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A New Drug for Parkinson's Disease

It is known that consuming only one cup of coffee per day due to the antagonism of the A2A receptor by caffeine (Figure 1) lowers the incidence of Parkinson’s disease significantly.[4] Another purine derivative, Istradefylline (Figure 1), as an A2A receptor antagonist is thought to be able to treat the symptoms of Parkinson’s disease through activating the γ-aminobutyric acid (GABA) pathway of the subthalamic nucleus. Unfortunately, it has some disadvantages, such as poor solubility in water, and low photostability. Due to its double bond (marked red in Figure 1), it easily converts to Z-isomer when exposed to UV radiation in a solution state.[5] To be considered an efficient lead, these issues need to be addressed. For this purpose, vicinal fluorination will be used to improve and solve these problems. Difluorination is proved to greatly influence photostability, selectivity, and solubility.[6]
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A New Drug for Parkinson's Disease
It is known that consuming only one cup of coffee per day lowers the incidence of Parkinson’s disease significantly, due to the antagonism of the A2A receptor by caffeine (Figure 1) lowers the incidence of Parkinson’s disease significantly.
[4] Another purine derivative, Istradefylline (Figure 1), as an A2A receptor antagonist is thought to be able to treat the symptoms of Parkinson’s disease through activating the γ-aminobutyric acid (GABA) pathway of the subthalamic nucleus.
Unfortunately, it has some disadvantages, such as poor solubility in water, and low photostability.
Due to its double bond (marked red in Figure 1), it easily converts to Z-isomer when exposed to UV radiation in a solution state.
[5] To be considered an efficient lead, these issues need to be addressed.
For this purpose, vicinal fluorination will be used to improve and solve these problems.
Difluorination is proved to greatly influence photostability, selectivity, and solubility.
[6]

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