Typical Types of Drug Modification Flashcards

1
Q

Homologation

A

increasing compounds by a constant unit;

  • hydrophobic pocket increases binding with increasing length; too large and does not fit into hydrophobic pocket
  • increasing chain length increases lipophilicity and ability to cross membranes
  • branched chains are less lipophilic than straight ones
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2
Q

Chain Brancing

A

pharmacological changes; lowers potency if lipophilicity is important or could change activity; could interfere with receptor binding

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3
Q

Bioisosterism

A

substituents or groups with chemical or physical similarities that produce similar biological properties; can attenuate toxicity, modify activity of lead, or alter pharmacokinetics of lead

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4
Q

classic bioisosteres

A

peripheral layer of electrons are considered identical

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5
Q

non-classic bioisosteres

A

do not have the same number of atoms; do not fit steric/electronic rules of classic isosteres

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