Synthesis of new 8-(5-substituted amino-1,3,4-oxadiazol-2-yl) and 8-(5-substituted amino-1,3,4-thiadiazol-2-yl) methoxyquinolines with antibilharzial activity.

Several 5-substituted amino-1,3,4-oxadiazol-2-yl and 5-substituted amino-1,3,4-thiadiazol-2-yl derivatives with different 8-hydroxyquinoline moieties in the 2-position were prepared and tested for their antiparasitic activity. Preliminary biological tests on mice experimentally infested with Schistosoma mansoni revealed that the new compounds show moderate schistosomicidal activity.

Antidiabetic activity of some 1-substituted 3,5-dimethylpyrazoles.

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.

Synthesis and antidiabetic activity of some sulfonylurea derivatives of 3,5-disubstituted pyrazoles.

Two series of 3,5-disubstituted pyrazolesulfonylurea derivatives were prepared and evaluated as hypoglycemic agents. Preliminary biological testing revealed that the new compounds possess potent hypoglycemic activity.

Synthesis and antidiabetic activity of some sulfonylurea derivatives of 3,4,5-trisubstituted pyrazoles.

Three series of 3,4,5-trisubstituted pyrazolesulfonylurea derivatives were prepared and evaluated as hypoglycemic agents. Preliminary biological testing revealed that the new compounds possess moderate hypoglycemic activity.

Preparation and antidiabetic activity of cyclic sulfonylthiourea derivatives.

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.

Formation of thiazoles, thiazines, and thiadiazines from 1-phthalazine thiosemicarbazides as potential anticonvulsants.

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.

New spectrophotometric assay for pilocarpine.

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.

A sensitive colorimetric method for estimation of ascorbic acid.

The reaction of ascorbic acid with ammonium molybdate to give molybdenum blue was investigated and used for microestimation of the vitamin in the pure state, dosage forms and plasma. The proposed method couples sensitivity (as little as 2 microg/ml can be determined) and specificity since no interference was found in the presence of common reducing sugars, antioxidants and degradation products of the vitamin. Recovery varied from 98.

Synthesis of new mercaptotriazoles with potential antibilharzial activity.

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.

Preparation and antidiabetic activity of some sulfonylurea derivatives of 3,5-disubstituted pyrazoles.

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.

Synthesis of 4-substituted aminobenzoate quaternary salts as potent antispasmodic agents.

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.

Synthesis of some substituted pyrazole-3-carboxylic acids with possible hypoglycemic and antimicrobial activity.

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).

Synthesis of some 2.5-disubstituted anilino-3.6-dichloro-1.4-benzoquinones as antimicrobial agents.

The potent antimicrobial properties of several chloroquinones prompted the synthesis of nineteen new 2.5-disubstituted anilino-3.6-dichloro-1.

New biphenyl derivatives i: 1-(4-biphenylyl)-2-phenylethylamines as potential antispasmodic and cardiovascular agents.

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 scope of the reactions of hydrazines and hydrazones. Part 4: Trisubstituted pyrazoles of possible hypoglycemic and antibacterial 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.

Synthesis of some phthalazine derivatives chemically related to hydralazine.

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.