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新药的发展非常迅速,目前进入临床使用的药物95％是1935年以后出现的。新药的品种繁多,现就几个主要方面综述新药开发途径的进展动态。 一、合理设计新药 七十年代以前,药物化学家常需广泛合成筛选成千上万的化合物,凭机遇发现新药。例如,经过研究的磺胺类化合物已上万种,而进入临床使用的不过几十种。至今,大约从一万个化合物中才能筛选出一个可用于临床的新药。这种筛选盲目性大、命中率低。因此,药物学家开始总结药物合成的规律,合理地定向设计新药。
The development of new drugs is very rapid, 95% of the drugs currently in clinical use are emerging after 1935. A wide range of new drugs, are summarized in several major aspects of developments in new drug development trends. First, the rational design of new drugs Before the seventies, drug chemists often need extensive synthesis screening of thousands of compounds, with the opportunity to discover new drugs. For example, there have been tens of thousands of sulfonamides that have been studied, but dozens of for clinical use. To date, only about 10,000 compounds have been screened for a new drug that is clinically useful. This screening blindness, hit rate is low. Therefore, pharmacologists began to summarize the laws of drug synthesis, rationalize the design of new drugs.