英汉对照药物化学介绍

选自《药学英语》第四版(史志祥主编,人民卫生出版社,2011年)

Medicinal or pharmaceutical chemistry is a discipline at the intersection of chemistry and pharmacology, and involves the identification, synthesis and development of new chemical entities suitable for therapeutic use. The content of medicinal chemistry also includes the study of existing drugs, their chemical structure, physical and chemical properties, chemical stability, biological properties, structure-activity relationships (SAR), metabolism, chemical mechanism of interaction between drugs and biological targets, etc.

药物化学是化学和药理学之间的交叉学科，其内容涉及适合于治疗用途的新化学单体药物的鉴定、化学合成和开发利用。药物化学的内容还包括对现有药物的化学结构、理化性质、化学稳定性、生物活性特征、构效关系（SAR）、体内代谢以及药物与其生物靶点相互作用的化学机制的研究等。

Medicinal chemistry is a discipline mainly concerned to new drug research. Early advances in medicinal chemistry were concerned principally with the estimation, isolation, structural determination, and synthesis of medicinal agents of natural origin. A second major area was the synthesis of simplified fragments of complex drug molecules. Recent medicinal chemistry obtained a great progress by the explosive development of molecular biology, physical chemistry, organic chemistry, high-speed computer and new, powerful analytic methods including various types of chromatography, radioimmunoassay, mass spectrometry, X-ray crystallography, and nuclear magnetic resonance spectroscopy, etc.

药物化学是与新药研究有关的一门学科。药物化学的早期发展主要涉及天然药活性成分的预测、分离、结构鉴定以及合成研究等方面。第二个主要的研究领域是对复杂药物分子进行结构简化。近期的药物化学受分子生物学、物理化学、有机化学、高速计算机及新尖端分析方法（各种色谱分析、放射性免疫鉴别、质谱、X射线晶体分析法和核磁共振）的爆炸性进展的影响而获得迅速的发展。

The science of medicinal chemistry involves the design and synthesis of novel drugs. There are two major considerations that have to be taken into in any drug design project. First of all, drugs interact with molecular targets in the body, and so it is important to choose the correct target for the desired pharmaceutical effect. It is then a case of designing a drug that will interact as powerfully and selectively as possible for that target—an area of medicinal chemistry known as pharmacodynamics. Secondly, a drug has to travel through the body in order to reach its target, so it is important to design the drug so that it is able to carry out that journey. This is an area known as pharmacokinetics.

药物化学科学包含新药的设计和合成。在所有药物设计领域中，有两个主要因素不得不被考虑。首先，药物在体内和分子靶位相互作用，因此，为了得到预期的疗效，选择正确的靶位非常重要。接下来需要设计一种药物与其靶位尽可能强有力地、选择性地相互作用。这一药物化学领域被称为药效动力学。其次，为了到达靶位，药物必须通过机体而被吸收，因此设计的药物能够完成这一“旅程”非常重要，这一领域被称为药代动力学。

How do drugs have their effect in the human body? How are new drugs discovered and designed to be as effective as possible? Medicinal Chemistry offers an engaging insight in this field, and reflects the change in emphasis of newly pharmaceutical research, takes us from the largely trial-and-error approach to drug design to the rational approach, and explores the most recent advances in molecular biology and

选自《药学英语》第四版(史志祥主编,人民卫生出版社,2011年)

genetics which have revolutionized drug design. Virtually, a large numbers of analogs were synthesized based on the structure of a known active compound, but little was known about the detailed mechanism of drug action or the structures of the targets with which they interacted. Advances in the biological sciences have now resulted in a much better understanding of drug targets and the mechanisms of drug action. As a result, drug design is as much 'target oriented' as 'lead compound oriented'. 药物如何在体内产生药效？如何发现和设计尽可能有效的新药？在这一领域，药物化学不但能够提供所需的知识，而且能反映新药研究的规律及重点变化趋势，使我们从大量反复试验的方法过渡到理性的合理设计，并利用分子生物学和遗传学的最新进展，彻底改变了药物设计。实际上在已知活性化合物结构的基础上合成了大量类似物，但是对于药物作用的详细机制或与其相互作用的靶位结构却知之甚少。现在，生命科学的发展已经使我们对药物靶位和药物相互作用机制有了更好的理解，致使药物设计的“靶位导向”越来越接近于“先导化合物导向”。

The chief role of the medicinal chemist is to design and synthesize the target structures required. Therefore, the medicinal chemist is an essential member of any drug design team since he or she has to identify whether proposed target structures are likely to be stable and whether they can be synthesized or not.

药物化学家的主要任务是设计、合成所需要的目标结构。因此药物化学家是每一个新药设计团队中不可缺少的成员，他（她）必须辨别候选的目标结构是否稳定、能否被合成。 With a striking new knowledge and greatly enriched learning features, the new achievement of medicinal chemistry conveys the fascination of working in a field which overlaps the disciplines of organic chemistry, biochemistry, physiology, microbiology, cell biology, pharmacology, computational chemistry, pharmacognosy, molecular biology, statistics, and physical chemistry. However, the rapid advances made in two particular scientific areas are worth emphasizing: Molecular biology and genetic engineering have produced a deluge of potential new targets for drug design and have unraveled the structures and mechanisms of traditional targets; the molecular biology and computer science especially furnish a new insight for the rational research and development of new drugs in medicinal chemistry.

随着相关学科的深入发展和知识领域的更新，药物化学学科获得了新的发展机遇。药物化学相关学科主要包括有机化学、生物化学、生理学、微生物学、细胞生物学、药理学、计算化学、生药学、分子生物学、统计学和物理化学等。然而，两个特定科学领域的迅速发展值得关注：分子生物学和基因工程已经为药物设计提供了大量的潜在新靶位，并弄清了传统靶位的结构和机制；分子生物学和计算机科学又为药物化学中的新药研发提供了全新的视角。 In medicinal chemistry, the search of lead compound and its structural modification are important two steps for looking for new drugs. The lead discovery processes include random screening, drug metabolism studies, clinical observations of drug action, rational approaches to lead discovery and computer-assisted drug design techniques, etc. Many approaches can be used for optimization of lead compound, such as lead optimization by pro-drug design, by bioisosterism, by soft drug or hard drug design, by QSAR method, etc. Computer aided drug design (CADD), a sophistic drug discovering techniques, is a topic area in modern medicinal chemistry for the discovery of lead compound and its pharmaceutical development.

在药物化学中，先导化合物的研究及其结构优化是新药发现的两个重要步骤。先导化合物

选自《药学英语》第四版(史志祥主编,人民卫生出版社,2011年)

的发现中，常用的方法包括随机筛选、药物代谢研究、药物作用的临床观察、合理设计及计算机辅助设计技术等。而对先导化合物的结构优化中，前药设计、电子等排原理、软药和硬药设计及定量构效关系等方法最为常用。计算机辅助药物设计（CADD）是新药发现的尖端技术和前沿领域，是在现代药物化学中寻找先导化合物及其药用开发研究的前沿领域。

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