Synthesis of nicotinimidamides a tandem CuAAC/ring-cleavage /cyclization/oxidation four-component reaction and their cytotoxicity.

Nicotinamide and its derivatives, recognized as crucial drug intermediates, have been a focal point of extensive chemical modifications and rigorous pharmacological studies. Herein, a series of novel nicotinamide derivatives, nicotinimidamides, were synthesized a tandem CuAAC/ring-cleavage/cyclization/oxidation four-component reaction procedure from -acetyl oximes, terminal ynones, sulfonyl azides, and NHOAc. This strategy is significantly more efficient than previously reported, and the cytotoxicity of the nicotinimidamides is also tested.

Chemoselectivity of the CuAAC/Ring Cleavage/Cyclization Reaction between Enaminones and α-Acylketenimine.

Ketenimines represent an important class of reactive species, useful synthetic intermediates, and synthons. However, in general, ketenimines preferentially undergoes nucleophilic addition reactions with hydroxyl and amino groups, and carbon functional groups remain a less studied subset of such systems. Herein, we develop a straightforward syntheses of pyridin-4(1)-imines that is achieved by cyclization of a reacting enaminone unit with α-acylketenimine which is generated from the reactions of sulfonyl azides and terminal ynones (CuAAC/Ring cleavage reaction).

Synthesis of Pyridin-1(2)-ylacrylates and the Effects of Different Functional Groups on Their Fluorescence.

While fluorescent organic materials have many potential as well as proven applications and so have attracted significant attention, pyridine-olefin conjugates remain a less studied subset of such systems. Herein, therefore, we report on the development of the straightforward syntheses of pyridin-1(2)-ylacrylates and the outcomes of a study of the effects of substituents on their fluorescent properties. Such compounds were prepared using a simple, metal-free and three-component coupling reaction involving 2-aminopyridines, sulfonyl azides and propiolates.

Rasmussen's encephalitis is characterized by relatively lower production of IFN-β and activated cytotoxic T cell upon herpes viruses infection.

Background: The etiology of Rasmussen's encephalitis (RE), a rare chronic neurological disorder characterized by CD8+ T cell infiltration and unihemispheric brain atrophy, is still unknown. Various human herpes viruses (HHVs) have been detected in RE brain, but their contribution to RE pathogenesis is unclear.

Methods: HHVs infection and relevant immune response were compared among brain tissues from RE, temporal lobe epilepsy (TLE) and traumatic brain injury (TBI) patients.

HCMV infection and IFITM3 rs12252 are associated with Rasmussen's encephalitis disease progression.

Objective: Rasmussen's encephalitis (RE) is a rare and severe progressive epileptic syndrome with unknown etiology. Infection by viruses such as human cytomegalovirus (HCMV) has been hypothesized to be a potential trigger for RE. Interferon-induced transmembrane protein-3 (IFITM3) single-nucleotide polymorphism (SNP) rs12252 is associated with the severity of viral infection disease.

Extraction and antioxidant activity of flavonoids of Morus nigra.

Morus nigra has a long history of medicinal use in Chinese medicine, but the study on it is limited, the flavonoids are one of the main biological active substances. In this study, the Morus nigra flavonoids were extracted by ultrasonic and antioxidant activities both in vitro and in vivo were measured. The results showed that hydroxyl radicals clearance rate and superoxide radical anion clearance rate in vitro increased with the concentration of the total flavonoids in the range of 0-1.

Replication of british rheumatoid arthritis susceptibility Loci in two unrelated chinese population groups.

Previous genome-wide association study by WTCCC identified many susceptibility loci of common autoimmune diseases in British, including rheumatoid arthritis (RA). Because of the genetic heterogeneity of RA, it is necessary to replicate these susceptibility loci in other populations. Here, three SNPs with strong RA association signal in the British were analyzed in Han Chinese, and two SNPs (rs6457617 and rs11761231) were genotyped in the test cohort firstly.