摘要
列举近年开发的新药以说明药物设计的途径。从中草药中分出的活性物质,是新药开发的源泉。天然成分以及现有药物的结构改造常能增强其药理作用,拓宽某作用谱、降低毒性与提高治疗指数。定量构效关系的运用可避免盲目筛选药物,提高命中率。应用前药原理适当改造药物结构,可改变其理化性质,从而改善其吸收、分布与代谢。对某些酶的抑制以及对某些受体作用的探索,将导致新药的发现。
Some principles of drug design are reviewed with appropriatelyillustrated examples. Among the bioactive substances isolated recently fromChinese native plants, some have been served as useful drugs. Molecular modifi-cation of the natural ingredients as well as existing drugs may be expected forthe enhancement of potency, spectrum of activity and increase of the therapeuticratio.Quantitative structure-activity studies may be useful in some cases indesigning therapeutic agents without exhaustive synthesis and screening. Prodrugscan be utilized to modify the physicochemical properties of various drugs so asto modify their pharmacokinetics and consequently to improve absorption,distribution, and metabolism. Many drugs are designed after investigation oftheir pharmacological effect to enzyme inhibition or receptor antagonism.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1989年第7期292-298,共7页
Chinese Journal of Pharmaceuticals
关键词
中草药
天然成分
新药
制备
natural ingredients, enzyme inhibition, QSAR, receptor antagonism, specificity, molecular modification
