C-H Halogenation of Pyridyl Sulfides Avoiding the Sulfur Oxidation: A Direct Catalytic Access to Sulfanyl Polyhalides and Polyaromatics.

Palladium-catalyzed oxidative C-H halogenation and acetoxylation reactions of S-unprotected sulfides, selectively directed by pyridinyl groups, allows the formation of C-X bonds (X = I, Br, Cl, OAc) by using simple halosuccinimide or phenyliodine diacetate (PIDA) oxidants. The undesired formation of sulfoxides and/or sulfones, which are usually observed under oxidative conditions, is fully obviated. Under the solvent-dependent conditions that we proposed, sulfide C-H functionalization is achieved in less than 1 h without any direct electrophilic halogenation at the pyridine moiety. N-Directed ortho-C-H activation of aryl also facilitates dibromination reactions which are hardly accessible with sulfone and sulfoxide counterparts because of their higher structural rigidity. This general method gives a straightforward access to polyhalide sulfides, without an organosulfur reduction step or protection-deprotection sequence. Polyhalide sulfides are valuable synthons that give a practical entry to new constrained polyaromatic and biphenyl sulfides, including synthetically challenging unsymmetrical examples.

Inhibition of key digestive enzymes related to hyperlipidemia and protection of liver-kidney functions by Cystoseira crinita sulphated polysaccharide in high-fat diet-fed rats.

The objective of this current study was to investigate the possible hyperlipidemic and antioxidative effects of Cystoseira crinita sulfated polysaccharide (CCSP) in rats fed with a high-fat diet, exhibited an inhibitory activity on pancreatic lipase in vitro. In vivo administration of this extract to HFD-rats lowered body weight and potentially inhibited key enzymes of lipid metabolism and absorption as lipase activity in both plasma and small intestine, which led to a notable decrease of blood LDL- cholesterol (LDL-Ch) and triglycerides (TG) levels, and an increase in HDL-cholesterol (HDL-Ch) levels in HFD-rats. CCSP was also observed to protect the liver-kidney functions efficiently, by decreasing of aspartate transaminase (AST), alanine transaminase (ALT), lactate dehydrogenase (LDH) and Creatine phosphokinase (CPK) activities and creatinine, albumin, T-bilirubin, uric acid, and urea rates in plasma. The histological analysis of liver and kidney tissues further established the positive effect of CCSP.

Hypolipidemic effect of dihydroisoquinoline oxaziridine in high-fat diet-fed rats.

Obesity is a serious health problem that increases the risk of many complications, including diabetes and cardiovascular disease. This study aims to evaluate, for the first time, the effects of oxaziridine 3 on lipoprotein lipase activity in the serum of rats fed with a high-fat diet (HFD) on body weight, lipid profile and liver-kidney functions. The administration of oxaziridine 3 to HFD-rats lowered body weight and inhibited the lipase activity of obese rats leading to notable decrease of T-Ch, TGs and LDL-Ch levels accompanied with an increase in HDL-Ch concentration in serum. Moreover, the findings of this study revealed that oxaziridine 3 helped to protect liver tissue from the appearance of fatty cysts. Additionally, oxaziridine 3 administration to HFD-rats induces antioxidant activity proven by the increase of superoxide dismutase (SOD) and catalase (CAT) activities and the decrease in Thiobarbituric acid reactive substances (TBARS) levels. It also induces the protection of liver-kidney functions confirmed by a decrease in the levels of toxicity parameters in blood.

Ultrasonic activation of Heck type reactions in the presence of Aliquat-336.

Without phosphine and base, palladium catalysts such as PdCl(2), Pd(OAc)(2) and PdCl(2)(PhCN)(2) in water/DMF mixtures with Aliquat-336 proved to be excellent catalytic systems for Heck reactions involving several aryl bromides with styrene and acrylic compounds. Yields are remarkably improved under ultrasonic irradiation and the products show a high purity.

2-Hydr-oxy-3,3-dimethyl-7-nitro-3,4-dihydro-isoquinolin-1(2H)-one.

In the title compound, C(11)H(12)N(2)O(4), a new hydroxamic acid which belonging to the isoquinole family, the heterocyclic ring adopts a half-chair conformation. The nitro group is essentially coplanar with the aromatic ring. Inter-molecular O-H⋯O hydrogen bonds assemble the mol-ecules around inversion centres to form pseudo-dimers.