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4- Salicylamides are inhibitors for an enzyme called scytalone dehydratase. SAR shows that there are three important hydrogen bonding interactions. Explain whether you think quinazolines could act as a bioisostere for salicylamides. Salicylamides HBA OH Ph HBA H HBD N 5- Structure IX (X = NH) is an inhibitor of a metalloenzyme called thermolysin and forms interactions as shown. Explain why the analogue (X = O) has reduced binding affinity by a factor of 1000 and why the analogue (X = SH) has roughly the same binding affinity. NHR Quinazolines Ala-113 styl H Structure IX n²+ R

4- Salicylamides are inhibitors for an enzyme called scytalone dehydratase. SAR shows that there are three important hydrogen bonding interactions. Explain whether you think quinazolines could act as a bioisostere for salicylamides. Salicylamides HBA OH Ph HBA H HBD N 5- Structure IX (X = NH) is an inhibitor of a metalloenzyme called thermolysin and forms interactions as shown. Explain why the analogue (X = O) has reduced binding affinity by a factor of 1000 and why the analogue (X = SH) has roughly the same binding affinity. NHR Quinazolines Ala-113 styl H Structure IX n²+ R

Biochemistry
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
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4- Salicylamides are inhibitors for an enzyme called scytalone dehydratase. SAR shows that there are three important hydrogen bonding interactions. Explain whether you think quinazolines could act as a bioisostere for salicylamides. HBA OH O 00 N NHR Quinazolines Salicylamides Ph HBA 5- Structure IX (X = NH) is an inhibitor of a metalloenzyme called thermolysin and forms interactions as shown. Explain why the analogue (X = O) has reduced binding affinity by a factor of 1000 and why the analogue (X = SH) has roughly the same binding affinity. Structure IX H HBD Ala-113 R
Transcribed Image Text:4- Salicylamides are inhibitors for an enzyme called scytalone dehydratase. SAR shows that there are three important hydrogen bonding interactions. Explain whether you think quinazolines could act as a bioisostere for salicylamides. HBA OH O 00 N NHR Quinazolines Salicylamides Ph HBA 5- Structure IX (X = NH) is an inhibitor of a metalloenzyme called thermolysin and forms interactions as shown. Explain why the analogue (X = O) has reduced binding affinity by a factor of 1000 and why the analogue (X = SH) has roughly the same binding affinity. Structure IX H HBD Ala-113 R
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