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An improved laboratory synthesis of YC-071, a potent azole antifungal agent, has been developed. Compared with the original route, the new route is operationally simple, requiring only limited purification of all the intermediates. The new route is an important scalable synthesis, which meets the need for YC-071 for use in preclinical studies.

A series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and HRMS. The in vitro antifungal activities of the target compounds were evaluated. The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.

Background: Sedentary behaviour (sitting) is a highly prevalent negative health behaviour, with individuals of allages exposed to environments that promote prolonged sitting. Excessive sedentary behaviour adversely affects health inchildren and adults. As sedentary behaviour tracks from childhood into adulthood, the reduction of sedentary time inyoung people is key for the prevention of chronic diseases that result from excessive sitting in later life. The sedentaryschool classroom represents an ideal setting for environmentalchange, through the provision of sit-stand desks. Whilstthe use of sit-stand desks in classrooms demonstrates positiveeffects in some key outcomes, evidence is currently limitedby small samples and/or short intervention durations, withfewstudiesadoptingrandomisedcontrolledtrial(RCT)designs. This paper describes the protocol of a pilot cluster RCT of a sit-stand desk interventioninprimaryschoolclassrooms.Methods/Design:A two-arm pilot cluster RCT will be conducted in eight primary schools (four intervention, four control)with at least 120 year 5 children (aged 9–10 years). Sit-stand desks will replace six standard desks in the interventionclassrooms. Teachers will be encouraged to ensure all pupils are exposed to the sit-stand desks for at least 1 h/dayon average using a rotation system. Schools assigned to the control arm will continue with their usual practice, noenvironmental changes will be made to their classrooms. Measurements will be taken at baseline, beforerandomisation, and at the end of the schools’academic year. In this study, the primary outcomes of interest will beschool and participant recruitment and attrition, acceptability of the intervention, and acceptability and complianceto the proposed outcome measures (including activPAL-measured school-time and school-day sitting, accelerometer-measured physical activity, adiposity, blood pressure, cognitive function, academic progress, engagement, andbehaviour) for inclusion in a definitive trial. A full process evaluation and an exploratory economic evaluation willalso be conducted to further inform a definitive trial

Potential intervention domain barriers and solutions to barriers using the Capability, Opportunity, Motivation to perform a Behaviour model (COM-B), Theoretical Domains Framework (TDF) and behaviour change techniques (BCT). (DOCX 45 kb)

SPIRIT checklist. (DOCX 51 kb)

In order to find novel antibacterial agents with superior antibacterial activity and overcoming multidrug resistance, a series of pleuromutilin derivatives with novel C(14) side chain were synthesized and evaluated for their in vitro antibacterial activities. The results of antibacterial acticities indicated that most of the derivatives showed potent activities against Gram-positive organisms. In particular, compound 10d exhibited the most potent inhibitory activity compared with pleuromutilin and linezoid, emerged as potential molecule for further investigation.

This paper theoretically studies the high-electron-mobility transistor (HEMT) driven by the terahertz radiation. It calculates the gate-to-source/drain admittance and the detection responsivity of the HEMT as a function of the signal frequency. It finds that the peaks of the admittances and the responsivity show redshift, and the heights of the peaks decrease with increasing the lengths of the source-to-gate and gate-to-drain spacing. Such phenomena may be useful in designing different HEMTs by utilizing the effects associated with the plasma oscillations excitation.

Diffuse alveolar hemorrhage (DAH) is a life-threatening clinical pathologic syndrome caused by a variety of diseases. We report a case of DAH related to combination therapy of chemoradiotherapy and erlotinib. As to know, DAH following chemoradiotherapy was only reported among hematopoietic stem cell transplant recipients with hematologic malignancies till now. DAH associated with chemoradiotherapy for oesophageal carcinoma has not been reported. This is the first DAH report on erlotinib-combined chemoradiotherapy for esophageal cancer. The authors believe epidermal growth factor receptor tyrosine kinase inhibitor erlotinib increased the lung injury. Molecular targeted drugs are gradually applied to be combined with chemoradiation, whether this combination will cause the increase of serious adverse reactions need further study. This case can provide certain reference for erlotinib in the treatment. Meanwhile, after long term hormone therapy for DAH, the patient was diagnosed with pneumocystis carinii pneumonia. It reminds us to attach importance to the immunosuppressive diseases after long-term hormone treatment.