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制药工程 专业英语 Unit 21
药理作用:通过其余体内大分子进行手性识别和匹配产生活性而起到治疗的
作用。一对对映体的手性药物在手性结构上的差异往往会导致它们在药 理活性、药物代谢及毒性等方面产生不同的体内的药理活性。
根据一对对映体的手性药物药理作用和药效,可分为:
一个有药理活性,而它的对映体没有药理活性;
一对对映体有相反的药理活性,一个有活性,对映体甚至可能显毒性; 一对对映体药理活性相同,但有差别; 一对对映体有迥乎不同的药理活性; 一对对映体药理活性完全相同。
Chiral technology has progressed a long way. This article is confined to its most visible application in pharmaceuticals, but its role extends well into other fields. It has found applications in biochemicals, pesticides, aroma and flavour chemicals, dyes and pigments, liquid crystals, non-linear optical materials, and polymers. In fact, chiral technology represents a huge commercial business opportunity that has yet to be fully realized.
While in the past many drugs developed synthetically have not been chiral, those derived from natural products almost always are (for example, the penicillins). It is obvious that single-isomer drugs are more specific in mode of action compared with the corresponding racemates.
2
Words
encompass chirality (a. chiral) enantiomer diastereomer mesomer racemate unwanted clear-cut tolerability impetus building block cholesterol menthol stationary/mobile phase assay chiral selector tartaric acid ensuing embryos counterclockwise vt. 包含;包围,环绕 n. 手(征)性 (a. 手(征)性的) n. 对映(异构)体 n.非对映(异构)体 n. 内消旋体 n. 外消旋体(化合物) a. 有害的;不需要的 a.清晰的;轮廓鲜明的 n.耐受性; 容忍度 n. 动力;促进;冲力 n. 砌块;积木;构件 n.胆固醇;胆甾醇 n. 薄荷醇,薄荷脑 固定相/流动相 n.化验,试验;vt. 分析,测试 手性选择试剂 酒石酸 a. 跟着发生的 n. 胚胎;晶胎 adv. 逆时针地
如果某一药物是手性的,在生物学范畴里其对映体总具有不 同的活性。一种药物可能会与细胞受体发生特异性的相互作用而 产生期望的结果,而另外一种药物则可能产生无用的作用,或通 过某些其他的相互作用而可能导致有害的作用。
In the clear-cut example where one isomer of a chiral compound is ‘good’ and the other ‘bad’, there is obvious benefit from developing the drug as the single isomer to enhance its safety and tolerability. In addition, this can also speed the progress of the drug through regulatory channels, thereby saving R&D costs. 在明确的例子中,手性化合物的一个异构体是“对人体有益的 ”,而另一个异构体则是“对人体有害的”,发展单一异构体的 药物以加强其安全性和耐受性,可以获得显而易见的利润。此外 ,这也可以通过监管渠道加快药品的发展,从而节省研发成本。
手性技术已走过了很长的发展历程。本文不仅限于它在药 物方面有着最显著的应用,其作用也扩展到其他领域中。它已 应用于生化药剂,农药,芳香和香料化学品,染料及颜料,液 晶,非线性光学材料和聚合物。事实上,手性技术显示出一个 巨大的尚未得到充分实现的商业机遇。
A summary of available chiral technology for obtaining singleisomers is listed below. Some of these, such as fermentation and crystallisation, have long been available to chemists but their successful application required specialist expertise (for example, microbiology for the former, physical chemistry for the latter). Their use has also been patchy, as experience indicated that they could only address some chiral problems. 获得单一异构体的实用手性技术总结如下。其中的一些方法, 如发酵和结晶,长期以来一直被化学家所采用,但它们的成功应 用需要专门的技术(例如,发酵需要微生物学知识,而结晶需要 物理化学知识)。但它们的作用是补缀的,因为经验表明,它们 只能解决某些手性问题。
虽然过去的许多已开发的合成药物并不是手性的,但那些来 自天然产物的药物则几乎总是手性的(例如,青霉素类)。很显 然,单一异构体药物比相应的外消旋体具有更特效的作用模式。
However this, together with the incentives for developing singleisomers for clinical and commercial benefits, does not solely account for the fact that around 80% of drugs entering development are chiral, exclusively now in single-isomer form.
手性几乎并不是化学中的新概念,但在过去的几年里手性技 术的进步已对制药研究和开发产生了越来越大的影响。如今,手 性技术对合理的药物设计正起着强大的影响。
It aids the conception and discovery of new receptor-based or enzyme-inhibiting small molecule drugs, especially where high selectivity of action is sought. Its acceptance is largely because there is now an abundance of technology in place for the manufacture of single-enantiomer chiral drugs.
The professional English of pharmaceutical engineering
Wang Xinliang
East China University of Science and Technology
概念简介
手性药物: 具有手性结构及药理活性的具有治疗疾病作用的手性化合物。
Chirality is hardly a new concept in chemistry, yet advances in chiral technology have had a growing impact on pharmaceutical research and development over the past few years. Chiral technology now exerts a strong influence on rational drug design.
对那些不熟悉手性技术的人们而言,该术语包括生产单一手 性形式(对映体)化合物的技术,具有足够复杂性的分子结构的化 合物是手性的;也就是说,这时分子不能与其镜像叠加(重合)。 随着分子变得更加复杂,药品的特异作用性增加;对更具特异性 作用的药品的追求将导致更大比例的药品为手性。
If a drug is chiral, then in biological terms the enantiomers invariably differ in activity. One may specifically interact with a cell receptor to produce the desired outcome while the other might have no useful application or might have an unwanted effect through some other interaction.
尽管如此,一个不争的事实是:进入开发的药品中大约80 %的是手性的,而现在则全为单一异构体形式;为了临床和商 业利益开发单一异构体并不是其唯一的理由。
Rather this is a consequence of the increased complexity of drug structures today as greater selectivity of action is sought. As an indication of this increased complexity, a drug today will typically need around a dozen steps for its synthesis from basic organic chemicals. About ten years ago, only half this number would, on average, have been required. 相反,这是一个为了寻找到更大特异性的相互作用而日益增 加药物结构的复杂性的结果。作为这种日益增加的复杂性的一个 标志,现在的药物合成从基本有机化学品开始,通常需要大约12 步。而大约十年前,平均而言,则合成步骤的数字只需要一半。