To detect and evaluate biological activity, bioassays are used to differentiate the effect and potency of the test agent compared with controls of known action and effect I In vitro n Vivo Cell culture Disease-specific Animal models
• To detect and evaluate biological activity, bioassays are used to differentiate the effect and potency of the test agent compared with controls of known action and effect. In vitro Cell culture In vivo Disease-specific Animal models
New methods, as high throughput screening, are capable of examining 15000 chemical compounds a week using 10-20 biological assays High-throughput screening (HTS) s a method for scientific experimentation especially used in drug discovery and relevant to the fields of biology and chemistry
• New methods, as high throughput screening, are capable of examining 15000 chemical compounds a week using 10-20 biological assays. • High-throughput screening (HTS) is a method for scientific experimentation especially used in drug discovery and relevant to the fields of biology and chemistry
To be effective this requires a sizea ble and chemically diverse collection of compounds to examine, which many pharmaceutical and chemical companies have in“ chemicallibraries,” (为了有效地利用它,这需要有相当大量 的不同化学物质来测试,通常许多制药 公司或化学品公司有“化合物库
• To be effective, this requires a sizeable and chemically diverse collection of compounds to examine, which many pharmaceutical and chemical companies have in “chemical libraries. ” （为了有效地利用它，这需要有相当大量 的不同化学物质来测试，通常许多制药 公司或化学品公司有“化合物库”）
Molecular modification involves the chemical alteration of a known and previously characterized organic compound for the purpose of enhancing its usefulness as a drug (分子修饰涉及化学改变已知和特性明了 的有机化合物以改善其作为药物的有效 性
• Molecular modification involves the chemical alteration of a known and previously characterized organic compound for the purpose of enhancing its usefulness as a drug. （分子修饰涉及化学改变已知和特性明了 的有机化合物以改善其作为药物的有效 性。）
Aims for molecular modification Enhancing its specificity for a particular body target site Increasing its potency; Improving its rate and extent of absorption; Modifying to advantage its time-course in the body; Reducing its toxicity Changing its physical or chemical properties to provide pharmaceutically desired features:
Aims for molecular modification • Enhancing its specificity for a particular body target site; • Increasing its potency; • Improving its rate and extent of absorption; • Modifying to advantage its time-course in the body; • Reducing its toxicity; • Changing its physical or chemical properties to provide pharmaceutically desired features;