Synthesis of biscoumarin derivatives by the reaction of aldehydes and 4-hydroxycoumarin using ruthenium (III) chloride hydrate as a versatile homogeneous catalyst

The one-pot domino Knoevenagel-type condensation/Michael reaction of aromatic, heteroaromatic and aliphatic aldehydes with 4-hydroxycoumarin in aqueous media in the presence of ruthenium salt as homogeneous catalyst was investigated. It was found that 5 mol% of RuCl3.nH2O catalyzes biscoumarin synthesis in high yields (70-95%) under optimised, mild, green and environmentally benign reaction conditions in short times (25-35min)

In vitro release and cytotoxicity study of encapsulated sulfasalazine within LTSP micellar/ liposomal and TSP micellar/niosomal nano-formulations

The micelles/liposome formulation for the first time has been constructed via thin-film hydration method containing soy lecithin (L), tween 80 (T), squalene (S), and polyvinyl alcohol (P) (LTSP nanoparticles). Similar ingredients except for lecithin were used for preparing micellar/niosomal vesicular SSZ nano formulation (TSP nanoparticles). The percent drug loading and encapsulation efficiency of SSZ was 7.39% and 98.5 ± 0.3 % for the 7.5:100 (w/w) ratio of SSZ: total weight of LTSP, while the percent drug loading and encapsulation efficiency of SSZ was 4.7% and 62.85 ± 0.3 % in the TSP nano formulation. Dynamic light scattering (DLS) and trans- mission electron microscopy (TEM) results showed that both formulations formed spherical micelles and vesicles with globule sizes of 25 ± 1.2 nm and 100 ± 20.5 nm respectively. The cell toxicity evaluations showed that both LTSP and TSP nano formulations without drug were nontoxic (at the range of this experiment) for Human Dermal Fibroblasts (HDF) as a normal cell line, but SSZ loaded nano formulation exhibited increased cell toxicity with half-maximal inhibitory concentration (IC50) of 940 mM for SSZ alone to near 240 mM for SSZ loaded nano formulation (approximately four times). In vitro release experiments exhibited sustained release of SSZ from both nano formulations. The LTSP micellar/liposomal and TSP micellar/niosomal nano formulation for SSZ delivery can be considered as appropriate approaches for improving its bioavailability and probably they are good candidates for future clinical investigations

Original scientific paper The enantioselective �-keto ester reductions by Saccharomyces cerevisiae

Abstract: The enantioselective yeast reduction of aromatic �-keto esters, by use of potassium dihydrogen phosphate, calcium phosphate (monobasic), magnesium sulfate and ammonium tartrate (diammonium salt) (10:1:1:50) in water at pH 7 as a buffer for 72–120 h with 45–90 % conversion to the corresponding aromatic �-hydroxy esters was achieved by means of Saccharomyces cerevisiae

Ultrasound-promoted one-pot four-component synthesis of novel biologically active 3-aryl-2,4-dithioxo-1,3,5-triazepane-6,7-dione and their toxicity investigation

<p>We have described a novel four-component reaction (4MCR) between oxalyl chloride <b>1,</b> anilines <b>2a–h,</b> and two molecules of ammonium thiocyanate <b>3</b> in acetone under ultrasound irradiation to give 3-aryl-2,4-dithioxo-1,3,5-triazepane-6,7-diones. A synthetically useful ultrasound effect was observed and title products were obtained in high yields after 15–35 min sonication. Our procedure compared to the conventional heating method has the benefit of higher reaction yields and shorter reaction times. The IR spectra showed the presence of N–H, C═O and C═S groups in these compounds and ¹H, ¹³C NMR and Mass spectral results verified their structures. Cellular investigations showed that these compounds are toxic toward cancer cells.</p