Ti-Catalyzed Formal [2π + 2σ] Cycloadditions of Bicyclo[1.1.0]butanes with 2-Azadienes to Access Aminobicyclo[2.1.1]hexanes.

Saturated bicyclic amines are increasingly targeted to the pharmaceutical industry as sp3-rich bioisosteres of anilines. Numerous strategies have been established for the preparation of bridgehead aminobicyclics. However, methods to assemble the bridge-amino hydrocarbon skeleton, which serves as a meta-substituted arene bioisostere, are limited. Herein, a general approach to access 2-aminobicyclo[2.1.1]hexanes (aminoBCHs) by titanium-catalyzed formal [2π + 2σ] cycloaddition of bicyclo[1.1.0]butanes and 2-azadienes was developed. Simple derivatization of aminoBCHs leads to various medicinally and agrochemically important analogues.

[Chemical Evolution and Formation Mechanism of Groundwater in Hetao Irrigation Area].

Groundwater resources are important sources of water in the arid region of northwestern China, but their overexploitation and utilization has led to a series of ecological and environmental problems. Exploring the characteristics and mechanism of groundwater chemical evolution is important for the rational use of groundwater resources. The characteristics of groundwater chemical evolution were studied in the Yongji Irrigation Area of Hetao Irrigation District and the formation mechanism of the chemical compounds in groundwater were investigated using cluster analysis, factor analysis, and other statistical methods. The influence degree of different factors was calculated. The results showed that the major cations in groundwater in the study area were Na+ and K+, and the major anions were Cl- and HCO3-. Moreover, Na+, K+, and Cl- showed high spatial variability and were the main factors contributing to groundwater salinization. The major chemical compounds in the groundwater in the study area were Cl-Na, HCO3 ·Cl ·SO4-Na, and HCO3-Na. Based on the cluster analysis results, the groundwater was divided into four categories (A1, A2, B1, and B2), of which A1 was highly mineralized by Cl-Na type water, while A2, B1, and B2 were mainly HCO3 ·Cl ·SO4-Na and HCO3-Na type water. Principal component analysis results suggest that groundwater chemistry was mainly affected by salinization, carbonate karstification, and human activities with the influence degrees of 45.976%, 23.853% and 16.678%, respectively. Evaporation, salt rock dissolution, and cation exchange were important sources of Na+ and Cl- accumulation in the irrigation area. Agricultural irrigation (leaching of soil salts) and drought (intense transpiration) were the key drivers of groundwater salinization in the irrigation area.

Relationships of Inflammatory Factors and Risk Factors with Different Target Organ Damage in Essential Hypertension Patients.

BACKGROUND: Atherosclerosis (AS) is an inflammatory disease. Inflammation was considered to play a role in the whole process of AS. This study aimed to analyze the relationships of inflammatory factors and risk factors with different target organ damages (TOD) in essential hypertension (EH) patients and to explore its clinical significance. METHODS: A total of 294 EH patients were selected and divided into four groups according to their conditions of TOD. Forty-eight healthy subjects were selected as control. The clinical biochemical parameters, serum amyloid A, serum tryptase, and lipoprotein-associated phospholipase A2 (Lp-PLA2) in each group were detected, and the related risk factors were also statistically analyzed. RESULTS: Fibrinogen (Fbg) was the most significant independent risk factor in acute coronary syndrome (ACS) group (odds ratio [OR]: 22.242, 95% confidence interval [CI]: 6.458-76.609, P< 0.001) with the largest absolute value of the standardized partial regression coefficient B' (b': 1.079). Lp-PLA2 was the most significant independent risk factor in stroke group (OR: 13.699, 95% CI: 5.236-35.837, P< 0.001) with b' = 0.708. Uric acid (UA) was the most significant independent risk factor in renal damage group (OR: 15.307, 95% CI: 4.022-58.250, P< 0.001) with b' = 1.026. CONCLUSIONS: Fbg, Lp-PLA2, and UA are the strongest independent risk factors toward the occurrence of ACS, ischemic stroke, and renal damage in EH patients, thus exhibiting the greatest impacts on the occurrence of ACS, ischemic stroke, and renal damage in EH patients, respectively.

Relationship between coronary atherosclerosis plaque characteristics and high sensitivity C-reactive proteins, interleukin-6.

BACKGROUND: The relationship between inflammatory markers and the characteristics of coronary atherosclerosis plaques is uncertain. The aim of the present study was to evaluate the relationship between the characteristics of coronary atherosclerosis plaques and inflammatory markers such as high sensitivity C-reactive proteins (Hs-CRP) and interleukin-6 (IL-6). METHODS: All patients suspected of having coronary heart disease (CHD) underwent Siemens 64-slice CT angiography (64-SCTA) to distinguish the quality of plaque of coronary artery lesions. Blood samples were taken to measure levels of serum Hs-CRP and IL-6 in different plaque groups and the control group and compared with the value of 64-SCTA for detection of coronary artery plaque. RESULTS: The sensitivity of detecting coronary artery plaque by 64-SCTA was 87.4%, the specificity was 87.1%, the positive predictive value was 82.2%, and the negative predictive value was 91.0%. Comparing the levels of serum Hs-CRP and IL-6 among plaque groups, the mean levels of serum Hs-CRP and IL-6 in three plaque groups were significantly higher than those in the control group (P < 0.01). The mean levels of serum Hs-CRP and IL-6 in the soft plaque group and mixed plaque group were significantly higher than those in hard plaque group (P < 0.01). Plaque burden in the soft plaque group and mixed plaque group was significantly higher than in the hard plaque group (P < 0.01), but there was no statistical difference between the soft plaque group and mixed plaque group (P = 0.246). There was a negative correlation between the CT scale and Hs-CRP and IL-6 levels in the soft plaque group (r = -0.621, P < 0.01, and r = -0.593, P < 0.01 respectively). There was a positive correlation between the plaque burden and Hs-CRP and IL-6 levels in the soft plaque group (r = 0.579, P < 0.05 and r = 0.429, P < 0.05 respectively). CONCLUSIONS: 64-SCTA is an effective way to distinguish the different quality of coronary atherosclerosis plaque. Serum Hs-CRP and IL-6 levels can be considered as the indexes to judge the degree of CHD and may reflect the activity of plaque in CHD patients. Thus it is important for clinical diagnosis and risk evaluation of acute coronary syndrome (ACS) patients.