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Lecture 7

CHEM669 Lecture 7: 405-669 January Summary Points

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Fredrick West

CHEM 405/669, Winter 2017 Chemistry 405/669–2017 Pharmaceutical Chemistry Important Points from January Lectures Below are some of the key issues that were covered in lectures during the month of January. Students are encouraged to review the PDF files of the lecture slides, especially the “points to ponder.” Lecture 1 (January 10). This was an introductory lecture that did not cover a lot of core content. However, please note the following points: •The concept of drug development pipeline was introduced, emphasizing the lengthy process and the large amount of compound attrition as a project moves from the early medicinal chemistry stages to late development (clinical trials, etc.). •Top-selling drugs of 2014 were discussed, and the distinction between biologics and small molecules was introduced. Note that this class will mostly deal with small molecule drugs. •The Gilead HCV drug sofasbuvir (Sovaldi) was presented as an example of a modern blockbuster drug, including its origins, mode of action (including the pro-drug side-chain), and synthetic chemistry. Lecture 2 (January 12). This lecture introduces a number of terms and concepts that will be encountered again and again throughout the course. Students are encouraged to review all of them, particularly these: •Early stage discovery and development: G-protein-coupled receptors (GPCRs), high-throughput screening (HTS), hit, hit-to-lead, lead, antagonist50IC , Ki, Kd, pharmacophore. •Drug development: lead optimization, Lipinski’s rules, logP, pharmacodynamics (PD), pharmacokinetics (PK), ADME, bioavailability, CYP inhibition, hERG. •Dosing and formulation: active pharmaceutical ingredient (API), maximum tolerated dose (MTD), therapeutic index. Lecture 3 (January 17). This was the first of three lectures on common therapeutic targets and molecular scaffolds. Notable take-home messages include: •Concept of drug selectivity (COX-1 vs COX-2). •Opiates and their synthetic analogues (including: codeine as a prodrug form of morphine). •Common classes of antibiotics: sulfa, b-lactams, aminoglycosides, tetracycline, macrolides (e.g. erythromycin), fluoroquinolones, oxazolidinones. •Cancer chemotherapeutics: antimetabolites (e.g. methotrexate), DNA-modifying agents, tubulin- binding drugs. •Antivirals: HIV—reverse transcriptase inhibitors, protease inhibitors; HCV—polymerase inhibitors and NS5A inhibitors. Lecture 4 (January 19). This was a continuation of the targets and scaffolds story. Notable take- home messages include: CHEM 405/669, Winter 201 7 •Cardiovascular drugs (hypertension)—b-blockers, ACE inhibitors (inspired by a snake venom peptide), calcium channel block
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