Meral Tuncbilek

Penetration of the pulp chamber by bleaching agents in teeth restored with various restorative materials.

It is thought that externally applied bleaching agents may penetrate into the pulp chamber. This study was conducted to evaluate the diffusion of peroxide bleaching agents into the pulp chamber of teeth restored with various restorative materials. Sixty-five human extracted anterior maxillary teeth were separated into the 13 groups containing 5 teeth. Five teeth (control group) were not subjected to any cavity preparation and restoration. Standardized class V cavities were prepared in the other 60 teeth and restored using composite resin (Charisma), polyacid modified composite resin (Dyract), or resin-modified glass ionomer cement (Vitremer). All teeth were sectioned 3 mm apical to the cementoenamel junction to remove the intracoronal pulp tissue, and the pulp chamber was filled with acetate buffer to absorb and stabilize any peroxide that might penetrate. Vestibular crown surfaces of teeth in the experimental groups were subjected to four different bleaching agents for 30 min at 37 degrees C, whereas the teeth in the control groups were exposed only to distilled water. Then the acetate buffer solution in the pulp chamber of each tooth was removed, and the pulp chamber of each tooth was rinsed with 100 ml of distilled water twice. Leukocrystal violet and enzyme horseradish peroxidase were added to the mixture of the acetate buffer and rinse water. The optical density of the resulting blue solution was determined spectrophotometrically and converted into microgram equivalents of hydrogen peroxide. Higher hydrogen peroxide concentrations resulted in a higher pulpal peroxide penetration. The highest pulpal peroxide penetration was found in resin-modified glass ionomer cement groups, whereas composite resin groups showed the lowest pulpal peroxide penetration.

Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA.

The novel benzimidazole derivatives (3, 5, 8, 9, 12-14, 18-41) were prepared in this paper and the antimicrobial activities of these compounds against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA, standard and clinical isolates), Bacillus subtilis, Escherichia coli and Candida albicans were evaluated. Compounds 24-26 which have no substitution of N-1 position displayed better antibacterial activities than those of standards (ciprofloxacin, ampicillin and sultamicillin) against both the drug-resistant bacteria (MRSA, standard and clinical isolates). These derivatives (24-26), 2,5,6-trihalogenobenzimidazole analogues (8, 12), 5,6-dichloro-2-amino derivative (13), and 5-chloro-2-(4-benzyloxyphenyl)benzimidazole (35) exhibited the most potent antibacterial activity with MIC 3.12 microg/ml against S. aureus.

Synthesis and Antimicrobial Activity of Some New 2-Phenyl-N-substituted Carboxamido-1H-benzimidazole Derivatives

Some 1H‐benzimidazole‐carboxamide derivatives were prepared and their antimicrobial activities against Staphyloccus aureus, Escherichia coli and Candida albicans evaluated. Compounds 18, 22, and 25 exhibited the best activity against Candida albicans.

Synthesis of novel 6-(4-substituted piperazine-1-yl)-9-(β-D-ribofuranosyl)purine derivatives, which lead to senescence-induced cell death in liver cancer cells.

Novel purine ribonucleoside analogues (9-13) containing a 4-substituted piperazine in the substituent at N(6) were synthesized and evaluated for their cytotoxicity on Huh7, HepG2, FOCUS, Mahlavu liver, MCF7 breast, and HCT116 colon carcinoma cell lines. The purine nucleoside analogues were analyzed initially by an anticancer drug-screening method based on a sulforhodamine B assay. Two nucleoside derivatives with promising cytotoxic activities (11 and 12) were further analyzed on the hepatoma cells. The N(6)-(4-Trifluoromethylphenyl)piperazine analogue 11 displayed the best antitumor activity, with IC(50) values between 5.2 and 9.2 μM. Similar to previously described nucleoside analogues, compound 11 also interferes with cellular ATP reserves, possibly through influencing cellular kinase activities. Furthermore, the novel nucleoside analogue 11 was shown to induce senescence-associated cell death, as demonstrated by the SAβ-gal assay. The senescence-dependent cytotoxic effect of 11 was also confirmed through phosphorylation of the Rb protein by p15(INK4b) overexpression in the presence of this compound.

Synthesis and antimicrobial activity of some new benzimidazole carboxylates and carboxamides

Some benzimidazole carboxylates and carboxamides were synthesized and evaluated for their antimicrobial activities against Staphylococcus aureus, Escherichia coli and Candida albicans. Among the investigated compounds 2d exhibited best activity against C. albicans.

Synthesis and antimicrobial evaluation of some new substituted purine derivatives.

A series of 8,9-disubstituted adenines (4, 5, 8), 6-substituted aminopurines (10-13) and 9-(p-fluorobenzyl/cyclopentyl)-6-substituted aminopurines (16, 17, 19-30) have been prepared and the antimicrobial activities of these compounds against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA, standard and clinical isolate), Bacillus subtilis, Escherichia coli and Candida albicans were evaluated. 6-[(N-phenylaminoethyl)amino]-9H-purine (12) which has no substitution at N-9 position and 9-cyclopentyl-6-[(4-fluorobenzyl)amino]-9H-purine (24) exhibited excellent activity against C. albicans with MIC 3.12 microg/mL. These compounds displayed better antifungal activity than that of standard oxiconazole. Furthermore, compound 22 carrying 4-chlorobenzylamino group at the 6-position of the purine moiety exhibited comparable antibacterial activity with that of the standard ciprofloxacin against both of the drug-resistant bacteria (MRSA, standard and clinical isolate).

Synthesis of novel substituted purine derivatives and identification of the cell death mechanism.

Novel 9-(substituted amino/piperazinoethyl)adenines (4-12), 6-(substituted piperazino/amino)purines (15-27), 9-(p-toluenesulfonyl/cyclopentyl/ethoxycarbonylmethyl)-6-(substituted amino/piperazino)purines (28-34, 36, 37, 38-41) were synthesized and evaluated initially for their cytotoxic activities on liver Huh7, breast T47D and colon HCT116 carcinoma cells. N(6)-(4-Trifluoromethylphenyl)piperazine derivative (17) and its 9-(p-toluene-sulfonyl)/9-cyclopentyl analogues (28, 36) had promising cytotoxic activities. Compounds 17, 28 and 36 were further analysed for their cytotoxicity in a panel of a liver cancer cell lines. The compound 36 had better cytotoxic activities (IC50 ≤ 1 μM) than the nucleobase 5-FU and nucleosides fludarabine, cladribine, and pentostatine on Huh7 cells. Cytotoxicity induced by 36 was later identified as senescence associated cell death by SA-β-Gal assay.

Antioxidant properties of flavone-6(4')-carboxaldehyde oxime ether derivatives.

Thein vitro antioxidant properties of some flavone-6(4)-carboxaldehyde oxime ether derivatives (la-f, lla-f) were determined by their effects on the rat liver microsomal NADPH-dependent lipid peroxidation (LP) levels by measuring the formation of 2-thiobarbituric acid reactive substances. The free radical scavenging properties of the compounds were also examinedin vitro by determining their capacity to scavenge superoxide anions and interact with the stable free radical 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The most active compounds,llb (Flavone-4′-carboxaldehyde-O-ethyl oxime) andId (Flavone-6-carboxaldehyde-O-[2-(1-pyrolidino) ethyl] oxime), caused 98 and 79% inhibition of superoxide anion production and DPPH stable free radical at 10p-3 M, respectively.

The structure of 1-(p-fluorophenylmethyl)-2-(4-methyl-1-piperazinyl)-1H-benzimidazole hydrogen fumarate

The crystal and molecular structure of the title compound has been determined by X-ray analysis. The 1-(p-fluorophenylmethyl)-2-(4-methyl-1-piperazinyl)-1H-benzimidazole ion cocrystallizes with fumaric acid, (C19H22N4F+·C4H3O4−), in space group P-1 with cell dimensions a = 9.938(1), b = 10.131(1), c = 12.712(1) Å, α = 86.57(1), β = 69.41(2), and γ = 67.22(2)°. The piperazine N4 atom is protonated and contacts the deprotonated O atom of the fumarate anion through a hydrogen bond. The benzimidazole ring is nearly planar and makes a dihedral angle of 111.25(12)° with the fluorophenyl ring. The piperazine ring adopts a chair conformation.

Synthesis and antiaggregator activity of some new derivatives of 4H-1-benzopyran-4-one

Summary A series of 2-[2-alkyl-1 H -benzimidazol-5(6)-yl]-4 H -1-benzopyran-4-one analogues 7a-7e was synthesized by the reaction with 3′,4′-diaminoflavone and aliphatic carboxylic acids. 3′,4′-Diaminoflavone 6 was prepared via the reduction of 2-(4-amino-3-nitrophenyl)-4 H -1-benzopyran-4-one 5a . The compounds 7a-e and 14a-f were tested in vitro for their inhibitory activities against human platelet aggregation induced by collagen, ADP and A23187. The compound with a COOR group as a side chain, 2-(2-alkyloxycarbonyl-2,3-dihydro-l,4-benzodioxin-6-yl)-4 H -1-benzopyran-4-one 14a-f , has potent activity, and so compound 13 was also prepared as an analogue of series 14 and tested for its antiaggregator activity.