chapter 1

• Chemotheraphy

  • involve drugs that target cancerous cells or tissues
  • may involve antimicrobial drugs that target infectious microorganisms
• How do AM drugs work?

  • destroying or interfering with microbial structures and enzymes
  • kills it or inhibiting their growth
• Remains of people from Nubia

  • dating from 350-550 AD have shown residue of tetracycline suggesting the purposeful fermentation of tetracycline producing streptomyces during beer making process
  • this beer was used to treat gum disease and wounds
• Indian and chinese herbalists

  • recognized antimicrobial properties of plants
• Healers of many cultures

  • understood the antimicrobial properties of fungi and their use of moldy bread or mold containing products to treat wounds is well documented
• about 80% of the world's population still relies on plant derived medicine
• • in the early 1900s, german physician and scientist paul ehrlich discovered compounds capable of killing infectious microbes without harming the patient
  • in 1909 after screening more than 600 arsenic contaning compounds, ehrlich's assistant Sahachiro hata found magic bullet
  • compound 606 targets bacterium treponema pallidum against syphilis
  • compound 606 was marketed under the name salvarsan
• Sulfanilamide was the first synthetic antimicrobial drug
• German scientist Josef Klarer, Fritz Mietzsch and Gerard Domagk discovered the antibacterial activity of a synthetic dye, Protonsil for streptococcal and staphylococcal infections
• Domagk was awarded for his work in Prontosil and sulfanilamide (Nobel prize in medicine in 1939)
• Synthetic antimicrobials

  • Quinolines
  • Oxazolidinones
  • Sulfa drugs
• Protonsil was used to treat streptococcal and staphylococcal infections on mice
• Sulfanilamide served as the foundation for chemical development of the family of sulfa drugs
• Gerard Domagk's daughter was the first human recipient of the drug from a streptococcal infection due to poke of a needle
• Gerard Domagk was awarded with Nobel Prize in Medicine


  1939
• • in 1928, fleming returned from holiday and examined some old plates of staphylococci in his lab, he observed that contaminating mold growth, penicillium notatum inhibited staphylocccal growth on one plate
  • credited with the discovery of penicillin-- first natural antibiotic
  • penicillin is against streptococci, meningcocci and corynebacterium diphtheriae
• isolation and mass production of penicillin were accomplished by howard florey and ernst chain of oxford university who purified penicillin and reported its success as antimicrobial agent against streptococcal infection in 1940
• fleming, florey, and chain were awarded with the nobel prize in physiology and medicine in 1945
• in the early 1940s, scientist dorothy hodgkin who studied crystallography at oxford, used x ray to analyze the structure of nat prods. in 1946, she determined the structure of penicillin which she was awarded the nobel prize in chemistry in 1964
• in the 1940s, selman waksman, a soil microbiologist at rutgers university, led a team discovered several antimicrobials like actinomycin, streptomycin and neomycin . it stemmed from her study of fungi and actinobacteria including soil bacteria of streptomyces. he earned nobe prize in physiology and medicine in 1952.
• the actinomycetes are the source of more than half of all natural antibiotics and serve as an excellent reservoir for more discovery
• semisynthetic antimicrobial - is a chemically modified derivative of a natural antibiotic