In the design of H2 antagonist, the polar guanidine group was proposed to interact with the antagonist binding region by two hydrogen bonds. Compound A is designed based on modification of compound B and has higher antagonist activity compared to compound B. H2N NH NH2 NH HN Guanidine Guanidine HN What drug design strategy has been used here? O Rigidification O Simplification O Substituent variation O Chain Extension

Organic Chemistry
9th Edition
ISBN:9781305080485
Author:John E. McMurry
Publisher:John E. McMurry
Chapter29: The Organic Chemistry Of Metabolic Pathways
Section29.SE: Something Extra
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In the design of H2 antagonist, the polar guanidine group was proposed to interact with the
antagonist binding region by two hydrogen bonds. Compound A is designed based on modification
of compound B and has higher antagonist activity compared to compound B.
H2N
NH
NH2
NH
HN
Guanidine
Guanidine
HN
What drug design strategy has been used here?
O Rigidification
O Simplification
O Substituent variation
O Chain Extension
Transcribed Image Text:In the design of H2 antagonist, the polar guanidine group was proposed to interact with the antagonist binding region by two hydrogen bonds. Compound A is designed based on modification of compound B and has higher antagonist activity compared to compound B. H2N NH NH2 NH HN Guanidine Guanidine HN What drug design strategy has been used here? O Rigidification O Simplification O Substituent variation O Chain Extension
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