Seref Demirayak

Microwave supported synthesis of some novel 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and investigation of their anticancer activities.

The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities.

Some Pyridazinone and Phthalazinone Derivatives and Their Vasodilator Activities

In this study, 6-[(4-arylidene-2-phenyl-5-oxoimidazolin-1-yl)phenyl]-4,5-dihydro-3(2H)-pyridazinone and 4-[(4-arylidene-2-phenyl-5-oxoimidazolin-1-yl)phenyl]-1(2H)-phthalazinone derivatives were synthesized by reacting 6-(4-aminophenyl)-4,5-dihydro-3(2H)-pyridazinone or 4-(4-aminophenyl)-1(2H)-phthalazinone compound with different 4-arylidene-2-phenyl-5(4H)-oxazolone derivatives. The vasodilator activities of the compounds were examined bothin vitro andin vivo. Some pyridazinone derivatives showed appreciable activity.

Synthesis and antibacterial activities of some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives

In this study, some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives were synthesized by reacting 2-(2-methyl-5-nitro-1H-imidazolyl)ethylamine dihydrochloride, which was prepared using metronidazole, with some 1,4-dicarbonyl compounds. The structure elucidation of the compounds was performed by IR, 1H-NMR and mass spectroscopic data and elemental analysis results. Antimicrobial activities of the compounds were examined and notable activity was obtained.

Synthesis and anti-cancer activity evaluation of new aurone derivatives.

Abstract In this study, we have synthesized 2-[3- or 4-(2-aryl-2-oxoethoxy)arylidene]benzofuran-3-one derivatives (D1–D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1–A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1–C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with α-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.

Synthesis and Anticancer Activities of Some Thiazole Derivatives

In this study, 2-substituted 4-[3/4-(4-arylthiazole-2-yl)aminophenyl]thiazole derivatives and 2-[4-[2-substituted 4-methylthiazole-5-yl]thiazole-2-yl]amino-5-arylidenethiazoline-4-one derivatives have been synthesized. The cytotoxic and/or growth inhibitory effects of the 16 selected compounds were evaluated in vitro against approximately 66 human tumor cell lines derived from nine neoplastic diseases. Some of the compounds were found to act as anticancer agents.

Synthesis, characterization and antimicrobial activity of a Zn(II) complex with 1-(1H-benzoimidazol-2-yl)-ethanone thiosemicarbazone

A new Zn(II) complex with 1-(1H-benzoimidazol-2-yl)-ethanone thiosemicarbazone [Zn(NO3)(H2O)(C10H11N5S)]NO3 was prepared and characterized by elemental analyses, FT-IR, 1H NMR spectroscopy, thermogravimetric analysis (TGA), X-ray diffraction (XRD), and single-crystal X-ray diffraction analysis. The coordination geometry of the pentacoordinated zinc is a distorted square pyramid. The antimicrobial activity of the complex was evaluated using a broth micro-dilution method against a panel of human pathogenic Gram positive, Gram negative bacteria and the yeast Candida albicans. The best inhibitory effect was observed against Enterobacter aerogenes (MIC = 0.031 mg mL−1).

Synthesis and cytotoxic and analgesic activities of some 1, 5-diaryl-3-ethoxycarbonylpyrrole derivatives

Some 1,5-diaryl-3-ethoxycarbonyl-2-methylpyrrole derivatives were obtained by reacting 1-aryl-3-ethoxycarbonylpent-1,4-diones and a suitable aniline derivative or sulfanilamide under Paal-Knorr pyrrole synthesis conditions. The cytotoxicity of the compounds was tested and all compounds, except for compound 2 h, showed a time-dependent increase in cytotoxic activity. Analgesic activities of the compounds were determined by using the tail-flick and tail-immersion methods; some of the compounds showed potent analgesic activity.

Synthesis and Analgesic Activities of Some 2-(Benzazolylacetyl)amino-3-ethoxycarbonylthiophene Derivatives

In this study, some 2-[2-(benzazole-2-thioxy)acetylamino]-3-ethoxycarbonylthiophene and 2-[2-(benzazole-1-yl)acetylamino]-3-ethoxycarbonylthiophene compounds were obtained by the reaction of 2-chloroacetylamino-3-ethoxycarbonylthiophene derivatives and a suitable benzazole-2-thione or benzimidazole derivatives. Analgesic activities of the compounds were tested by using tail-flick and tail-immersion methods. It is reported that some of the compounds showed remarkable analgesic activities.

Some nitroimidazole derivatives as possible antibacterial agents.

In this study, six 1-[2(benzazol-2-yl)thioethyl]-2-methyl-5- nitroimidazole derivatives were synthesized. Antibacterial activities of the compounds obtained were examined and it was found that they are effective against aerobe bacteria.

Synthesis of some imidazolyl-thioacetyl-pyrazolinone derivatives and their antinociceptive and anticancer activities

In this study, some 4-(1,5-diarylimidazol-2-yl)thioacetyl-1-phenyl-2,3-dimethyl-3-pyrazoline-5-one derivatives were prepared by reacting 4-(2-chloroacetyl)-1-phenyl-2,3-dimethyl-3-pyrazoline-5-one and 2-mercapto-1, 5-diarylimidazole derivatives. The antinociceptive and anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds, 2a, 2d, 2g, and 2j, showed remarkable antinociceptive activity, and one of the compounds, 2i, showed weak anticancer activity.