The development of new pharmaceuticals fundamentally relies on the ability to design and synthesize new compounds. Synthesis is an enabling discipline for medicinal chemistry - without it, the development of new drugs cannot progress from design to implementation, and ultimately to a cure. This unit will tackle important factors in drug design, and will highlight the current arsenal of methods used in the discovery of new drugs, including rational drug design, high throughput screening and combinatorial chemistry. We will develop a logical approach to planning a synthesis of a particular target structure. The synthesis and chemistry of heterocycles, which comprise some 40% of all known organic compounds and are particularly common in pharmaceuticals, will be outlined. Examples will include important ring systems present in biological systems, such as pyrimidines and purines (DNA and RNA), imidazole and thiazole (amino acids and vitamins) and porphyrins (natural colouring substances and oxygen carrying component of blood). Throughout the course, the utility of synthesis in medicinal chemistry will be illustrated with case studies such as anti-influenza (Relenza), anaesthetic (benzocaine), anti-inflammatory (Vioxx), antihypertensive (pinacidil) and cholesterol-lowering (Lovastatin) drugs.
Two 1-hour lectures per week and two 4-hour practicals per week for half of semester.
Assignment, prac reports and oral, final examination (100%)
(CHEM2401 or CHEM2911 or CHEM2915) and (CHEM2402 or CHEM2912 or CHEM2916)Prohibitions