PHAR2210 Lecture Notes - Lecture 20: Semisynthesis, Glycan, Cephalosporin

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Bacterial cell wall peptidoglycan as a drug target: Lattice of glycan chains (2 alternating aminosugars: nacetyl-muramic acid. Peptidoglycan can comprise 10-15% dry weight of cell (maintain rigidity: gram-positive bacteria: 50-100 molecules thick, gram-negative bacteria: 1 or 2 molecules thick. 1928: fleming (right), st. mary"s hospital, penicillium mould inhibited staphylococcus growth. Florey (oxford): extracted active substance and tested as drug in bacteria infected animals and humans: after the us military perfected large-scale production in ww2, penicillin ushered in golden. Led to dozens of penicillins (widely used drugs) + semi- synthetic penicillins (differ in side chain substituents) Several categories, e. g. narrow, moderate & broad spectrum. Basic pharmacology of the penicillins: useful in bacterial infections of lungs, oral cavity, soft tissues, skin, joints, gi tract, etc, good distribution in body (not cns) Typically undergo little or no metabolism in liver: excretion unchanged by kidneys is typical, mostly well tolerated, although allergies can occur.

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