The present paper reports a new method for the synthesis of a Cu(II) ternary system using N,N'-bis[(4-methylphenyl)sulfonyl]ethylenediamine and 1,10-phenantroline as ligands. The binding of the complex to DNA was investigated by thermal denaturation. Its potency as artificial nuclease has also been tested and an efficient oxidative DNA cleavage was observed in the presence of a reducing agent (sodium ascorbate).
The esters (3a-f) and amides (4a-c) of 2-(3,4-dihydro-3-oxo-2H-[1,2,4] triazino[4,3-c]-quinazolin-4-yl)acetic acid were synthesized by prior esterification or aminolysis of the acid 2. The structure of the synthesized compounds was confirmed by spectroscopic investigations. Almost all substances, which have been tested in vitro for the antioxidant activity in nitrosative stress, have shown significant antioxidant activity in comparison with N-acetylcystein (N-ACC). Compound 3f revealed the best antioxidant properties in a nitrosative stress model. Few weeks after the implementation of the new legislation, it seems that its purpose has at least partially been achieved; a number of "dreams shops" closed or changed their field of activity. However, it is possible that some of the consumers of such products, which have rather moderate risks, will replace them with drugs associated with higher risks, acquired from the black market. Whether the general outcome would be positive or negative will remain to be seen.
The purpose of the present work was to select substituents by using Topliss modified approach to synthesize new 1,3 oxazines with antimicrobial effect. In the series of 6-[4-substitutedphenyl]-4-phenyl-6H-1,3-oxazin-2-amines and N-[6-(4-substitutedphenyl)-4-phenyl-6H-1,3-oxazinyl] acetamides, substituents at fourth position of the phenyl ring were selected according to the Topliss modified approach and the initial set of compounds was synthesized. The antimicrobial screening revealed that compounds with methoxy substituent having negative sigma (-0.04) and negative pi (-0.27) values are good antimicrobial agents showing low minimum inhibitory concentration (MIC). The hydroxyl group substituent with more negative sigma (-0.61) and pi (-0.37) values was selected to synthesize final set compounds and were found better antimicrobials than the initial set of compounds. The study revealed that electron donating polar substituents at fourth position of the phenyl ring are required to improve antimicrobial potential in the series of 6-[4-substitutedphenyl]-4-phenyl-6H-1,3-oxazin-2-amines and N-[6-(4-substitutedphenyl)-4-phenyl-6H-1,3-oxazinyl] acetamides.
A novel series of binuclear complexes of the [M2L(AcO)(2)(H2O)(4)] type, where M= Cu(II), Ni(II), Co(II) or Mn(II) and L= (C39H34N4O6)(2-), were synthesized by template condensation of 1,3-bis(2'-formylphenyl)-1,3-dioxapropane, L-tryptophan and metal acetate in methanolic medium. The complexes of M(II):L (2:1) type were characterized by elemental analyses, molar conductivity measurements, IR, electronic spectra and magnetic susceptibility measurements. The low value of molar conductivity indicates them to be non-electrolytes. Based on the magnetic and electronic spectral data, an octahedral / distorted octahedral geometry may be proposed for all the complexes. The new complexes were screened for their antimicrobial activity towards ten microbial strains, by qualitative and quantitative assays. Our results indicated that the [Cu2L(AcO)(2)(H2O)(4)] complex was the most active of the studied compounds, concerning both the intensity of the antimicrobial activity and the microbial spectrum.
Some 2-R-5-formyl-1,3,4-thiadiazole derivatives have been synthesized and characterized by their spectral data. Thus, the present paper describes the formation and hydrolysis, through Sommelet reaction, of some hexamethylenetetramine salts from which some new heterocyclic aldehydes resulted.
A series of 5-arylamino-1,3,4-thiadiazol-2-yl acetic acid esters have been synthesized by the cyclization of the corresponding thiosemicarbazides with concentrated sulphuric acid followed by the esterification of the amide group. The thiosemicarbazides derivatives were obtained by nucleophilic addition of cyanoacetic acid hydrazide to different arylisothiocyanates. The newly synthesized compounds were characterized by their physical parameters and the structures were elucidated by spectral data and elemental analysis.
The 4-phenyl-1-[α-acylamino-β-(p-X-phenyl)]acriloyl thiosemicarbazides 3a-h were synthesized using 2-R-4-(p -X-benzylidene)-oxazol-5-ones 1a-h as starting materials. The reaction of compounds 1a-h with hydrazine hydrate led to the formation of acid hydrazides 2a-h. The thiosemicarbazide derivatives 3a-h were obtained by nucleophilic addition of corresponding acid hydrazides 2a-h to phenylisothiocyanate. The newly synthesized compounds structures were elucidated by spectral data and elemental analysis.
Cyclization of 4-phenyl-1-[α-acylamino-β-(p-X-phenyl)]acriloyl thiosemicarbazides 2a-h with concentrated sulfuric acid conduCted to 2-phenylamino-5-[(α-acylamino)-p-X-stiryl]-1,3,4-thiadiazole 3a-h. The newly synthesized compounds structures were elucidated by elemental analysis and spectral data.