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Published on: November 17, 2011
Imidazolidin-2-one prostaglandin analogues
P Barraclough1, W P Jackson, C J Harris
1Department of Medicinal Chemistry, Wellcome Research Laboratories, Beckenham, Kent.
Archiv Der Pharmazie
|August 1, 1991
Summary
A new analogue of BW245C, imidazolidin-2-one 3, was synthesized and tested. This compound showed similar platelet aggregation inhibition, suggesting the 5-keto group is not essential for activity.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Biochemistry
Background:
- BW245C is a known inhibitor of platelet aggregation.
- The 5-keto group's role in BW245C's activity was previously unclear.
Purpose of the Study:
- To synthesize and evaluate the 5-desoxy analogue of BW245C.
- To determine the importance of the 5-keto group for platelet inhibitory activity.
Main Methods:
- Synthesis of imidazolidin-2-one 3 via reduction of N-benzyl hydantoin derivative 6.
- Assay of compound 3's inhibitory effect on platelet aggregation compared to BW245C.
Main Results:
- Imidazolidin-2-one 3 was successfully synthesized.
- Compound 3 exhibited comparable potency to BW245C in inhibiting platelet aggregation.
Conclusions:
- The 5-keto group of BW245C is not essential for its platelet inhibitory activity.
- Imidazolidin-2-one 3 represents a potentially valuable analogue for further research into antiplatelet agents.
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