Sulphonamide Antibacterial Agent

Beschreibung

Lecture 1 Notes
Becky Harrison
Mindmap von Becky Harrison, aktualisiert more than 1 year ago
Becky Harrison
Erstellt von Becky Harrison vor mehr als 5 Jahre
55
0

Zusammenfassung der Ressource

Sulphonamide Antibacterial Agent
  1. Drug Names
    1. Code Name
      1. Chemical Name
        1. Generic/Non-Proprietary Name
          1. Trade Name
          2. Gram Test
            1. Heteroaromatic purple stain mixed with bacteria
              1. Sticks to outer membrane
                1. Decolourisation with organic solvent
                  1. Gram Positive: Purple
                    1. Gram Negative: Red
              2. Mode of Action
                1. Prontosil
                  1. Azodye
                    1. Prodrug; reduced to sulphanilamide.
                    2. Prodrug
                      1. Compound metabolised in vivo to active form of drug.
                    3. SAR
                      1. Para-Amino essential (primary!)
                        1. Aromatic Ring and Sulphonamide essential
                          1. Sulphonamide primary or secondary only
                            1. R' only modifiable.
                            2. Improved Sulpha Drugs
                              1. Sulphanilamide
                                1. Poorly water soluble
                                  1. Toxic via crystallisation in kidneys
                                  2. Second Generation
                                    1. Improved solubility via increased polarity
                                      1. pKa close to that of most of the body.
                                    2. Site of Action
                                      1. Dihydropterase Synthase
                                        1. Involved in folic acid biosynthesis
                                        2. Folic Acid
                                          1. Essential for 1-Carbon unit transport of all oxidation states.
                                            1. Required for DNA synthesis.
                                          2. Competitive Inhibitors
                                            1. Sulphanilamide competes with PABA for dihydropterate synthase.
                                              1. Bacterial DHFR different in structure than human's
                                                1. Trimethoprim - competitive inhibitor of DHFR
                                              2. Septrin
                                                1. Synergistic
                                                  1. Trimethoprim and Sulphamethoxazole
                                                    1. Example of: Anti-metabolite and Bacteriostatic Drug

                                                    Medienanhänge

                                                    Zusammenfassung anzeigen Zusammenfassung ausblenden

                                                    ähnlicher Inhalt

                                                    Using GoConqr to study science
                                                    Sarah Egan
                                                    Electrolysis
                                                    lisawinkler10
                                                    Elements, Compounds and Mixtures
                                                    silviaod119
                                                    Chemistry General Quiz - 2
                                                    lauren_johncock
                                                    Chemistry Quiz General -3
                                                    lauren_johncock
                                                    Chemistry Module C2: Material Choices
                                                    James McConnell
                                                    AS Chemistry - Enthalpy Changes
                                                    Sarah H-V
                                                    The Periodic Table
                                                    asramanathan
                                                    Acids and Bases
                                                    Sarah Egan
                                                    Ionic Bondic Flashcards.
                                                    anjumn10
                                                    Acids and Bases
                                                    silviaod119