Synthesis of some hetaryl substituted benzofurans of potential antitumor activity

Acetyl-benzo [b] furan [1] reacts with DMF - DMA to give the novel 1-[benzofuran-2-yl]-3-[dimethylamino rpropen-2-one [2]. The reaction of the latter with hydroxylamim: or hydrazine hydrate furnished 5- [benzofuran-2-yl]-isoxazole [3] and 3-[benzofuran-2-yl]-1 H-pyrazole [4], respectively. Also. reaction of2 with various active methylene compounds and hydrazonoyl halides afforded regioselectively the respective 2,3.6- trisllbstituted pyridine [Sa-c] and [pyrazol-4-yl]methanones [10a-t]. respectively. Also. reaction of 10 with hydrazine hydrate afforded the corresponding pyrazolopyriú:lazines [II a-c]. Preliminary screening for the antitumor activity of the synthtsized compounds against the liver carcinoma cell line HEPG-2 has been carried out. The results revealed that the compounds 3. 4 and 13b showed high degree of activity. while the other compounds showed low activity

Synthesis and antimicrobial activity of some substituted 1, 3, 4-oxadiazole and other heterocycles derived from 4, 5-dimethoxy-2-nitrophenyl-thioacetic acid hydrazide

Anumber of substituted oxadiazoles, benzothiazinones and other heterocycles were synthesized from 4, 5-dimethoxy-2-nitrophenylthioacetic acid hydrazide. The structures of the prepared compounds were confirmed via their elemental analysis and the usual physical measurements. The prepared compounds have been screened for their antimicrobial activities against examples from gram positive, gram negative bacteria and fungi. Two of the tested compounds showed high activity comparable with the reference Levofloxacin while the others showed moderate to low activity