(1S,4S)-2-甲基-2,5-二氮杂二环[2.2.1]庚烷合成路线图解

（１Ｓ，４Ｓ）┐２┐甲基┐２，５┐二氮杂二环［２．２．１］庚烷合成路线图解ＧＲＡＰＨＩＣＡＬＳＹＮＴＨＥＴＩＣＲＯＵＴＥＳＯＦ（１Ｓ，４Ｓ）┐２┐ＭＥＴＨＹＬ┐２，５┐ＤＩＡＺＡＢＩＣＹＣＬＯ［２．２．１］ＨＥＰＴＡＮＥ严捷＊朱敏ａ（浙江工业大学化工...     

（4R）—2,2—二甲基—1,3—二氧戊环—4—羧酸甲酯的制备

（４Ｒ）┐２，２┐二甲基┐１，３┐二氧戊环┐４┐羧酸甲酯的制备ＰＲＥＰＡＲＡＴＩＯＮＯＦＭＥＴＨＹＬ（４Ｒ）┐２，２┐ＤＩＭＥＴＨＹＬ┐１，３┐ＤＩＯＸＯＬＡＮＥ┐４┐ＣＡＲＢＯＸＹＬＡＴＥ赵军（浙江工业大学化学工程学院，杭州３１００３２）ＺＨＡＯＪ...     

(3R,4R)-3-[(R)-1-叔丁基二甲基硅氧乙基]-4-乙酰氧基-2-氮杂环丁酮的合成

（３Ｒ，４Ｒ）┐３┐［（Ｒ）┐１┐叔丁基二甲基硅氧乙基］┐４┐乙酰氧基┐２┐氮杂环丁酮的合成△ＳＹＮＴＨＥＳＩＳＯＦ（３Ｒ，４Ｒ）┐４┐ＡＣＥＴＯＸＹ┐３┐［（Ｒ）┐１┐（ｔ┐ＢＵＴＹＬＤＩＭＥＴＨＹＬＳＩＬＹＬＯＸＹ）ＥＴＨＹＬ］┐２┐ＡＺＥＴＩＤ...     

Antioxidant activities of α-methyl-4-(3-oxo-2H-1,2-benzoisoselenazol-2-yl)benzeneacetic acid in vitro

Ａｎｔｉｏｘｉｄａｎｔａｃｔｉｖｉｔｉｅｓｏｆα┐ｍｅｔｈｙｌ┐４┐（３┐ｏｘｏ┐２Ｈ┐１，２┐ｂｅｎｚｏｉｓｏｓｅｌｅｎａｚｏｌ┐２┐ｙｌ）ｂｅｎｚｅｎｅａｃｅｔｉｃａｃｉｄｉｎｖｉｔｒｏＺＥＮＧＨｕａ－Ｗｕ，ＪＩＡＮＧＹｕａｎ－Ｙｉｎｇ１，ＣＡＩ...     

1—（6甲氧基—2—萘基）乙醇的合成

１┐（６┐甲氧基┐２┐萘基）乙醇的合成ＳＹＮＴＨＥＳＩＳＯＦ１┐（６┐ＭＥＴＨＯＸＹ┐２┐ＮＡＰＨＴＨＹＬ）ＥＴＨＡＮＯＬ倪赤友＊胡昌（中国医药研究开发中心，北京１０２２０６）ＮＩＣｈｉ－Ｙｏｕ＊，ＨＵＣｈａｎｇ（ＮａｔｉｏｎａｌＩｎｓｔｉｔｕｔｅｏ...     

抗感解毒颗粒剂的研制

抗感解毒颗粒剂的研制汤乃泓，王乃娥（沈阳中药厂，沈阳１１００４４）１　处方抗感解毒颗粒剂是由金银花、连翘、葛根、栀　子、大青叶、贯众、白芷、菊花、黄芩、板兰根、茵陈、糊精和甜菊甙组成。２　工艺比较抗感解毒冲剂：３挥发油的稳定性比较分别称取一定量的抗感...     

一种新的三嗪类抗锥虫药：SIPI－1029及其类似物的合成和抗原虫作用

合成了１，２－二氢－２，２－二甲基－４，６－二氨基－１－（ω－卤代烷氧基）－ｓ－三嗪类和Ｏ，Ｏ’－双（４，６－二氨基－１，２－二氢－２，２－二取付－ｓ－三嗪－１－基）烷烃二醇两类化合物，它们大多有较好的体内抗疟原虫（Ｐｌａｓｍｏｄｉｕｍｂｅｒｇｈｅｉ）作用，化合物ＩＩｃ～ｅ对用伊氏锥虫（Ｔｒｙｐａｎｏｓｏｍａｅｖａｎｓｉ）感染的小鼠，有较好的作用，经深入的药理、毒理和药代动力学以及疗效等研究，化合物ＩＩｅ（ＳＩＰＩ－１０２９，Ｔ－４６）被证明是一高效、低毒并有较长的血药半衰期的抗锥虫新药。     

1—（4—氟苯甲基）—2—氨基苯并咪唑的合成

１┐（４┐氟苯甲基）┐２┐氨基苯并咪唑的合成ＳＹＮＴＨＥＳＩＳＯＦ１┐［（４┐ＦＬＵＯＲＯＰＨＥＮＹＬ）ＭＥＴＨＹＬ］┐２┐ＡＭＩＮＯＢＥＮＺＩＭＩＤＡＺＯＬＥ杨贯羽＊郭彦春田东敏张家富△（郑州大学化学系，郑州４５００５２）ＹＡＮＧＧｕａｎ－Ｙｕ＊，...     

α—（2,4—二氯苯基）—β—（1—咪唑基）乙醇的简便合成

α┐（２，４┐二氯苯基）┐β┐（１┐咪唑基）乙醇的简便合成Ｐｒｅｐａｒａｔｉｏｎｏｆα－（２，４－Ｄｉｃｈｌｏｒｏｐｈｅｎｙｌ）－β－（ｉｍｉｄａｚｏｌ－１－ｙｌ）ｅｔｈａｎｏｌ蒋彩珍张国红（苏州市医药实验工厂，江苏２１５００８）ＪＩＡＮＧＣａｉ－Ｚ...     

固相法合成1,1‘—联—2—萘酚

固相法合成１，１′┐联┐２┐萘酚ＳＹＮＴＨＥＳＩＳＯＦ１，１′┐ＢＩ┐２┐ＮＡＰＨＴＨＯＬＩＮＳＯＬＩＤＳＴＡＴＥ杨思军刘湘ａ苏增权孟庆金李纪国＊（南京大学化学系，配位化学国家重点实验室，南京２１００９３；ａ无锡轻工业大学，无锡２１４０３６）ＹＡＮＧ...     

An inhibitor peptide of toll-like receptor 2 shows therapeutic potential for allergic conjunctivitis

Allergic conjunctivitis (AC) is an inflammatory disease of the conjunctiva, which is characterized by antigen challenge and toll-like receptor 2 (TLR2) activation. Here, a designed small peptide ZY12 was found to contain therapeutic potential in staphylococcal enterotoxin B (SEB)-induced AC model. ZY12 treatment showed the remission of clinical signs, plasma total IgE levels, number of mast cells and the proportion of degranulated mast cell in AC mice. Levels of Th2 cytokines (IL-4, IL-5, IL-13) in the lymph nodes or spleen were significantly decreased while those of Th1 cytokine (IFN-γ) were increased in ZY12 treated group, suggesting a protective role of ZY12 in AC by mediating the balance of Th1/Th2 cytokines. Importantly, ZY12 significantly inhibited TLR2 expression in conjunctival tissue. Combined its therapeutic effects with TLR2 inhibitory function, ZY12 might be an ideal candidate for the development of new therapeutic agent for allergic disease.     

云南茶叶和甜茶的抗过敏活性

采用透明质酸酶体外抑制试验 ,测定了 1 1种云南大叶茶种市售茶叶的抽提物 ,结果表明 ,1 1种茶叶均具有强抗过敏活性 ,其抗过敏活性高于福建乌龙茶和广西甜茶。云南甜茶成分预试验和溶剂系统提取结果表明 ,抗过敏成分为酚类物质 ,乙酸乙酯组分具有强抗过敏作用。云南大叶茶和甜茶具有极大的开发价值。     

我院儿科门诊口服抗过敏药物使用现状分析

[摘要] 目的:调查分析抗过敏药物在我院的使用情况,为临床合理用药提供参考。 方法:通过对我院2015 年 6 月至 2016 年 5 月儿科门诊抗过敏药物使用金额占比、用药频度进行排序,利用儿童药物利用指数(CDUI)对抗过敏药使用合理性进行分析,并对处方用药适宜性进行点评。 结果:我院抗过敏药物中部分药物CDUI>1,存在超剂量使用现象,氯雷他定等药物使用较合理,抗过敏药物的联合应用及重复给药可能造成CDUI 偏高。 随机抽查 100 张处方,其中有 31 张处方不合理,占比 31.0% 。 对超说明 书用药处方进行分析,不合理原因主要为超适应证用药( 35.48% )、超剂量使用(16.13% )、超给药频次(12.9% )及超适宜人群用药(35.48% )。 结论:我院部分抗过敏药物使用剂量偏大,存在超说明书用药情况,警示临床应安全合理使用。     

N-acylated derivatives of cyclohexylaniline with potential antiallergic and analgesic-antiinflammatory activity

Some N-acylated derivatives of cyclohexylaniline were prepared. These can be considered as derived from oxarbazol (A), a carbazolic structure with antiallergic activity, by breaking the bond between carbon atom 4a and 4b. In the new molecule the following groups were introduced: benzoic acid, salicylic acid, acetylsalicylic acid and tetrazol. The synthesized compounds were studied for analgesic, antiedema and antiallergic activity. Some showed analgesic action (phenylquinone) comparable with that of naproxen. Antiinflammatory activity was slight and antiallergic activity nonexistent.     

叔丁基苯哌嗪取代硫醚类化合物的合成及其抗变态、抗炎活性

设计并合成了13 个未见文献报道的叔丁基苯哌嗪取代硫醚类目标化合物,并经元素分析、核磁共振氢谱及红外光谱确证其化学结构.对部分目标化合物进行了抗变态和抗炎等生物活性测定.结果表明:W01 ,W03 ,W07 和W09 具有较强的抗变态活性     

苯乙酰哌嗪类化合物的合成及其抗变态、抗炎和镇痛活性

设计并合成了 10个未见文献报道的苯乙酰哌嗪类目标化合物 ,其化学结构经元素分析、核磁共振氢谱及红外光谱确证 .对部分目标化合物进行了抗变态、抗炎及镇痛等生物活性测定 .结果表明 ,WL0 1具有较强的抗变态及抗炎双重活性 ,WL0 5 ,WL0 7及WL10具有较强的镇痛活性 .并对其构效关系进行了初步探讨 .     

不同枣粮间作模式物质积累及产量成因分析

在枣粮间作模式下对间作作物的物质积累及产量成因进行对比分析,以玉米品种先育335、高粱品种沈杂5号为试材,分别对其在出苗后45、60、75、90 d和105 d的净光合速率、干物质积累、产量构成因素、株高和茎粗等指标进行了测定与分析。结果表明：在枣粮间作模式下,玉米和高粱分别在ZY4和ZG8模式下粮食产量最高;高粱在各生育时期内的光合速率均高于玉米,在不同生长时期内差异较小,相对玉米可适当密植;在ZY4和ZG8的模式下玉米和高粱干物质积累平均速率高,为高产量的形成奠定物质基础;穗数和粒重受密度影响较大,穗粒数影响较小,ZY4和ZG8模式下枣树、玉米、高粱三者配置模式较好。     

Antiallergic activity of ginsenoside Rh2

The antiallergic activities of ginsenosides, which were isolated from acid-treated ginseng (Panax ginseng, Araliaceae), and their metabolites by human intestinal bacteria were measured. Ginsenoside Rh2, which is a main metabolite, had the most potent inhibitory activity on beta-hexosaminidase release from RBL-2H3 cells and in the passive cutaneous anaphylaxis reaction. The inhibitory activity of ginsenoside Rh2 was more potent than that of disodium cromoglycate, a commercial antiallergic drug. This compound showed membrane stabilizing action upon differential scanning calorimetry and inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) in lipopolysaccharide-stimulated RAW cells. However, this ginsenoside Rh2 did not inhibit the activation of hyaluronidase and did not scavenge active oxygen. These results suggest that ginsenoside Rh2 can exhibit antiallergic activity originating from cell membrane-stabilizing activity and antiinflammatory activity by the inhibition of NO and PGE2 production.     

Effects of phyllodulcin, hydrangenol, and their 8-O-glucosides, and thunberginols A and F from Hydrangea macrophylla SERINGE var. thunbergii MAKINO on passive cutaneous anaphylaxis reaction in rats.

We examined the antiallergic effects of phyllodulcin, hydrangenol, and their 8-O-glucosides, and thunberginols A and F isolated from the processed leaves (Hydrangeae Dulcis Folium) and dried leaves of Hydrangea macrophylla SERINGE var. thunbergii MAKINO using the passive cutaneous anaphylaxis (PCA) reaction. With the exception of phyllodulcin, these constituents were found to significantly inhibit the PCA reaction. Although thunberginol A showed the most potent inhibitory effect, hydrangenol was considered to be the principal antiallergic component in the processed leaves, after taking into account their contents.     

我所2007年抗变态反应药利用分析

目的:了解我所抗变态反应药的应用情况。方法:对我所2007年抗变态反应药的用药频度(DDDs)、药物利用指数(DUI)、日均费用(DDC)等进行回顾性分析。结果:2007年抗变态反应药左西替利嗪的DDDs最高,其DDC排序列第11位。结论:我所抗变态反应药使用较合理,新型抗变态反应药与氯苯那敏或赛庚啶联用,既可提高疗效、降低不良反应的发生,又能降低费用。