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.

In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5-d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7-substituted-5-methyl-3-phenylthiazolo[4,5-d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d] pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coil and P. aeruginosa, and all were inactive against S. aureus.

Four novel series of 4(3H)-quinazolinone derivatives have been prepared by cyclization of the key intermediates 3-aryl-2-(3-aryl-3-oxopropenyl)-4-(3H)-quinazolinones with different reagents: 3-aryl-1-iminocarbamoyl-1H-pyrazol-5-yl)-4(3H)-quinazolines, 3-aryl-2-(3-aryl-1-thiocarbamoyl-1H-pyrazol-5-yl)-4(3H)-quinazolines, 3-aryl-2-(3-aryl-4,5-dihydro-1,2-oxazol-5-yl)-4(3H)-quinazolinones , and 3-aryl-2-(4-aryl-2-thioxo-1,2,5,6-tetrahydro-1,3-diazin-6-yl )-4(3H)- quinazolinones. The antiinflammatory activity of representatives of these compounds is comparable to or higher than that of proquazone.

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 Antimicrobial Testing of Novel Oxadiazolylbenzimidazole Derivatives. -Some of the title compounds, e.g. (II) and (V), show weak antimicrobial activity. -(HABIB, N. S.; SOLIMAN, R.; ASHOUR, F. A.; EL-TAIEBI, M.; Pharmazie 52 (1997) 10, 746-749; Dep. Pharm. Chem., Fac. Pharm., Alexandria Univ., Alexandria 21521, Egypt; EN)