The process of relating the chemical structure to biological action is called Structure - Activity Relationship (SAR).True/False

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True

B

False

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N-arachidonyl-glycine (see structure below) was discovered as a glycine transport inhibitor that provided analgesia in chronic pain. However, the compound is not suitable for development as a drug because of low potency, metabolic instability and poor selectivity. To overcome these limitations, a series of bioactive lipids have been developed, including oleoyl-D-lysine (structure below). The following questions relate to the principles used to develop more potent, metabolically stable, and more selective compounds. Arachidonyl-glycine Oleoyl-D-lysine Oleoyl-D-lysine was developed from N-arachidonyl-glycine. What limitations does oleoyl-D-lysine overcome compared to N-arachidonyl-glycine? From the 4 statements, choose the best combination of responses to answer the question. The D-lysine amino acid limits metabolism compared to the glycine head group The oleoyl tail is less susceptible to oxygenation than the arachidonyl tail The more flexible oleoyl tail is better able to fit into the binding pocket. The positive charge on the lysine allows formation of π-cation bonds to improve potency

The process of relating the chemical structure to biological action is called Structure - Activity Relationship (SAR).

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