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

Synthesis and Characterization of D-Lyxono-γ-lactone

D-lyxono-γ-lactone has been prepared in two steps from galactose. The first step potassium lyxonate was obtained in 64% yield and the title compound has been isolated in next step with 75% yield. The structures of the products were characterized by IR, 1H, 13C, mass and microanalysis study

Synthesis and Characterization of 9-Phenyl-9H-purin-6-amines from 5-Amino-1-phenyl-1H-imidazole-4-carbonitriles

9-Phenyl-9H-purin-6-amine derivatives have been synthesized in high yields by reaction between 5-amino-1-phenyl-1H-imidazole-4-carbonitrile with HC(OEt)3 and Ac2O followed by reaction with ammonia

Synthesis of Novel 6-Cyano-9-(aryl)-9H-purine Derivatives Via Formamidine Intermediates

Novel 9-substituted cyanopurine derivatives (4a-d) were synthesized in three steps in high yield. Diaminomaleonitrile (1) reacted with triethyl orthoformate to afford (Z)-N-[2-amino-1,2-dicyanovinyl] formimidate (2) which was converted to aryl-(Z)-N-[2-amino-1,2-dicyanovinyl] formamidines (3a-d) in the presence of a catalytic amount of anilinium chloride and aromatic amines in ethanol at room temperature under inert atmosphere (Argon). Furthermore, the reaction of (3a-d) with triethyl orthoformate afforded novel 6-cyano-9-(aryl)-9H-purine derivatives (4a-d) which can be used without further purification. All compounds have been fully characterized by spectroscopic data

Copper Tridentate Schiff Base Complex Supported on SBA-15 as Efficient Nanocatalyst for Three-Component Reactions under Solventless Conditions

The anchorage of a supported copper Schiff base complex on SBA-15 materials provides highly efficient heterogeneous catalysts towards the solvent-free synthesis of dihydropyrimidinones derivatives via the Biginelli condensation reaction. The novel nanocatalysts exhibited a highly ordered mesostructure with a surface area of 346 m2g−1 and an average pore diameter of 8.6 nm. Additionally, the supported copper nanocatalysts were reused at least ten times, remaining almost unchanged from the initial activity. Both the mesoporous scaffold and the tridentate Schiff base ligand contributed to the stabilization of copper species

Novel, One-Pot, Three-Component, Regioselective Synthesis of Fluorine-Containing Thiazole and Bis-3<i>H</i>-thiazole Derivatives Using Polyvinyl Pyridine as Heterogeneous Catalyst, and Evaluation of Their Antibacterial Activity

<div><p></p><p>A convenient, one-pot, three-component regioselective synthesis of novel 2,2′-(1,4-phenylene)-bis-(3-aryl-2-substituted imino-4-aryl-3H-thiazole) derivatives from 1,4-phenylene diisothiocyanate, aryl amines, and various phenacyl bromide, and also the regioselective synthesis of 3-alkyl-2-(aryl imino)-4-cyclopropyl-5-(2′-fluorophenyl)-thiazole derivatives from alkylisothiocyanate, aryl amines, and 2-bromo-2-(2-fluorophenyl)-1-cyclopropylethanone in the presence of poly-4-vinyl pyridine as heterogenous basic catalyst are described. This efficient method produced the products at room temperature with excellent yields (82–96%). The structures of all products were characterized by spectral and elemental analyses. The antimicrobial activity of the synthesized compounds was evaluated against <i>Salmonella enterica, Micrococcus luteus, Bacillus subtilis</i>, and <i>Pseudomonas aeruginosa</i>.</p></div