Syntheses and in vitro antimicrobial evaluation of some benzimidazol-2-ylmethylthioureas, benzimidazol-2-ylacetylthiosemicarbazides and products of their condensation with monochloroacetic acid.

N-Benzimidazol-2-ylacetyl-N'-[alkyl- and arylthio (carbamoyl)]hydrazines and N-benzimidazol-2-ylmethyl-N'-alkyl- and -arylthioureas were subjected to condensation with monochloroacetic acid to afford N-benzimidazol-2-ylacetyl-N'-2,3, 4,5-tetrahydro-4-oxo-3-alkyl- and -arylthiazol-2-ylidenehydrazines and 3-benzimidazol-2-ylmethyl-2-alkyl- and arylimino-2,3-dihydrothiazol-4-(5H)ones, respectively. In preliminary antimicrobial testing, some compounds turned out to have significant activity against Staphylococcus aureus.

Syntheses and in vitro antimicrobial activities of thiazolo-[3,2-a]benzimidazol-3(2H)-ones.

Taking advantage of the nucleophilic reactivity of the 2-methylene carbon atom in thiazolo[3,2-a]-benzimidazol-3(2H)-one, a number of 2-isatinylidene and 2-arylazo derivatives have been prepared. The novel compounds were subjected to antimicrobial testing.

5-(2-Oxo-3-indolinylidene)thiazolidine-2,4-dione-1,3-di-Mannich base derivatives: synthesis and evaluation for antileukemic activity.

A novel series of 5-(2-oxo-3-indolinylidene)thiazolidine-2,4-dione, having the 1- and 3-positions of the isatin and thiazolidine rings respectively, substituted by various Mannich bases, was prepared. Five compounds were evaluated for antileukemic activity against P388 lymphocytic leukemia in the mouse. The di-Mannich base with a dimethylamino component exhibited the highest activity of the tested compounds.

Novel bis(5-arylamino-2-oxo-4-thiazolidinylidene)hydrazine derivatives as potential antineoplastic agents.

A new series of N,N'-bis(5-arylamino-3-benzyl-2-oxo-4-thiazolidinylidene)hydrazine s has been prepared for potential anticancer activity. The synthesis was achieved by reacting 3-benzylthiazolidin-2-one-4-thione with its 4-hydrazone derivative to give N,N'-bis(3-benzyl-2-oxo-4-thiazolidinylidene)hydrazine, which was subjected to dibromination followed by reaction with various primary aromatic amines. Some compounds were evaluated against leukemia P 388 in the mouse.

Novel thiazolidine-2,4-dione-4-thiosemicarbazone and 4-[(3,4-diaryl-3H-thiazol-2-yl)azo]thiazolidin-2-one derivatives: synthesis and evaluation for antimicrobial and anticancer properties.

Two novel series of 3-benzylthiazolidine-2,4-dione-4-thiosemicarbazones (V - IX) and 3-benzyl-4-[(3,4-diaryl-3H-thiazol-2-yl)azo]thiazolidin-2-on es (X - XXII) were synthesized as potential antimicrobial and anticancer agents. The products were found to be inactive against a variety of microorganisms and the preliminary antileukemic evaluation of some representative compounds against P 388 lymphocytic leukemia indicated insignificant activity.

Effect of urea on the activity of certain ophthalmic drugs in man.

The role displayed by urea (2-10%) solutions, on the miotic and mydriatic activities of pilocarpine hydrochloride and homatropine hydrobromide respectively, was investigated on the human eye. At different concentrations, urea exerts no effect on the miotic activity of pilocarpine, whereas in the case of homatropine a negative effect is experienced. For the parameters, area under pupil diameter--time curve (AUC) and maximum pupillary response (MPR), a linear relationship exists between response to homatropine and urea concentration.

Novel indolene-spiro-hydroxytetronimides as potential antineoplastic and antiviral agents.

In a continuing search for new antineoplastic and antiviral agents, the preparation of some substituted indol-2(3H)-one-3-spiro-2'-3',4'-dihydroxy-5'-imino-2',5'-dihydrofurans was designed. The synthesis was achieved by reacting isatin, 1-alkyl- or 1-aralkylisatin derivative with glyoxal sodium bisulfite and potassium cyanide. However, when 1-substituted aminomethyl derivatives of isatin or of 5-bromoisatin were used in this reaction, the indolone-spiro-hydroxytetronimide unsubstituted at position 1 was, unexpectedly, the only product isolated.

Utilization of fodder yeast and agro-industrial by-products in production of spores and biologically - active endotoxins from Bacillus thuringiensis.

A number of newly-devised fermentation media were evaluated with respect to their ability to support sporulation and biosynthesis of endotoxins by strains of Bacillus thuringiensis that are biologically active against Spodoptera littoralis, Heliothis armigera, and Spodoptera exigua. Fodder yeast from dried cells of Saccharomyces cerevisiae could be used as a complete mono-component medium for production of highly active spore-delta-endotoxin complexes from B. thur.

On the diffusion of chloramphenicol from oleaginous ointment bases.

The rate of diffusion of chloramphenicol from oleaginous ointment bases was investigated. It was found that the rate of diffusion of the drug from beeswax is markedly higher than that from hard paraffin. Cetrimide, whether present in the waxy base or in the aqueous diffusion medium, enhances markedly the rate of diffusion of chloramphenicol.

Synthesis and antimicrobial action of some bis-thiazolidines.

alpha, delta-Bis(thiazolidinidione-2,4-hydrazone-4-yl-3)butane (1) was reacted with heterocyclic and aromatic aldehydes in boiling glacial acetic acid, where the corresponding analogs of alpha, delta-bis (thiazolidindione-2,4-N-arylidenehydrazone-4-yl-3)butane (2) were separated. While with some other heterocyclic and aromatic aldehydes, and under the same conditions, the corresponding analogs of alpha, delta-bis(thiazolidinidione-2,4-N-arylidenehydrazone-4-arylidene-5-yl-3) butane (3) were obtained. The synthesized compounds exhibit antimicrobial activity.

A paper chromatographic method for separation and determination of synephrine in injectable solutions.

A new analytical method using ascending paper chromatographic technique was developed for identification and quantitative determination of residual synephrine in fresh and deteriorated samples. This method was found to be stability indicating; one to five degradation products have been successfully separated from drug samples subjected to accelerated stability testing at 60 degrees C for 3 months.

Synthesis of some dibenzazepines of possible therapeutic interest.

Among the hypotensive drugs are the N-alkyldibenz[c,e]-azepines. A representative of this class is 6-allyl-6,7-dihydro-5H-dibenz[c,e]azepine (azapetine). The present investigation involved the preparation of a new series of N-[6,7-dihydro-5H-dibenz[c,e]azepin-6-yl] acid amides namely; acetamide, benzamide, phehyl acetamide, salicylamide and p-hydroxybenzamide derivatives.

Interaction between thiamine hydrochloride and lipoic acid.

An interaction between thiamine hydrochloride and DL-alpha-lipoic acid in aqueous solution was depicted. Evidence is presented through spectrophotometric as well as vapour pressure measurements to show that thiamine hydrochloride and DL-alpha-lipoic acid form a single 1:1 complex. The stability constant and the molar extinction coefficient of the complex (at 244 nm) were determined at 25 degrees C and found to be 3.

Studies on the stability of injectable solutions of some phenothiazines. Part 2: Effect of chelating agents and antioxidants.

Chelating agents (disodium EDTA, DTPA, HEDTA and NTA) exhibit a stabilizing action towards phenothiazines to different extents. This could be correlated to the stability constants of their metal chelates as well as to the dependency of these constants on the pH-value of the solution. Antioxidants (sodium bisulphite, sodium dithionite, and sodium metabisulphite) also exert a stabilizing effect which could be correlated--in the first place--to the pH-value of the solution.

[Studies on the stability of injectable solutions of some phenothiazines. Part 1: Effects of pH and buffer systems].

The stability of phenothiazines is affected by the pH-value of the solution. At the pH-values of maximum stability, triflupromazine hydrochloride and chlorpromazine hydrochloride are more stable than promazine hydrochloride. The stability of chlorpromazine hydrochloride in the Sörensen's phosphate buffer is slightly higher than that in the McIlvaine's citric acid-phosphate buffer system.

Remote-controlled device for sampling arterial blood in unrestrained animals.

A device is described that allows remote-controlled sampling of arterial blood in unrestrained animals. An artery and a vein are dissected in local anesthesia and connected by a plastic catheter, the sampling catheter. The flow of arterial blood in this artificial shunt can be blocked by kinking the sampling catheter by a remote-controlled device.