modification...

SUMMARYIn a double-blind trial in 28 human volunteers, a new local anaesthetic agent, aptocaine, was compared intradermally at 1, 2 and 3% concentrations with lignocaine 2% and bupivacaine 0.5%. In a second trial in 27 subjects, 1% aptocaine was compared with mepivacaine and prilocaine, both 1, ...

2,4,5-Trimethoxy chalcones and analogues were synthesized from asaronaldehyde derived from β-asarone. These novel compounds when tested against three human tumour cell lines (MCF-7, SW-982 and HeLa) using MTT assay, revealed that chalcones possessing electron donor groups in para position to ca...

Three novel Py2N2-cobalt(III) complexes with the 5-hydroxy-1,4-naphthoquinone nuclei (NQ) were evaluated as potential hypoxia-activated anticancer prodrugs. The complexes were synthesized and fully characterized by IR and UV–Visible spectroscopies, ESI mass spectrometry and CHN elemental analys...

1-(5-Chloroindol-3-yl)-3-hydroxy-3-(2H-tetrazol-5-yl)-propenone (5CITEP) is an inhibitor of the HIV-1 integrase (IN). Theoretical studies were performed on the interaction of this inhibitor with surrounding amino acids. Density functional theory (DFT) calculations were conducted to identify the ...

Electrolysis of 3-(5-hydroxy-3-methylpyrazol-4-yl)-3-arylpropionitriles in alcohol in an undivided cell in the presence of sodium bromide as mediator results in fast and efficient cyclization with the formation of the substituted spirocyclopropylpyrazolones in 60–90% substance yield. The fast (...

Spectroscopic studies on newly synthesized biologically active pyridazin-3(2H)-one derivative 5-(2-hydroxy-5-methoxy-phenyl)-2-phenyl-2H-pyridazin-3-one (HMPP) molecule have been studied at room temperature in various solvents of different polarities. Theoretically, the ground state dipole momen...

4-Hydroxy-2(or 5)-ethyl-5(or 2)-methyl-3(2H)-furanone (HEMF) is considered a key flavor compound in soy sauce. The compound has a caramel-like aroma and several important physiological activities, such as strong antioxidant activity. Here, we report the identification and characterization of an ...

New Schiff base ligand was prepared by condensation of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with o-phenylenediamine. Cu(II), Ni(II), Co(II), VO(IV), Zn(II), Cd(II) and UO2(VI) complexes were prepared and characterized on the basis of elemental analyses, IR, (1H and 13C) NMR, electron...

A biocatalytic approach was employed for the asymmetric reduction of sterically demanding ketones to prepare 3-hydroxy-5-oxo-5-phenylpentanoates and 5-hydroxy-3-oxo-5-phenylpentanoates. Screening a collection of microorganisms led to the identification of stereocomplementary microbial strains th...

In this work, we report the synthesis and characterization of three novel copper(II) complexes of naphthyl derived 3-hydroxy-4-pyridinone chelators. Their antibacterial activity against several Gram-positive and Gram-negative reference strains and multidrug-resistant clinical isolates was assess...

para-Substituted benzoic acid esters of cyclohexanol, 1,4-dihydroxycyclohexane, 4-hydroxy-cyclohexanone and of the corresponding exo-methylene derivative were synthesized and the conformational equilibria of the cyclohexane skeleton studied by low temperature 1H and 13C NMR spectroscopy. The geo...

Electron-impact ionization mass spectra, the decay of metastable ions, ionization and appearance energies and bond energies, as dissociation energies, are reported for the title compounds. An ionization energy of 9.47 eV was obtained for benzoic acid, 9.43 eV for benzoic acid n-butyl ester, 9.61...

The present work reports the electrochemical fabrication of an ionic liquid functionalized multiwalled carbon nanotubes–polyaniline ([email protected]/PANI) nanocomposite coating and its application in the headspace-solid phase microextraction (HS-SPME) and gas chromatography (GC) determination...

An approach for the determination of benzoic acid (BA) and total paraben content using mercaptosuccinic acid capped CdTe quantum dots (MSA-CdTe QDs) as an optical probe is presented. The levels of these preservatives in the samples of liquid foodstuff could be determined by both visible and fluo...

An efficient and practical asymmetric synthesis of 1-tert-butyl 3-methyl (3R,4R)-4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidine-1,3-dicarboxylate 1, a useful intermediate for the synthesis of nociceptin antagonists, has been developed. This method includes the following key steps: (1) dias...

A novel Schiff base ligand 3-(hydroxyimino)-2-butanone-2-(1H-benzimidazol-2-yl)hydrazone has been synthesized by the condensation reaction of 2-Hydrazinobenzimidazole with diacetyl monoxime in presence of acetic acid catalyst. The ligand has crystallized as its acetate salt, due to the charge-as...

Facile and efficient procedures for the N-acylation reaction of amide derivatives with various acid anhydrides and the cyclization reaction of N-acylated amide derivatives with various hydrazine hydrochlorides were described. The reactions were carried out under microwave irradiation to give pro...

An efficient protocol for the synthesis of 2-arylquinoline N-oxides has been developed via KMnO4-mediated cross-coupling reaction of quinoline N-oxides with aromatic hydrazines in moderated to good yields. The reactions proceeded efficiently over a broad range of substrates with excellent regios...