Double 1,4-addition of (thio)salicylamides/thiosalicylic acids with propiolate derivatives: a direct, general synthesis of diverse heterocyclic scaffolds.

A simple and practical ring-closure procedure to prepare a range of diverse heterocycles has been developed. In this transformation, a variety of substituted (thio)salicylamides and thiosalicylic acids undergo a double 1,4-addition reaction with propiolate derivatives in the presence of an inorganic base (K3PO4), as a result benzothiazinones, benzoxazinones and benzoxathiinones were prepared in good to excellent yields, respectively, even in gram scales. In addition, further transformation towards more complex structures and oxicam drug analogues has also been successfully carried out.

Identification of epigenetic factor KAT2B gene variants for possible roles in congenital heart diseases.

Congenital heart disease (CHD) is a group of anatomic malformations in the heart with high morbidity and mortality. The mammalian heart is a complex organ, the formation and development of which are strictly regulated and controlled by gene regulatory networks of many signaling pathways such as TGF-ß. KAT2B is an important histone acetyltransferase epigenetic factor in the TGF-ß signaling pathway, and alteration in the gene is associated with the etiology of cardiovascular diseases. The aim of this work was to validate whether KAT2B variations might be associated with CHD. We sequenced the KAT2B gene for 400 Chinese Han CHD patients and evaluated SNPs rs3021408 and rs17006625. The statistical analyses and Hardy-Weinberg equilibrium tests of the CHD and control populations were conducted by the software SPSS (version 19.0) and PLINK. The experiment-wide significance threshold matrix of LD correlation for the markers and haplotype diagram of LD structure were calculated using the online software SNPSpD and Haploview software. We analyzed the heterozygous variants within the CDS region of the KAT2B genes and found that rs3021408 and rs17006625 were associated with the risk of CHD.

Sodium Iodide (NaI)-Catalyzed Cross-Coupling for C-S Bond Formation via Oxidative Dehydrogenation: Cheap, Direct Access to Unsymmetrical Aryl Sulfides.

A simple and practical NaI-catalyzed direct C-H sulfenylation of arenes has been developed under air. In this reaction, aryl sulfides were obtained in moderate to excellent yields with high regioselectivity from readily available aromatic compounds and aryl/alkyl thiols, even on gram scale. To demonstrate the practicability of this reaction, two bioactive compound skeletons were synthesized in good yields. This method can also be used to late-stage modification of curcumin.

[Experimental study of the permeability of Fel Ursi's in eye].

OBJECTIVE: To determine whether Tauroursodeoxycholic acid (TUDCA) can penetrate the blood-ocular barrier after orally administration of Fel Ursi. METHODS: 56 rabbits were divided into two groups, 48 rabbits were used in experimental group, and other 8 rabbits were served as control. 100 mg/ml Fel Ursi were a fused into rabbits stomach. 2 ml blood from vein of auris-edge, aqueous humor from left eye and vitreous sample from right eye were obtained at 0.5, 1.0, 2.0, 4.0, 6.0 and 8.0 h after Fel Ursi administration. Concentration of TUDCA from all of samples was determined by HPLC. RESULTS: TUDCA Concentrations were (999.1 +/- 17.2) - (1300.6 +/- 78.2) microg/ml, (12.7 +/- 1.4) - (47.8 +/- 4.7) microg/ml, and (10.8 +/- 2.9) - (57.9 +/- 7.9) microg/ml in blood, aqueous humor and vitreous respectively. There was no significant differences in the concentration of TUDCA in samples of aqueous humor and vitreous (P > 0.05). However the concentration of TUDCA in rabbit blood was much higher compared with that in aqueous humor and vitreous (P < 0.01). CONCLUSION: Fel Ursi can reach intraocular tissue through penetrating blood-aqueous barrier and blood-vitreous barrier after orally application.