NHIBITORS OF CELL B-LACTAMASE WALL SYNTHESIS INHIBITORS Clavulanic acid B-LACTAM OTHER Tazobactam ANTIBIOTICS ANTIBIOTICS Vancomycin /Teichoplanin Bacitracin PENICILLINS CEPHALOSPORINS CARBAPENEMS MONOBACTAMS Penicillin G Imipenem/cilastatin' Aztreonam Penicillin V Meropenem Methicillin Nafcillin Oxacillin 1st GENERATION 2nd GENERATON 3rd GENERATION 4th GENERATION Cloxacillin Dicloxacillin Cefazolin Cefaclor Cefixime Cefepime Ampicillin Cefadroxil Cefamandole Cefoperazone Amoxicillin Cephalexin Cefonicid Cefotaxime Carbenicillin Cephalothin Ceforanide Ceftazidime Ticarcillin Cephapirin Cefotetan Ceftizoxime Piperacillin Cephradine Cefoxitin Ceftriaxone Mezlocillin Cefuroxime Moxalactam Azlocillin Cefprozil Cefdinir Cefpodoxime
acyl side chain β- actam ring thiazolidine ring H HH CHa R,+C-N-C—C 653CH penIcillIns 7 H amIdase C-N COOH Source: Penicilliumspl,青霉菌 β- actamase acyl side chain B-lactam ring dihydrothiazine ring O H HH R,+C-N-C---C H amidase CB-N1 3C-H cephalosporins R Source: Cephalosporium spp COOH (now called Acremoniumspp β- actamase 枝顶孢菌)
amidase b-lactamase b-lactam ring amidase b-lactamase b-lactam ring Source:Penicilliumspp, 青霉菌 Source:Cephalosporium spp (now called Acremonium spp. 枝顶孢菌)
Sir Alexander Fleming The nobel prize in Physiology or medicine 1945 Discoverer of penicillin Co-recipients: Florey and chain (They made it possible to produce large quantities)
Sir Alexander Fleming The Nobel prize in Physiology or Medicine 1945 Discoverer of Penicillin Co-recipients: Florey and Chain (They made it possible to produce large quantities)
Penicillins Action mechanisms Inhibit the activity of peptidoglycan transpeptidase(PBP) Increase the activity of cell wall autolytic enzyme C-terminal TP Linke z>-0山 N-ter inal Peptide ugar Bacterial cell m mmmmmm membrane WALL FACTORY The GT domain of PBP pulls peptidyl lipid sugars from the membrane and polymerizes them, thereby creating a peptidyl sugar backbone. this backbone structure is then passed to the tP do- main, which cross-links the peptides to construct peptidoglycan compo- nents of bacterial cell wall
Penicillins Action mechanisms • Inhibit the activity of peptidoglycan transpeptidase (PBP) • Increase the activity of cell wall autolytic enzyme C-terminal N-terminal
Alanine (o b Squamate Lysine PEntaglycine Chan NAM NAG PenicillIn