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 strong steric repulsion at the GABA, receptor " Phenyl ring at C-5 position seems to be the best option with only pyridyl remarkable activity derivatives showing

Chemistry
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Author:Steven S. Zumdahl, Susan A. Zumdahl, Donald J. DeCoste
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Chapter1: Chemical Foundations
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1.Activity electron substituent increase with withdrawing?what does it means?does it means when NO2 ,CI ,Br is attached on that ring will increase the activity or without NO2 ,CI ,Br is attached will be better?? Please type!No hand writing!
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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