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Shu-yi Sophie Chen

Polytechnic University, Hong Kong

Title: The structure activity relationship of antidepressants and the specificity in drug therapy

Biography

Biography: Shu-yi Sophie Chen

Abstract

Antidepressants are prescribed commonly in depression therapy in the pharmaceutical methods; however, the long term administration time which is approximately 10 to 20 days and the unpleasant side eff ects are still accompanied during the medication therapy. Consequently, the full profi le of the medicinal chemistry of the antidepressants is discussed for an ideal structure in drug affi  nity. Antidepressants can be divided into diff erent types that depend on diff erent neurotransmitters as a target to serve as reuptake inhibitors. Furthermore, antidepressants can be categorized into (SSRIs) selective serotonin reuptake inhibitors and (SNRIs) selective norepinephrine selective reuptake inhibitors. Th e structure activity relationship of antidepressants is the goal in this project to explore the full profi le of specifi c structure in binding affi  nity and specifi city. A better view of the structure in antidepressants is benefi cial to establish a highly potent and precise antidepressant design. Halogens are found common in the antidepressants compound for the purpose of drug affi  nity. Especially, the fl uorine atom will serve as hydrogen bond acceptors that contribute to a high affi  nity in protein-ligand interaction, particularly in association with O-H or N-H group in the binding protein. Both the fl uoxetine and paroxetine contains fl uorine as the substituted group. However, the position matters when it comes to the affi  nity that the substituted group in fl uoxetine occupy only 4’-position while paroxetine occupies both 4’- and 3’-position on the aryloxy ring that proposes the spatial confi guration of the substitution group is signifi cant. Furthermore, the fl uoxetine contains trifl uoromethyl group on the phenolic rings in the Para-position exhibit 6-fold potency in SSRI activity compared to its parent non-fl uorinated structure.  In summary, a more clear direction in the development of antidepressants can be suggested to be related to both the types and positions of substituents on the aromatic rings.  Mostly, these antidepressants are not only treated to depression disorder but also can be used in other health condition such as NRIs in chronic pains and ADHD. Hence, an outcome of improved effi  cacy in terms of its specifi city and potency of antidepressants can benefi t people to overcome the healthy condition and provide a more profi le in the drug design