According to the structure-activity relationships (SARs) of modafinil, a therapeutic drug of hypnolepsy, we designed and synthesized two series of compounds 2-[(diphenylmethane)sulfinyl] acetamides and 2-[(diphenylmethyl)thio] acetamides, and measured their biological activities. The target compounds (6a-6o) were synthesized beginning with diphenyl carbinol by substitution, oxidation, acylation and so on. Their structures were confirmed by ESI-MS, 1H NMR and elemental analysis. The central stimulatory effects of the target compounds were determined by the independent activity assay on mice. Compounds 6c, 6f and 6n have considerable activities, while the central stimulative effect of 6h is slightly better than the positive control modafinil.

ObjectiveTo explore the effect of blood flow restriction (BFR)-based aerobic exercise and low-intensity resistance program on bone strength, hormone secretion, lung function and exercise capacity in postmenopausal patients with chronic obstructive pulmonary disease (COPD), to relieve the risk of fragility fractures and mortality. MethodsFrom June, 2020 to January, 2021, 67 postmenopausal patients with COPD were selected from seven community hospitals such as Chongqing Yuxi Hospital, etc. The patients were randomly divided into control group (n = 33) and experimental group (n = 34). Both groups received conventional treatment and implemented a pulmonary rehabilitation program consisting of aerobic exercise and low-intensity resistance, while the experimental group finished the low-intensity resistance under BFR, for 24 weeks. Before and after intervention, the femoral neck bone mineral density (BMD) was measured with dual-energy X-ray; the interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), 25-hydroxyvitamin D₃ [25(OH)D₃], estradiol (E₂), bone-specific alkaline phosphatase (BALP), tartrate-resistant acid phosphatase (TRACP), osteocalcin (BGP), β-I collagen cross-linked C-terminal peptide (β-CTX), growth hormone (GH) and insulin-like growth factor-1 (IGF-1) levels were measured with ELISA; the forced expiratory volume in the first second (FEV₁) and forced vital capacity (FVC) were measured with lung function test; the maximum oxygen uptake (VO_2max) and anaerobic threshold (AT) were measured with cardiopulmonary exercise test; the body mass index (BMI) and muscle mass were measured with bioelectrical impedance; the peak torque of knee flexion and extension, and fatigue index were measured with isokinetic muscle strength test; and they were also assessed with distance of 6-minute walk test (6MWT), modified Falls Efficacy Scale (MFES), Timed Up and Go Test (TUGT), and Tinetti Performance Oriented Mobility Assessment (Tinetti). ResultsFour cases dropped down in the control group, and five in the experimental group. All the indexes improved in the experimental group after intervention (|t| > 2.208, P < 0.05), and most of the indexes improved in the control group (|t| > 2.052, P < 0.05); while the E₂, GH, IGF-1, IL-6, TNF-α, TRACP, β-CTX, BALP, FEV₁, AT, distance of 6MWT, muscle mass, peak torque of knee flexion and extension, fatigue index, time of TUGT, and scores of Tinetti and MFES were better in the experimental group than in the control group (|t| > 2.141, P < 0.05). ConclusionExercise under BFR may improve the bone strength, lung function, estrogen secretion and exercise ability of postmenopausal patients with COPD, which may help to relieve the risk of fragility fractures.

OBJECTIVETo summarize the features of clinical manifestations, laboratory tests and imaging findings of patients with cardiac amyloidosis (CA).

METHODSA total of 60 CA patients (including 41 male and 19 female patients) from 4 centers admitted between May, 2012 and November, 2013 were included in the study. The demographic data, medical history, clinical manifestations, laboratory test data, ECG, cardiac ultrasound, and cardiac magnetic resonance (CMR) imaging of the patients were analyzed.

RESULTSTwo-thirds of the 60 CA patients, were middle-aged or elderly men, and 47% of the patients had AL-CA. The clinical manifestations included exertional dyspnea (73%), pedal edema (47%), hypotension (47%), and hypertrophy of the tongue (22%); abnormal laboratory test results included albuminuria (53%) and liver (15%) and kidney (28%) dysfunction; blood routine, urine and serum immunoglobulin quantification and immunofixation electrophoresis could help the screening of AL-CA. Kidney (53%) and liver (15%) involvement was common, and 86% of AL-CA patients had kidney involvement. Typical ECG characteristics included poor R wave progression (35%), low voltage in limb leads (33%), and a pseudo infarct Q wave (30%); the latter two were more frequent in AL-CA. The characteristics of ultrasound findings included left ventricle thickening (100%), left atrial enlargement (87%) and enhanced echo of the myocardial granules(92%), and diastolic dysfunction was obvious in all the CA patients regardless of the systolic function. The DT and E/e' of the mitral annulus could be used as an index to evaluate diastolic dysfunction in early stage of the disease. Left ventricular (LV) global subendocardial late gadolinium enhancement (LGE, 81%) accompanied by right ventricular (RV) and atrial LGE was the typical characteristic of CMR, and the range of LGE in the RV and the two atria was wider in AL-CA than in non-AL-CA. NT-proBNP (97%) and cardiac troponin (53%) in CA patients were both elevated, which helped in diagnosing and assessing the severity of cardiac involvement, according to which 50% of the patients were found to be at a high risk, 43% at an intermediate risk, and 7% at a low risk.

CONCLUSIONThe combination of the features of clinical, laboratory tests and imaging findings of CA have important diagnostic and prognostic value for CA.

Adult ; Aged ; Amyloidosis ; diagnosis ; pathology ; physiopathology ; Cardiomyopathies ; diagnosis ; pathology ; physiopathology ; Electrocardiography ; Female ; Humans ; Immunoglobulin Light-chain Amyloidosis ; Magnetic Resonance Imaging ; Male ; Middle Aged