CHEM 3LB3 Lecture Notes - Lecture 9: Paclitaxel, Angina Pectoris, Cubic Crystal System

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Lecture 9 from compound to drug & nitrogen in car tires. The drug discovery process: time, money & risk. Human clinical trials (2-5 years: file nda. Total: 12 to 25 years, m. Medicinal chemistry: identify and prepare molecules for use as medicines: salicylic acid. Good for wart removal: acetylsalicylic acid. Potent analgesic (similar to morphine: manzamine. Nature has had millions of years to generate a vast, diverse array of compounds (some of which are biologically active) Problems: where do you look, available options, time consuming, specificity, new chemical entities (nce) Combinational chemistry and high throughput screening: generates diverse libraries of synthetic materials via a combinatorial approach. Scaffold has 3 vectors can create: 3 amines, 3 carboxylic acids, 3 alkyl halides. Take your optimized lead and make it into a pharmaceutical. Lots of the drug is lost in liver due to oxidation. Drug needs to be soluble in the body (cannot be insoluble)