6-取代苯基-3(2H)哒嗪酮的合成、抗惊活性及其构效关系的研究

本文报道了14个6-取代苯基-4,5-二氢-3(2H)哒嗪酮和15个6-取代苯基-3(2H)哒嚎酮的合成及其抗电惊活性。其ED50值表明,以2′,4′-二氯苯基-3(2H)哒嗪酮的抗惊作用为最强。构效分析表明,苯环上的取代基对化合物的抗惊活性有明显影响,吸电子取代基和疏水性参数值较大的取代基有利于提高化合物的抗惊活性。     

6-取代苯基哒嗪的3位γ-氨基丁酸衍生物的合成及抗惊活性

GABA的合成类似物是开发新型抗惊剂和抗癫痫药物的新领域。由芳香醛与吗啉、氰化钾反应形成的α-芳基-α-(4-吗啉)乙腈,可对α,β-不饱和腈或酯进行1,4-加成,生成1,4-酮酸型化合物。此物与肼缩合,再经芳构化即得6-芳基-3(2H)哒嗪酮。后者再经氯化后。与GABA缩合,制备3-(N-GABA)-6-芳基哒嗪类及其分子内脱水产物3-(N-丁内酰胺)-6-芳基哒嗪类化合物。本文应用此法合成了17个上述苯代哒嗪的GABA衍生物,并初步测验了它们的抗惊(MES)活性。活性最强的是3-(N-GABA)-6-(2′,4′-二氯苯基)哒嗪(ED₅₀=21.05mg/kg)。     

4-甲氧羰基-4-N-丙酰苯胺基哌啶1位衍生物的合成及其镇痛作用

本文报道了一系列N-[-1(2-苯乙基-4-甲氧羰基-4-哌啶基]-N-丙酰苯胺(4-甲氧羰基芬太尼)哌啶环1位取代衍生物的合成及其镇痛活性;讨论了结构与镇痛活性之间的关系。药理试验结果表明,大部分化合物具有典型的吗啡样镇痛活性,是一类作用极强的麻醉性镇痛剂。特别是哌啶环1位β-苯环被取代乙烯基替代的化合物具有相当或接近子母体化合物的镇痛活性。其代表物1321的镇痛活性(ED_(50)=0.005mg/kg ip,小鼠,热板法)略强于4-甲氧羰基芬太尼(ED_(50)=0.0063 mg/kg)。     

消旋棉酚拆分的研究——Ⅳ.苏(-)或(+)-1-(对硝基苯基)-1,3-二羟基丙胺-2为拆分剂

本文介绍以光学活性苏-1-(对硝基苯基)-1,3-二羟基丙胺-2为拆分剂,与消旋棉酚缩合,用常压柱色谱或溶剂结晶法分离得到两个光学纯的非对映体,然后分别水解得(+)和(-)-棉酚。     

High-definition imaging of trabeculectomy blebs using spectral domain optical coherence tomography adapted for the anterior segment

Background:  The aim of this work was to image trabeculectomy blebs using spectral domain optical coherence tomography (SDOCT).
Methods:  In this prospective cross-sectional study, patients who had undergone trabeculectomy with at least 3 months of follow up were included. Blebs were imaged using an adapted SDOCT system (Cirrus HD-OCT, Carl Zeiss Meditec Inc., Dublin, CA, USA) and time domain anterior segment optical coherence tomography (ASOCT) (Visante OCT, Carl Zeiss Meditec Inc.). An observer masked to clinical data assessed the utility of SDOCT and ASOCT in visualizing structures in successful and failed blebs.
Results:  Fifty-one eyes were imaged, of which 43 (84.3%) were successful. SDOCT showed wall thickening (93.0% vs. 67.4%, P  = 0.006) and discrete hyporeflective spaces in the wall (88.4% vs. 14.0%, P  < 0.0001) in a greater proportion of successful blebs than ASOCT. SDOCT showed the bleb cavity (23.3% vs. 48.8%, P  = 0.02), scleral flap (34.9% vs. 90.7%, P  < 0.0001), subflap space (20.9% vs . 72.1%, P  < 0.0001) and ostium (9.3% vs. 88.4%, P  < 0.0001) in fewer successful blebs than ASOCT. The internal ostium was not visualized in any failed bleb using SDOCT, whereas ASOCT showed the ostium in 87.5% of failed blebs ( P  = 0.001). SDOCT showed cystic spaces in the bleb wall in a greater proportion of successful blebs than failed blebs (88.4% vs. 37.5%, P  = 0.005).
Conclusions:  SDOCT imaging was able to show fine superficial features in the bleb wall. However, SDOCT had limited clinical utility in that it did not provide useful information about deep features such as flap position, bleb cavity formation or patency of the subflap space and internal ostium.     

Over thousand liver transplants performed at a liver transplant center in China

Recently the Liver Transplantation Center of the First Affiliated Hospital,Zhejiang University School of Medicine announced the successful performance of 1021 liver transplants by October 17,2011.At a gathering celebrating this event,experts from the USA and China highly appreciated this achievement made     

EGFR expression as a predictive marker in esophageal squamous cell cancer:Review article

Esophageal cancer（ EC ） is a highly aggressive disease and 8＇h leading cause of death worldwide. Squamous cell cancer is the main histological type in China. Recent improvements in both surgical techniques and adju- vant/neoadjuvant radiotherapy and chemotherapy approaches have increased the survival of patients with the loco- regional disease. However, most of the patients with EC have advanced disease either at diagnosis or at follow-up. Despite recent advances in the treatment, these patients still do poorly. Over expression of the epidermal growth factor receptor in esophageal the role of epidermal growth cancer is associated with poor prognosis. However, very few researches have examined factor receptor（EGFR） in prediction and therapeutic sensitivity to esophageal squamous cell cancer（ESCC）. If pretherapeutic identification of esophageal squamous cell cancer which does not re- spond to chemoradiotherapy （CRT） can be done, it will help to improve the outcome of patients by selecting responders to treatment. In this review we describe the predictive significance of EGFR expression in ESCC.