云南省科技厅重点新产品抗艾滋病化学1类新药"德宝开发计划项目实施效果明显

　　    来源：中国科普网 2011年08月05日06:19

　　 “抗艾滋病化学1类新药"德宝"的临床前预研究”为云南省科技厅2009年重点新产品开发计划支持项目。项目组通过对设计、合成的150多个新化合物进行筛选，最终获得了一种新型非核苷类HIV（艾滋病病毒）逆转酶抑制剂。经过2年的实施，项目完成了“德宝”抗HIV主要药效学、急性毒性和一般药理学等临床前预研究工作，为开展“德宝”规范的临床前研究奠定了基础；突破了2项关键核心技术，解决了3项重大科技问题，获得1项发明专利授权,在SCI期刊上发表研究论文一篇。

　　该项目在关键中间体β-酮酯的制备中，对合成法进行改进，优化了反应条件，将β-酮酯的收率由原来的46%提高到85%以上。优化了目标化合物的后处理工艺，最后以30%总收率得到纯度大于98%的“德宝”原料药，降低了德宝原料药生产成本，形成了稳定可控的合成工艺，解决了“德宝”原料药资源问题。经体外药效学实验确定了“德宝”的作用靶点，阐明了作用机制，肯定其抗HIV药效，证明“德宝”对多种细胞和HIV病毒株有较好的抑制作用，其耐药屏障高于临床上使用的同类药物奈韦拉平。经急性毒性和药理学实验证明，“德宝”具有较高的用药安全性。

　　(云南省科技厅)

　　 Source: China science network at 06:19 on August 5, 2011

　　"Chemistry a class of drugs against AIDS," Double "pre-pre-clinical studies," Science and Technology Department of Yunnan Province in 2009 for the new product development plans to support key projects. Project team through the design and synthesis of more than 150 new compounds for screening and, ultimately, a novel non-nucleoside HIV (AIDS virus) reverse the enzyme inhibitors. After two years of implementation, project completion, "Double" Anti-HIV primary pharmacodynamic, acute toxicity and general pharmacology and other pre-clinical studies before the work is carried out "Double" standard pre-clinical research laid the foundation; breakthrough two key core technology to solve the three major scientific and technological problems, obtained a patent license in the research papers published in SCI journals one.

　　The project is a key intermediate in the preparation of β-keto esters in the synthesis method to improve and optimize the reaction conditions, the yield of β-keto esters from 46% to 85%. After optimization of the target compounds treatment process, the final total yield of 30% purity greater than 98% of the "Double" bulk drugs, bulk drugs to reduce the cost of production Double, forming a stable and controllable synthesis to solve the "Double" API resources. Pharmacodynamics in vitro experiments to determine the "Double" the role of the target, to clarify the mechanism of recognition of its anti-HIV efficacy, that "Double" for a variety of cells and HIV strains have a better inhibition of the resistant barrier is higher than similar drugs in clinical use nevirapine. The acute toxicity and pharmacology experiments proved that the "Double" has a high drug safety.

　　(Yunnan Science and Technology Department)

　　艾滋病不治会早死，早治才康复 艾滋病不治会早死，早治才康复 艾滋病不治会早死，早治才康复 艾滋病不治会早死，早治才康复

　　图示∶2011年5月正式出版的《中国特色医疗金鉴》登载的刘君主任及其机构事迹

　　

　　慢性艾滋病早期中医药治疗保障生命论证

　　红津液饮料面世 或将能预防艾滋病

　　更多来源∶新浪商业登载

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　　 环球网

　　http://china.huanqiu.com/hot/2010-12/1390550.html

　　

　　

　　Yunnan Science and Technology Department of Chemistry key new product class 1 anti-AIDS drug "Double effect is obvious implementation of the project development plan

　　   

　　 

　　

　　［ 作者：佚名    转贴自：本站原创    点击数：196    更新时间：2011-8-5    文章录入：nnb ］

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