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Solutions For An Introduction to Medicinal Chemistry Chapter 13 Problem 12Q

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Salicyclamide is an ortho-hydroxibenzamide or an amide of salicyl. The drug has antipyretic and analgesic properties. It is a non-prescription drug with medical uses that are similar to that of aspirin. It is used in combination with caffeine and aspirin for pain remedies that are over-the-counter.

Bioisostere is a term used in designing of drugs to signify a group, which can be utilized for replacement of another group. It includes the classical as well as non-classical isosteres involved in drug design.

They are usually to replace functional groups required for specific target binding. They display compound and garget specificity. They, however, do not provide guarantee for activity retention for each drug at each target.

Salicyclamide as well as quinazolines are regarded as potent inhibitors for scytalone dehydratase. They both contain two atoms as acceptors that bind at the specific site through hydrogen bonds. The water molecules that are conserved mediate the bond formation between the ligand and the functional groups.

Quinazolines would act as better inhibitors for scytalone dehydratase because of the replacement of hydrogen bonding groups with a cyano substituent shows affinity enhancement. It is because the nitrogen molecule mimics the water molecule that results in greater affinity.

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Solutions For Problems in Chapter 13