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Antimicrobial Drugs Chapter 20
20

Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

Jan 18, 2018

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Linda Edwards

B. General types of chemotherapeutics u 1. Structural analogues –competitive inhibitors –growth factors
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Page 1: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

Antimicrobial Drugs

Chapter 20

Page 2: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

I. Chemotherapeutics A. History

– Paul Ehrlich

– Structural analogues» 1935: Domagk

Page 3: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

B. General types of chemotherapeutics

1. Structural analogues– competitive inhibitors

– growth factors

Page 4: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

2. Antibiotics Chemicals secreted by organisms to kill off

other organisms Primarily isolated from

Page 5: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

C. Specificity of various antibiotics

Page 6: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.
Page 7: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

III. Sites of interaction Cell wall

Cell membrane

Essential metabolite biosynthesis

Protein synthesis

DNA replication and transcription

Page 8: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

IV. Cell wall inhibitors A. Penicillin family

– Benzylpenicillin

Page 9: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

B. Resistance to penicillin

Page 10: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

C. Penicillin family:modifications of side chain

Methicillin

Ampicillin

Carbenicillin

Oxacillin

Page 11: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

D. Other cell wall growth inhibitors

Cephalosporins

Bacitracin

Vancomycin

Page 12: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

V. Inhibitors of protein synthesis Aminoglycosides

Page 13: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

Aminoglycosides, cont Tetracyclines

Macrolides

Page 14: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

VI. Inhibitors of nucleic acid biosynthesis

Rifamycin

Quinolones

Page 15: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

VII. Interaction with plasma membrane

Page 16: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

VIII. Viral control Chemical inhibition

Interferon

Page 17: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

IX. Fungal control Unique membrane components

Folate biosynthesis

Page 18: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

Others block– chitin biosynthesis

– nucleic acid biosynthesis

– microtubule assembly

Page 19: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

X. Drug resistance Prevent entry

Alter binding site

Inactivate drug

Page 20: Antimicrobial Drugs Chapter 20. I. Chemotherapeutics u A. History Paul Ehrlich Structural analogues 1935: Domagk.

XI. And in the future. . .