New 2-phenacyl-1,2,4-triazol-3-ones were obtained by the reaction of 5-alkyl-1,2,4-triazol-3-ones with alpha-bromoacetophenone in alkaline medium. Selective reduction of the side chain carbonyl group to hydroxy group was achieved with NaBH4. The reaction of some compounds containing a phenolic hydroxyl with 4-toluenesulfonyl chloride or benzyl bromide in the presence of NaOH led to tosylated or benzylated derivatives. The tosylation or benzylation at the alcoholic hydroxyl was carried out in the presence of sodium metal. Some of the newly synthesized compounds revealed an antimicrobial activity; 6 of 14 new compounds that were studied by the National Cancer Institute were found to possess antitumor activity.

Some novel 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazol-3-one (3, 6, 8, 9) derivatives and or 3-(4-methylphenyl)[1,2,4]triazolo[3,4-b][1,3]benzoxazole (5) were synthesized from the reaction of various ester ethoxycarbonylhydrazones (1a-e) with several primary amines. The synthesis of 4-amino-5-(4-chlorophenyl)-2-[(5-mercapto-1,3,4-oxadiazol-2-yl)methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one (13) was performed starting from 4-Amino-5-(4-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (2) by four steps; then 13 was converted to the corresponding Schiff base (14) by using 4-methoxybenzaldehyde. Finally, two Mannich base derivatives of 14 were obtained by using morpholine or methyl piperazine as amine component. All newly synthesized compounds were screened for their antimicrobial activities and some of which were found to possess good or moderate activities against the test microorganisms.

Pyrazole derivatives R 0180Synthesis and Antimicrobial Activity of Some 3-Alkyl-4-(arylmethyleneamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones. -The new acetate (III) and hydrazine derivatives (IV) of the title triazolone system are synthesized. They show significant antibacterial, antifungal and antipseudomonal activities. -(KAHVECI*, B.; BEKIRCAN, O.; KARAOGLU, S. A.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 44 (2005) 12, 2614-2617; Dep. Chem., Karadeniz Tech. Univ., TR-53100 Rize, Turk.; Eng.) -A. Forchert 15-111

With the aim to find novel antimicrobial and anticancer agents, a variety of 5-oxo-[1,2,4]triazoles [cf. compounds (IV), (VI), (VII), and (VIII)] is synthesized and evaluated. Derivatives (IVa-c), (VII), and (VIIIa,c) possess antimicrobial activity, while compound (IVd) is active against the MCF7 breast cancer cell lines. -(DEMIRBAS*, N.; KARAOGLU, S. A.; DEMIRBAS, A.; SANCAK, K.; Eur. J. Med. Chem. 39 (2004) 9, 793-804; Dep. Chem., Karadeniz Tech. Univ., TR-61080 Trabzon, Turk.; Eng.) -R. Staver 02-118

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