四川大学华西医学中心：ß-内酰胺类抗生素（PPT讲稿）ß-lactam antibiotics

B-lactam antibiotics Liming Zhou Department of pharmacology

ß-lactam antibiotics Liming Zhou Department of pharmacology

Classification of drug The mechanism of antibacterial action Bacteria resistance

◼ Classification of drug ◼ The mechanism of antibacterial action ◼ Bacteria Resistance

B-lactam antibiotics in this chapter are classified into three sub-class I. The penicillins II. Cephalosporins II. Otherβ- actas

ß-lactam antibiotics in this chapter are classified into three sub-class. ◼ I. The penicillins ◼ II. Cephalosporins ◼ III. Other β-lactams

I. The penicillins A. natural penicillins: Penicillin g and penicillin V B Semisynthetic penicillins

I. The penicillins ◼ A. natural penicillins: Penicillin G and penicillin V ◼ B. Semisynthetic penicillins

II. Cephalosporins A First generation cephalosporins B. Second generation cephalosporins C. Third generation cephalosporins D.The fourth generation cephalosporins

II. Cephalosporins ◼ A. First generation cephalosporins ◼ B. Second generation cephalosporins ◼ C. Third generation cephalosporins ◼ D.The fourth generation cephalosporins

IL. Otherβ- actas ■A. Cephamycins ■B. Carbapenems ■C. Monobactams ■D. Oxacephem EB-lactamase inhibitor

III. Other β-lactams ◼ A. Cephamycins ◼ B. Carbapenems ◼ C. Monobactams ◼ D. Oxacephems ◼ E.β-lactamase inhibitor

The mechanism of antibacterial action The peptidoglycan is composed of glycan chains of N-acetyglucosamine and N-acetylmuramic acid The biosynthesis of peptidoglycan can be considered in three stages which the last one involves the completion of the cross-link. This is accomplished by a tranpeptidation reaction, which involves transpetidase. The B-lactam antibiotics combine with and inactivate the tranpeptidase

The mechanism of antibacterial action ◼ The peptidoglycan is composed of glycan chains of N-acetyglucosamine and N-acetylmuramic acid. ◼ The biosynthesis of peptidoglycan can be considered in three stages which the last one involves the completion of the cross-link. ◼ This is accomplished by a tranpeptidation reaction, which involves transpetidase. ◼ The ß-lactam antibiotics combine with and inactivate the tranpeptidase

Antimicrobials Effecting Cell Wall Synthesis+45 Vancomycin aig side chain or9 Dindin te th。amn 5Gnu口 NAM。eu| Interfere with the fornation Interfering with of Ihu peptide oid. ennis ooptidogycan synthesis between jacen1trnd段ae oootioogiyoon by inn biting panicillin-bindino protean optout youn toLmie T hta NA NAM BacItracIn Interferes with the transport af pupbuoel youn precursor gerot

The mechanism of antibacterial action NAc-Mur-NAc NAc-Mur-NAc L-Ala D-Glu D-Glu L-Lys--Gly-Gly L-Lys- Gly-Gly-Gly-Gly-Gly--D Gly-Gly--D- D-Al D-Alatranspeptida NAC-Mur-NA -NAc-Mur-NAc L-AI D-Glu D-Glu L-Lys--Gly-Gly- L-L Gly-Gly-Gly-Gly-Gly--D Gly-Gly--D-Al NAc: N-acetyglucosamine, Mur: N-acetylmuramic acid Ala: L-Alanine, D-Glu: D-Glutamine, L-Lys: L-Lysine, D-Ala: D-Alanine, Gly: Glycine The biosynthesis of cell wall peptidoglycan

The mechanism of antibacterial action

The mechanism of antibacterial action The tranpeptidase is inactivated by B-lactam antibiotics, they are the targets of B-lactam antibiotics and are named penicillin-binding protein(Pbps) a The PBPs vary in their affinities for different B-lactam antibiotics and several kinds of PBPs have confirmed

The mechanism of antibacterial action ◼ The tranpeptidase is inactivated by ß-lactam antibiotics, they are the targets of β-lactam antibiotics and are named penicillin-binding protein (PBPs). ◼ The PBPs vary in their affinities for different ß-lactam antibiotics and several kinds of PBPs have confirmed