Biomedical subjects
Publications and source records attributed to R Soliman.
Several new 1-substituted 3,5-dimethylpyrazoles were prepared for testing as hypoglycemic agents. A number of these containing para-substituted 1-carbonylphenylurea and para-substituted 1-carbamoylbenzenesulfonylurea derivatives were found to possess potent hypoglycemic activity.
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3-Substituted-4-oxothiazolin-2-yl-(1-phthalazinyl)hydrazones, 3-substituted-4-oxo-5,6-dihydro-1,3-thiazin-2-yl-(1-phthalazinyl)hydrazones, and 2-substituted-amino-5-oxo-4-(1-phthalazinyl)-6-hydro-1,3,4-thiadiazines were prepared and tested for their anticonvulsant activity. Some compounds showed weak to moderate anticonvulsant activity.
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3-Substituted 5-methyl-1-(p-[(3,5-dimethyl)pyrazol-1-yl]-, 5-methyl-1-(p-[(5-methyl-3-carboxy)pyrazol-1-yl]-, 1-(p-[(3-methyl-5-phenyl)pyrazol-1-yl]-, and 1-(p-[(3-methyl-4-bromo-5-phenyl)pyrazol-1-yl]benzenesulfonyl)-2-thiohydantoin and their 5-methyl-2-thiohydantoin and 5,6-dihydro-4(3H)-oxo-2(1H)-pyrimidinethione derivatives were prepared for evaluation as hypoglycemic agents. Biological testing showed that some of these compounds possessed antidiabetic activity.
A quick method for the determination of pilocarpine in eye drops in the presence of decomposition products is described. The method involves complexation of the alkaloid with bromocresol purple at pH 6. After treatment with 0.1N NaOH, the liberated dye is measured at 580 nm. The method has a relative standard deviation of 1.99%, and has been successfully applied to the analysis of 2 batches of pilocarpine eye drops. The recommended method was also used to monitor the stability of a pilocarpine nitrate solution in 0.05N NaOH at 65 degrees C. The BPC method failed to detect any significant decomposition after 2 h incubation, but the recommended method revealed 87.5% decomposition.
N-(Diethylaminoethyl)-4-substituted aminobenzoate quaternary salts, N-(diethylaminoethyl)-4-substituted aminobenzamide quaternary salts, 4-substituted acylaminobenzamide quaternary salts, and 4-substituted acylaminosalicylamide derivatives were prepared and tested for antispasmodic activity. Preliminary pharmacological tests on isolated guinea pig ileum revealed that the new compounds possess nonspecific inhibitory action on smooth muscles.
Several 3-mercaptotriazoles with the 8-hydroxyquinoline moiety in the 5-position were prepared and tested for antiparasitic activity. Preliminary biological tests on experimentally infected mice with Schistosoma mansoni worms revealed that the new compounds possess potent schistosomicidal activity.
Four series of p-[3,5-dimethyl- (and 5-methyl-3-carboxy-) pyrazole-1]benzenesulfonylureas, thioureas, 2-thiohydantions, and 5,6-dihydro-4(3H)-oxo-2(1H)-pyrimidinethiones were prepared for evaluation as hypoglycemic agents. Biological testing of these compounds showed that some possessed antidiabetic activity.
Condensation of ethyl 2,4-dioxo-6-phenyl hex-5-enoate (1) with 4-substituted sulphamyl phenylhydrazines (2) led to 1-aryl-3-ethoxycarbonyl-5-styrylpyrazoles (3) which on hydrolysis gave 1-aryl-5-styrylpyrazole-3-carboxylic acids (4) and upon permanganate oxidation gave 1-aryl-3-ethoxycarbonylpyrazole-5-carboxylic acids (5). Similar condensation of hydralazine (6) with (1) gave the corresponding pyrazole (7) which on hydrolysis gave the acid 8.
A series of 1-(4-biphenylyl)-2-phenylethylamine derivatives was synthesized as potential antispasmodic and cardiovascular agents related to papaverine. Preliminary pharmacological tests, on isolated guinea pig ileum and anesthetized cat blood pressure, showed that the new compounds possess nonspecific inhibitory action on smooth muscles.
The potent antimicrobial properties of several chloroquinones prompted the synthesis of nineteen new 2.5-disubstituted anilino-3.6-dichloro-1.4-benzoquinone derivatives by reacting 2.5-dichloro-p-benzoquinone with many of the official antimicrobial sulphonamides and other related amines. Testing of six representative samples for their antimicrobial activity revealed good inhibitory results on the growth of five microorganisms.
Condensation of delta-unsaturated 1.3-diketoesters (1) with 4-substituted arylhydrazines (2) or benzenesulphonyl-hydrazine (8) led to 1-aryl-3-ethoxycarbonyl-5-[alpha-substituted styryl]-pyrazoles (3), and 1-benzenesulphonyl-3-ethoxycarbonyl-5-styryl pyrazole (9). Potassium permanganate oxidation of 3 gave 5-acetyl (or benzoyl)-1-aryl-3-ethoxycarbonyl pyrazoles (6) which on hydrolysis gave the corresponding carboxylic acids (7). Hydrolysis of 3 gave the corresponding acids 4 which on treatment with thionyl chloride followed by ammonia afforded the corresponding carboxamides 5.
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The potent antihypertensive properties of hydralazine and dihydralazine prompted the synthesis of sixteen new phthalazine derivatives with thiosemicarbazide or beta-propionamide residues to investigate their possible antihypertensive activity.
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