Section 3 Macrolides Lincomycins vancomycins Yun-Bi Lu, PhD 卢韵碧 Dept of Pharmacology, School of Medicine, Zhejiang University yunbi@zju.edu.cn
Macrolides, Lincomycins &Vancomycins Section 3 Yun-Bi Lu, PhD 卢韵碧 Dept. of Pharmacology, School of Medicine, Zhejiang University yunbi@zju.edu.cn
Part A Macrolides Erythromycin(红零素 · Clarithromycin(克拉零亲) Azithromycin(阿奇霉素) Telithromycin(泰利零亲
• Erythromycin (红霉素) • Clarithromycin (克拉霉素) • Azithromycin (阿奇霉素) • Telithromycin(泰利霉素) Part A Macrolides
CH H3C OCH. H3C、CH3 --CH CH H3C 00—cH CH H2C、OH OH H2C、CH C OCH3 OH CH3 CH CH OH H3C 0o—cH O CLARITHROMYCIN CH 14 member rings 2 CH CH O H3CAN CH3 OCH CH CH H3C.HO OH -CHa H3C CH OH HO CH H3C CH ERYTHROMYCIN CH2 CH OCH 14 member rings CH CH CH AZITHROMYCIN 15 member rings
14 member rings 15 member rings 14 member rings
General properties of Macrolides 1. Antimicrobial spectrum Gt organisms G- cocci: Streptococcus pyogenes and pneumoniae Mycoplasma pneumoniae(肺支原体)and Legionnella(军团菌)etc 2. Antimicrobial activity: bactericidal and bacteriostatic depending on the concentration · more active at alkaline
1. Antimicrobial spectrum： • G+ organisms • G- cocci: Streptococcus pyogenes and pneumoniae • Mycoplasma pneumoniae(肺支原体) and Legionnella (军团菌)etc. 2. Antimicrobial activity: • bactericidal and bacteriostatic, depending on the concentration. • more active at alkaline General properties of Macrolides
3. Mechanism of action: 50S subun peptide macrolide bond 50s subunit A C cC U U A CGC G XXXXXXAUGCGCGGAUCC/ XXXXXXAUGCGCGGAUCCCCCACCUGA codon 1 codon 2 codon 3 codon 4 codon 5 codon 6 codon 7 (SER) (f-METL(ARG) (GLY) (SER) (PRO) (THR) (Stop) 30s start) 30s subunit macrolide subunit mRN
3. Mechanism of action: subunit macrolide