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
9th Edition
ISBN:9781319114671
Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Chapter1: Biochemistry: An Evolving Science
Section: Chapter Questions
Problem 1P
Related questions
Question
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?

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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