宁海县恒海·金湾小区规划设计

通过对宁海县"恒海·金湾"小区的设计分析,阐述了如何将高层公寓、单身公寓、集体宿舍及邻里中心等几种不同的功能合理的组织到同一用地中,形成比较合理的功能布局和建筑形式,为今后同类项目设计提供了借鉴和参考。     

Synthesis of New Tricyclic 1,2-Thiazine Derivatives with Anti-Inflammatory Activity

New, tricyclic compounds containing a sulfonyl moiety in their structure, as potential safer COX inhibitors, were designed and synthesized. New derivatives have three conjugated rings and a sulfonyl group. A third ring, i.e., an oxazine, oxazepine or oxazocin, has been added to the 1,2-benzothiazine skeleton. Their anti-COX-1/COX-2 and cytotoxic effects in vitro on NHDF cells, together with the ability to interact with model membranes and the influence on reactive oxygen species and nitric oxide, were studied. Additionally, a molecular docking study was performed to understand the binding interaction of the compounds with the active site of cyclooxygenases. For the abovementioned biological evaluation of new tricyclic 1,2-benzothiazine derivatives, the following techniques and procedures were employed: the differential scanning calorimetry, the COX colorimetric inhibitor screening assay, the MTT, DCF-DA and Griess assays. All of the compounds studied demonstrated preferential inhibition of COX-2 compared to COX-1. Moreover, all the examined tricyclic 1,2-thiazine derivatives interacted with the phospholipid model membranes. Finally, they neither have cytotoxic potency, nor demonstrate significant influence on the level of reactive oxygen species or nitric oxide. Overall, the tricyclic 1,2-thiazine derivatives are good starting points for future pharmacological tests as a group of new anti-inflammatory agents.     

盐酸氟西汀的不对称合成

盐酸氟西汀是目前临床广泛使用的一种新型抗抑郁药物,市场销售的盐酸氟西汀是以外消旋体形式存在的。研究表明,盐酸氟西汀的一对对映体具有不同的药效及半衰期,对其对映体的不对称合成研究显得十分重要,针对近年来盐酸氟西汀的不对称合成方法研究的进展进行论述。