Synthesis of Imidazo[1,2-a]pyridine-Fused 1,3-Benzodiazepine Derivatives with Anticancer Activity via a One-Pot Cascade GBB-3CR/Pd(II)-Catalyzed Azide-Isocyanide Coupling/Cyclization Process.

A new one-pot synthesis of imidazo[1,2-a]pyridine-fused 1,3-benzodiazepine derivatives via a sequential GBB-3CR/Pd(II)-catalyzed azide-isocyanide coupling/cyclization process was developed. The Groebke-Blackburn-Bienaymé three-component reactions (GBB-3CR) of 2-aminopyridine, 2-azidobenzaldehydes, and isocyanides in the presence of a catalytic amount of p-toluenesulfonic acid gave azide intermediates without separation. The reaction was followed by using another molecule of isocyanides to produce imidazo[1,2-a]pyridine-fused 1,3-benzodiazepine derivatives in good yields by the Pd(II)-catalyzed azide-isocyanide coupling/cyclization reaction. The synthetic approach produces novel nitrogen-fused polycyclic heterocycles under mild reaction conditions. The preliminary biological evaluation demonstrated that compound 6a inhibited glioma cells efficiently, suggesting potentially broad applications of the approach for synthesis and medicinal chemistry.

Synthesis of 4-Tetrazolyl-Substituted 3,4-Dihydroquinazoline Derivatives with Anticancer Activity via a One-Pot Sequential Ugi-Azide/Palladium-Catalyzed Azide-Isocyanide Cross-Coupling/Cyclization Reaction.

A new one-pot preparation of 4-tetrazolyl-3,4-dihydroquinazolines has been reported. The Ugi-azide reactions of 2-azidobenzaldehydes, amines, trimethylsilyl azide, and isocyanides produced azide intermediates without separation, which were treated with isocyanides to give 4-tetrazolyl-3,4-dihydroquinazoline derivatives through a sequential Palladium-catalyzed azide-isocyanide cross-coupling/cyclization reaction in moderate to good yields. The biological evaluation demonstrated that compound 6c inhibited breast cancer cells well and displayed broad applications for synthesis and medicinal chemistry.

Role of Presepsin for the Assessment of Acute Cholangitis Severity.

BACKGROUND: Presepsin is a new emerging inflammatory biomarker. The primary purpose of this study was to elucidate the predictive usability of presepsin for severity assessment in patients with acute cholangitis (AC). METHODS: A total of 119 treatment-naive patients with AC (64 males, 55 females) were enrolled in this study. Patients were classified with Grade I (mild), Grade II (moderate), or Grade III (severe) AC based on severity assessment guidelines. Presepsin concentrations were measured on admission. RESULTS: The median presepsin concentrations were 297 pg/mL (interquartile range (IQR) 234 - 386 pg/mL), 590 pg/mL (IQR 559 - 619 pg/mL), and 857 pg/mL (IQR 740 - 960 pg/mL) in patients with mild, moderate, and severe AC, respectively. Presepsin concentrations were significantly higher in patients with severe AC than in patients with moderate AC (p < 0.01), and in patients with moderate AC than in patients with mild AC (p < 0.01). With the receiver operating characteristic (ROC) analysis, the areas under the curves (AUCs) for presepsin to discriminate patients with moderate and severe AC were 0.935 (95% confidence interval (CI) 0.877 to 0.993, p < 0.001) and 0.942 (95% CI 0.885 to 0.998, p < 0.001), respectively. CONCLUSIONS: Compared with other conventional biochemical indicators such as WBC, CRP, and PCT, presepsin may be a useful parameter for the severity assessment of AC.

[Study about outcomes of non-pharmacological conservative treatment for lumbar spinal stenosis].

OBJECTIVE: To describe the short-term outcomes of a non-pharmacological conservative approach to patients with LSS. METHODS: This is a prospective consecutive case series with short-term follow-up of 21 consecutive patients who were diagnosed with LSS. Patients recruited from the outpatients of orthopaedic department and rehabilitation department in the Peking University People's Hospital from March 2010 to March 2011. Patients had baseline interviews with follow-up questionnaires in the end of the first and the third month. MAIN OUTCOME MEASURES: pain intensity was measured using the Numerical Rating Scale (NRS) and disability was measured using the Roland Morris Disability Questionnaire (RMDQ), as well as the 36-item Short Form Health Surrey (SF-36) and efficacy assessment for evaluation. RESULTS: All of 21 eligible consenting patients initially enrolling completed the follow-up. Pain at worst, functional status, quality of life improved significantly in the end of the first month. These were considered to be clinically meaningful in the end of the third month. No patients went on to require surgery. No major complications of treatment were noted. CONCLUSIONS: A non-pharmacological conservative treatment may be useful and safe in bringing about clinically meaningful improvement in pain and disability in patients with LSS. Before surgical management, a non-surgical approach should be taken into account at first.

[Dynamic assessment of grassland degradation in Naqu of northern Tibet].

Based on the past years vegetation cover, annual maximal grass yield and June-September mean modified soil-adjusted vegetation index (MSAVI) that were inversely deduced from the 10-day composite data of NOAA/AVHRR channels 1 and 2 and NDVI in 1982-2000, this paper analyzed the recent 20 years dynamics of grassland desertification in Naqu of northern Tibet. The results showed that in recent 20 years, the area of degraded grassland in Naqu was averagely 43.1% of the total land area. It was decreased in the former ten years while increased in the latter ten years, but overall, had a decreasing trend. The degraded area was larger in west part of Naqu than in its other regions. Among the eight climatic factors including temperature, precipitation, potential evapotranspiration, vapor pressure, wind velocity, sunshine hour, ratio of precipitation to evapotranspiration, and ratio of temperature to precipitation, the most remarkable factor affecting the dynamic of grassland degradation was the potential evapotranspiration.