【医学精品课件之抗生素】Antibiotics.ppt

Antibiotics;Classification (According their structures)：;Classification (According to their mechanism of actions;;;These all share a common β-lactam ring.? The ring is very strained and the bond between the carbonyl and the nitrogen in the β-lactam ring is very labile and hence makes the molecule reactive. The R-group substitute of the penicillin nucleus can be changed to give the molecule different antibacterial properties. The two naturally occurring penicillins from Penicillium notatum are Penicillin G,? [Benzyl penicillin, R = C6H6] and Penicillin V, [Phenoxymethyl penicillin, R = CH2O(C6H6)];The β-lactam structure is derived from two covalently bonded amino acid residues; cysteine and valine.? This forms via a tripeptide intermediate where the third amino acid is replaced by the variable R-group. ;Mechanism of Action;;Penicllin-binding poteins,PBPs;Penicliins Nature Penicillin (Fermentation-Derived Penicillins);Fleming found that it was effective against many Gram positive bacteria in laboratory conditions, and he even used locally applied, crude preparations of this substance, from culture filtrates, to control eye infections. However, he could not purify this compound because of its instability, and it was not until the period of the Second World War (1939-1945) that two other British scientists, Florey and Chain, working in the USA, managed to produce the antibiotic on an industrial scale for widespread use. In recognition for his contribution, Alexander Fleming was knighted in 1944. With Chain and Florey he was awarded the Nobel Prize in 1945. One sometimes finds what one is not looking for.; ;Because of its cheapness, efficacy, and remarkable lack of toxicity (except for acutely allergic patients). Peniciline G remains a remarkably useful agent for treatment of disease caused by susceptible microorganisms. It is the drug of choice for more infections than any other antibiotics. “ Fist is best” The disadvantages of Fermentation-Derived