Condensation of 3-acetylbenzo[5,6]coumarin (1) with hydrazine-carbodithioate esters and/or thiocarbohydrazide gave the corresponding N-[1-(benzocoumarin-3`-yl)ethylidene]hydrazonecarbodithioate (2a,b) and 1,5-bis[1-(benzocoumarin3`-yl)ethylidene]thiocarbohydrazide (3) respectively. Treatment of 2a with ethanolic ammonia solution and/or amines gave the corresponding thiosemicarbazone derivatives...

The reactions of iodoacetate and bromoacetate with ribonuclease have already provided some information on the relationship between the chemical structure and the catalytic a(*tivity of the enzyme. It is the purpose of this and the following paper to extend this information. In earlier studies, Gundlach, Stein, and Moore (1) showed that although alkylation at lysine, mrthioninc, or histidine res...

Harnessing the pharmacodynamic properties of vitamin D analogs: an old wine in a new bottle. Rahul Ray, Ph.D., Boston University School of Medicine, Boston, MA Therapeutic potential of 1,25(OH)2D3-analogs depends on their pharmacodynamic/ pharmacokinetic properties including bioavailability and catabolic potential. Affinity labeling analogs of 1,25(OH)2D3, that alkylate the ligand binding pocke...

Fluorinated 1,2,4-triazoles 3 and benzenesulfonyl urea and thiourea derivatives as well as their cyclic sulfonylthioureas 4–10 were prepared as antimicrobial agents. The chemistry involves the condensation of sulfanilamide derivatives 1 with trifluoroacetic anhydride to give N-di(trifluoroacetyl)sulfonamides 2 which upon reaction with hydrazine hydrate afforded the corresponding triazole deriva...

Traceless solid-phase synthesis of 1,3,7,8-tetrasubstituted xanthine (1,3,7,8-tetrasubstituted 1H-purine-2,6(3H,7H)-dione) derivatives has been developed. The solid-phase synthetic route began on a solid supported N'-cyano-N-substituted carbamimidothioate, which was prepared from cyanamide, isothiocyanate, and Merrifield resin. After N-alkylation of carbamimidothioate resin with ethyl 2-bromoac...

In this study, we aimed to develop new biologically active compounds with antibacterial properties. 4-amino-5-methyl-2H-1,2,4-triazol-3(4H)-one (1) was converted the corresponding Schiff bases (2) reaction a 4-anis aldehyde. Acetic acid ethyl esters containing [1,2,4] triazole ring (3) were synthesized by condensation of bromoacetate in basic media. The hydrazine hydrate led formation hydrazide...

The reaction of 5-(1-adamantyl)-4-phenyl-1,2,4-triazoline-3-thione (compound 5) with formaldehyde and 1-substituted piperazines yielded the corresponding N-Mannich bases 6a-f. The reaction of 5-(1-adamantyl)-4-methyl-1,2,4-triazoline-3-thione 8 with various 2-aminoethyl chloride yielded separable mixtures of the S-(2-aminoethyl) 9a-d and the N-(2-aminoethyl) 10a-d derivatives. The reaction of c...