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1.Substituents exhibit strong steric repulsion at the GABAA receptor ？what does it means？？ 2. Substitutions at C-6, C-8, and C-9 lower the activity？where is C-6, C-8, and C-9 ？can anyone help to lable out？

1.Substituents exhibit strong steric repulsion at the GABAA receptor ？what does it means？？ 2. Substitutions at C-6, C-8, and C-9 lower the activity？where is C-6, C-8, and C-9 ？can anyone help to lable out？

Biochemistry
Biochemistry
6th Edition
ISBN:9781305577206
Author:Reginald H. Garrett, Charles M. Grisham
Publisher:Reginald H. Garrett, Charles M. Grisham
Chapter27: Metabolic Integration And Organ Specialization
Section: Chapter Questions
Problem 12P
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1.Substituents exhibit strong steric repulsion at the GABAA receptor ？what does it means？？ 2. Substitutions at C-6, C-8, and C-9 lower the activity？where is C-6, C-8, and C-9 ？can anyone help to lable out？
General Structure-Function Association for Different Benzodiazepine Modifications. e.g. CH, Methyl substituent shows the highest increase in activity and bulky substituents such as a phenyl group lead to loss of activity Triazolo analogs tend to show a significantly higher activity e.g. CH, Decisive effect on the activity e.g. OH CH, Substituent leads to an e.g. NO, CI Br decrease in activity Activity increase with e.g. F CI electron withdrawing Halogen substituents in ortho- position lead to significantly enhanced activity substituent * Substitutions at C-6, C-8, and C-9 lower the activity Substituents exhibit steric strong repulsion at the GABA, receptor " Phenyl ring at C-5 position seems to be the best option with only pyridyl remarkable activity derivatives showing
Transcribed Image Text:General Structure-Function Association for Different Benzodiazepine Modifications. e.g. CH, Methyl substituent shows the highest increase in activity and bulky substituents such as a phenyl group lead to loss of activity Triazolo analogs tend to show a significantly higher activity e.g. CH, Decisive effect on the activity e.g. OH CH, Substituent leads to an e.g. NO, CI Br decrease in activity Activity increase with e.g. F CI electron withdrawing Halogen substituents in ortho- position lead to significantly enhanced activity substituent * Substitutions at C-6, C-8, and C-9 lower the activity Substituents exhibit steric strong repulsion at the GABA, receptor " Phenyl ring at C-5 position seems to be the best option with only pyridyl remarkable activity derivatives showing
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