Hayreddin Gezegen

Screening of biological activities of a series of chalcone derivatives against human pathogenic microorganisms.

In an effort to develop new antimicrobial agents, a series of chalcone derivatives, 3–60, were prepared by Claisen–Schmidt condensation of appropriate acetophenones and 2‐furyl methyl ketones with appropriate aromatic aldehydes, furfural, and thiophene‐2‐carbaldehyde in an aqueous solution of NaOH and EtOH at room temperature. The synthesized compounds were characterized by means of their IR‐ and NMR‐spectral data, and elemental analysis. All compounds were tested for their antibacterial and antifungal activities by the disc diffusion method. For the most active compounds, also minimum inhibitory concentrations (MICs) were determined.

The synthesis and screening of the antimicrobial activity of some novel 3-(furan-2-yl)-1-(aryl)-3-(phenylthio) propan-1-one derivatives

A series of thiophenol adducts (3a–m) were prepared by addition of thiophenol to chalcones (1a–m) in the presence of a catalytic amount of KOt-Bu in solvent free conditions. In addition, the antibacterial and antifungal in vitro properties were tested against some human pathogenic microorganisms by employing the disk diffusion technique. A majority of compounds were remarkably active against several of the microorganisms. Compound 3i was determined to be the most active compound.

Potassium–Tertiary Butoxide–Assisted Addition of Thioglicolic Acid to Chalcone Derivatives Under Solvent-Free Conditions

A series of chalcone derivatives containing thioglicolic acid (4a–j) was prepared by addition of thioglicolic acid to the chalcones (3a–j) in the presence of KOt-Bu under solvent-free conditions. The mechanistic pathway of the reaction can be explained by the Michael-type addition of thioglicolic acid to chalcone derivatives (3a–j).

Synthesis and Screening Antimicrobial Activities of Novel 1,3-Diaryl-3- (Phenylthio)Propan-1-One Derivatives

Abstract In this study, a series of novel β-mercapto carbonyl derivatives (3a–j) was prepared by addition of thiophenol (2) to chalcones (1a–j) in the presence of catalytic amount of iodine (10 mol%) in CH2Cl2. Antibacterial and antifungal in vitro properties of the synthesized compounds were tested against some human pathogenic microorganisms by employing the disk diffusion technique. For the most active compounds, also minimum inhibitory concentrations (MICs) were determined. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT

Iodine-Catalyzed Addition of Methyl Thioglycolate to Chalcones

Abstract A series of novel β-mercapto carbonyl compounds (3a–z), methyl 2-(3-oxo-1,3-diarylpropylthio)acetate, were synthesized and characterized via iodine-catalyzed addition of methyl thioglycolate to chalcones (1a–z). Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT

Synthesis, Characterization, and Antibacterial Activity of Novel Pyridones

Novel ethyl 2-oxo-4,6-diaryl-1,2,3,4-tetrahydropyridine-3-carboxylate and 4,6-diaryl-3,4-dihydropyridine-2(1H)-one derivatives have been synthesized from the cyclization of adducts of diethylmalonate to chalcones with ammonium acetate. The structures were established on the basis of extensive spectroscopic methods and further confirmed by X-ray crystallographic analysis. Antibacterial activity of obtained pyridones was investigated against four human pathogen microorganisms and the compounds showed poor activity. [Supplementary materials are available for this article. Go to the publishers online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.] GRAPHICAL ABSTRACT

2-(4-Bromo­phen­yl)-4-(4-meth­oxy­phen­yl)-6,7,8,9-tetra­hydro-5H-cyclo­hepta­[b]pyridine

In the title compound, C23H22BrNO, the cycloheptane ring adopts a chair conformation. The pyridine ring makes dihedral angles of 58.63 (15) and 8.27 (16)° with the benzene rings. The dihedral angle between the benzene rings is 56.68 (17)°. The crystal packing features C—Br⋯π interactions [Br⋯centroid distances= 3.813 (2) and 3.839 (2) Å; C—Br⋯centroid = 126.25 (10) and 138.31 (10)°, respectively, forming a three dimensional supramolecular architecture.

2-[1-(4-Bromo­phen­yl)-3-hy­droxy-3-(4-meth­oxy­phen­yl)prop­yl]cyclo­hexa­nol

In the title compound, C22H27BrO3, the cyclohexane ring adopts a chair conformation. The dihedral angle between the benzene rings is 41.9 (4)°. In the crystal, molecules are linked by O—H⋯O and C—H⋯O hydrogen bonds, forming a three-dimensional network. In addition, π–π stacking interactions [centroid–centroid distance = 3.953 (6) Å] between the benzene rings of the methoxybenzene groups occur.