Creation of bioactive organic compounds, including chemical modifications, will be discussed. This lecture is held in English.
生体物質の化学修飾を含めて,生理機能を有する有機化合物の創製について解説する。講義は英語で行われる。
Creation of bioactive organic compounds, including chemical modifications, will be discussed. This lecture is held in English.
Organic synthesis is one of the most powerful tools to create drugs for diseases, such as cancer, diabetes, flu, and etc. Thus the knowledge and skills of organic synthesis are prerequisite for theresearch in pharmaceutical industry. The aim of this class is to have you understand the logics and mechanisms underlying the design and synthesis of bioactive molecules. To make the class less bored, each lecture will deal with the synthesis of a few compounds, with which the basic principles behind the constituent reactions will be uncovered. Therefore, you do not have to attend all of the classes. The first half of this class will be based on the text book, “Top Drugs: Top Synthetic Routes”(John Saunders, Oxford University Press: Oxford, 2000). Our own research results are discussed in the latter half.
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Inhibitors of angiotensin converting enzyme
Blockade of angiotensin-II receptors
Calcium channel blockers
Antagonists of histamine receptors
Proton pump inhibitors
Modulation of central serotonin
Ligands for benzodiazepine receptor
Blockers of the H1 recptor
Inhibitors of HIV reverse transcriptase
Anti-bacterial DNA gyrase inhibitors
Glycosidase inhibitors against diabetes
Carbohydrate-based future drugs
Principles of mimics and mimetics
Dynamic molecules for future drugs
Peptide synthesis (optional)
配布資料等
出席,演習,レポートを総合して評価する。
Attendance and report