Structure 2-4 are analogues of lead compound (structure 1), stru and 3 had similar activity to the lead compound whereas struct showed a marked increase in activity. Which of the following ex best fit the facts? Drug N 2 Drug 3 Drug 11 N. Drug

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Chapter1: Chemical Foundations
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Structure 2-4 are analogues of lead compound (structure 1), stru
and 3 had similar activity to the lead compound whereas struct
showed a marked increase in activity. Which of the following ex
best fit the facts?
Drug
1
N
2
Drug
site
3
Drug
N.
Drug
O a. Introducing nitrogen removes aromatic hydrogen, the aro
hydrogen removed may have been bad for activity for ste
reasons.
O b. Introducing nitrogen means that additional hydrogen bonc
interactions is possible with an extra binding region in the bi
O c. Introducing nitrogen increases basicity and so increased bas
good for activity
O d. Introducing nitrogen increases the polarity and solubility of th
analogues, and so increased polarity is good for activity
Transcribed Image Text:Structure 2-4 are analogues of lead compound (structure 1), stru and 3 had similar activity to the lead compound whereas struct showed a marked increase in activity. Which of the following ex best fit the facts? Drug 1 N 2 Drug site 3 Drug N. Drug O a. Introducing nitrogen removes aromatic hydrogen, the aro hydrogen removed may have been bad for activity for ste reasons. O b. Introducing nitrogen means that additional hydrogen bonc interactions is possible with an extra binding region in the bi O c. Introducing nitrogen increases basicity and so increased bas good for activity O d. Introducing nitrogen increases the polarity and solubility of th analogues, and so increased polarity is good for activity
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