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
6th Edition
ISBN:9781305577206
Author:Reginald H. Garrett, Charles M. Grisham
Publisher:Reginald H. Garrett, Charles M. Grisham
Chapter24: Lipid Biosynthesis
Section: Chapter Questions
Problem 20P
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Question
![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](/v2/_next/image?url=https%3A%2F%2Fcontent.bartleby.com%2Fqna-images%2Fquestion%2F166181e4-f3b5-4c4d-b0c6-fbd3dd4c2b23%2Fb39fa52e-7502-4603-a987-3719514ddbf2%2Fbsaphkm_processed.jpeg&w=3840&q=75)
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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