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Novel Multifunctional Dopamine D

Novel Multifunctional Dopamine D

Dan Luo, Horrick Sharma, Deepthi Yedlapudi, Tamara Antonio, Maarten E A Reith, Aloke K Dutta

Bioorg Med Chem. 2016 Nov 1;24(21):5088-5102.

PMID: 27591013

Abstract:

Our ongoing drug development endeavor to design compounds for symptomatic and neuroprotective treatment of Parkinson's disease (PD) led us to carry out a structure activity relationship study based on dopamine agonists pramipexole and 5-OHDPAT. Our goal was to incorporate structural elements in these agonists in a way to preserve their agonist activity while producing inhibitory activity against aggregation of α-synuclein protein. In our design we appended various catechol and related phenol derivatives to the parent agonists via different linker lengths. Structural optimization led to development of several potent agonists among which (-)-8a, (-)-14 and (-)-20 exhibited potent neuroprotective properties in a cellular PD model involving neurotoxin 6-OHDA. The lead compounds (-)-8a and (-)-14 were able to modulate aggregation of α-synuclein protein efficiently. Finally, in an in vivo PD animal model, compound (-)-8a exhibited efficacious anti-parkinsonian effect.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP104632271-B	Pramipexole Related Compound D		104632-27-1	Price
AP106092095	Pramipexole Related Compound A		106092-09-5	Price

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