In vitro antitumour screening of some polysubstituted pyrazole analogs

Certain 1-[4-chlorophenyl]-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide derivatives, carrying various substituents at position 3- such as 1,2,4-triazolyl and 1,2,4-oxadiazolyl moieties have been previously synthesized and preliminarily evaluated for their antitumor activity at the National Cancer Institute's [NCI] in vitro disease-oriented antitumor screen unit. In the primary 60 cell line assay, three compounds [1-3] revealed potential broad spectrum antitumor activity against a wide range of different human cell lines of nine tumor subpanels. These compounds were further selected by the NCI for carrying out confirmatory screening procedures in order to assess their exact in vitro antitumor potentialities. A detailed discussion of the best in vitro antitumor results of these active analogs obtained from the three consecutive NCI procedures is reported in this paper. The active three compounds at the GI50 level exhibited TGI and LC50 levels with nearly the same order of activity; 3> 2> 1

Effect of natural starters used for sourdough bread in Morocco on phytate biodegradation

Phytase activity was studied in natural sourdough bread starters to determine physicochemical characteristics [phytic acid hydrolysis, dough rising capacity and pH] in the flour and during sourdough fermentation. Fermentation microorganisms [yeasts and lactic acid bacteria] were also characterized. Results showed a decrease of phytic acid in sourdoughs started with traditional starters, and wide variation in phytase activity. Microorganism counts were high at the end of fermentation, indicating higher fermenting activity of the starters. Yeast populations showed wide variation and lactic acid bacteria had high counts in the fermentation. Phytase activity was demonstrated in starter cultures made of lactic acid bacteria and yeast isolates, the most interesting of which were Saccharomyces cerevisiae combined with Lactobacillus plantarum and Leuconostoc mesenteroides

Effect of some temporary cements on the shear bond strength of dual-cured composite resin to enamel and dentin surfaces

The purpose of this in vitro study was to evaluate the shear bond strength of dual-cured composite cement after pretreatment of the enamel and dentin surfaces with eugenol-containing and eugenol-free temporary materials and comparing the results obtained with the control group [not pretreated with any temporary materials]. Cylindrical posts of dual-cured composite were bonded to the teeth surface by using syntac adhesive bond and positioned vertically to the flat dentinal area. The shear bond strengths were measured at composite-tooth surface interface by using a universal testing machine. The results of this study have shown that the shear bond strengths of dual-cured composite in the pretreated groups were highly significant in comparison with the control group at a significant level. It was concluded that the shear bond strength of dual-cured composite is effective on using temporary materials, particularly the eugenol-containing one. Also, syntac adhesive bond improved the bond strength of dual-cured composite/tooth interface

effect of dentin bonding agents on cervical microleakage of two types of composite resin restorations

This in vitro study was performed to evaluate the margin quality of two types of composite resin [Tetric Ceram and Kulzer]. Class II cavity preparations were restored using multi-incremental placement on the proximal surfaces of 60 extracted human molar teeth. In the first group [30 teeth], the cervical margin of class II cavity preparation lied apical to the cemento enamel junction. While, in the other group [30 teeth], the cervical margin lied above the cemento enamel junction. The restored teeth were immersed in methylene blue dye, the restorations were removed and the cavities were examined with stereomicroscopy for the detection of dye penetration. The results have shown that the teeth restored with Tetric Ceram type showed less microleakage than Kulzer type. For both types, the cervical microleakage at the composite resin/cementum interface was significantly greater than at the composite/enamel interface at a significant level

Proton and 13C nuclear magnetic resonance spectroscopy of some diarly and arylpyridyl ethers

The PMR as well as 13C-NMR spectra of some diaryl and arylpyridyl ethers have been studied to elucidate the effect due to various substituents, in these compounds, on the chemical shift [delta]

Intramolecular rearrangement of 2- [N-Aryl-Carbamoyl] -pyridinium salts to unsymmetrical diarylamines

The pyrylium salts [1] reacted with various ring substituted anilines to give the corresponding pyridinium salts [2] which were hydrolyzed to the betaines [3]. Reaction of [3] with thionyl chloride followed by an aniline afforded the amides [4], which were converted to the diarylamines [8] by the action of sodium hydride. The structures were confirmed by spectral data

Dithiocarbamate esters Part III: Synthesis and spectra of tetrahydroquinoline Dithiocarbamate and xanthate Esters

Reaction of sodium tetrahydroquinoline dithiocarbamate [2] with different halides, afforded the corresponding esters [3], while reaction of [2] with diiodomethane yielded the bis-dithiocarbamate esters [4]. Xanthate esters [7] were prepared from the reaction of the appropriate potassium xanthates [6] with the appropriate halide. Xanthic dithiocarbamate esters [8] were also prepared by the reaction of [6] and sodium dithiocarbamate in the presence of diiodomethane. The assigned structures of the new compounds were affirmed by micro analyses and spectral examination

Dithiocarbamate series II Preparation of new pyrrolidine-and indolinodithiocarbamate esters

Pyrrolidino and Indolinodithiocarbamate esters 3 were prepared from the reaction of the sodium salts 2 with different halides. Oxidative condensation of 2 with amines yielded the thicarbamyl sulphenamides 4. with diiodomethane 2 afforded the bis-dithiocarbamate esters 5. Mixed dithiocarbamate esters 6 were also prepared. Structures were confirmed by spectral data

Proton and carbon-13 nuclear magnetic resonance spectroscopy of some Diaryl and Pyridyl ethers

The PRM as well as[13C]NMR spectra, of some diaryl and Pyridyl ethers were recorded in order to elucidate the effect of changing the substituent on the chemical shifts [delta]

Ultraviolet and infrared spectra of some Diaryl and Pyridyl ethers

The ultraviolet and infrared spectra of some diaryl and pyridyl ethers were recorded in order to elucidate the effect of changing the structure on band position

Infrared and proton magnetic resonance spectroscopic investigation of charge transfer complexes of some heterocyclic compounds

The ir and[1]Hnmr spectra of addition compounds of picric acid and some heterocyclics are analysed in order to elucidate the type of interaction

Synthesis of new coumarin-3Carbonylurea and Thiourea derivatives

Condensation of coumarin-3-carboxyamide [1] with isocyanate and isothiocyanate derivatives afforded the urea [2] and thiourea [3] derivatives. Cyclization of the thiourea derivative [3a] with a-bromo esters yielded the 2-iminothiazc[1] idinones [4 and 5], while its condensation with ethyl beta-bromopropionate gave the 2-imino-4-oxo-5,6-dihydro-l,3-thiazine [6]