BSN 315 STRUCTURE ACTIVITY RELATIONSHIPS (SAR) – Questions With Expert Solutions

BSN 315 STRUCTURE ACTIVITY RELATIONSHIPS
(SAR) – Questions With Expert Solutions

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Terms in this set (38)



STRUCTURE ACTIVITY RELATIONSHIPS The Pharmacophore
(SAR) • Discerning what part of a molecule is responsible for
activity (the pharmacophore) both in vitro and in vivo is
at the heart of drug development.
• In vitro activity may give clues as to whether a drug is
active against e.g. an enzyme or a receptor
• In vivo activity gives additional information concerning
the transport of the drug to the site of action and its
metabolism


Example: Penicillin - Beta-lactam ring

, SAR: MORPHINE Separating the Analgetic and Addictive Properties of
Morphine
R = R' = H / Morphine
R = Me, R' = H / Codeine
R = R' = Acetyl / Heroin
Analgetic and addictive


Levorphanol (3 x potency of morphine):
Analgetic and addictive


R = Me / Benzomorphan (Analgetic and less addictive)
R = -I> Cyclazocine (Analgetic and non-addictive)


Demerol = 10-12% activity of morphine
Darvon = 50 - 66% activity of morphine
Methadone = Similar activity to morphine




STRUCTURE ACTIVITY RELATIONSHIP • Systematically modify the structure of the
pharmacophore
• Testing the activity of the compound each time
• Used to optimise drug molecules
• We will look at several different methods