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Prof.Dr. Meral Tunçbilek

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Academic year: 2021

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Prof.Dr. Meral Tunçbilek

ISOMERISM IN DRUG

(2)

Stereoselective activity

Stereoselective activity is common in drugs and other bioactive molecules.

Understanding the differences between enantiomeric activities is important in designing more active and more selective molecules.

The activity difference of the enantiomers results from the difference in the formation of the drug-receptor complex.

(3)

• The most important factor in the different activities of optical isomers is the stereoselectivity of the specific receptor.

(4)

(+)-(2S,3R,5S)-Muscarine

About twice the potency of acetylcholine and about 700 times more potent than its enantiomer (-)-(2R,3S,5R)-muscarine

(5)
(6)

• The majority of H1-receptor antagonists are chiral

molecules and their activities are stereoselective.

S-(+)-Chlorpheniramine (S-(+)-dextrochlorpheniramine)

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