Frasso, Michael
(2015)
Synthesis of (R)-Roscovitine Analogs as Potential Treatments for Lambert-Eaton Myasthenic Syndrome.
Master's Thesis, University of Pittsburgh.
(Unpublished)
Abstract
This thesis describes the preparation of pyrazolo[1-5-a]-1,3,5-triazine analogs of the Ca2+ channel agonist and cyclin-dependant kinase inhibitor (R)-roscovitine. Initially, methods to improve the published synthetic route to these analogs were investigated. Subsequently, several analogs with the pyrazolotriazine core were prepared and evaluated for agonist properties. Preliminary results suggest that this modified core retains and in some cases improves agonist behavior. A substantial increase in both the Ca2+ tail-current integral and the decay time constant tau were observed with the most active analogs MF-06 and MF-17. Modifications to the C-8 alkyl and C-2 aminobutanol sidechains did not improve agonist activity.
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Details
| Item Type: |
University of Pittsburgh ETD
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| Status: |
Unpublished |
| Creators/Authors: |
|
| ETD Committee: |
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| Date: |
9 January 2015 |
| Date Type: |
Publication |
| Defense Date: |
28 July 2014 |
| Approval Date: |
9 January 2015 |
| Submission Date: |
6 August 2014 |
| Access Restriction: |
5 year -- Restrict access to University of Pittsburgh for a period of 5 years. |
| Number of Pages: |
76 |
| Institution: |
University of Pittsburgh |
| Schools and Programs: |
Dietrich School of Arts and Sciences > Chemistry |
| Degree: |
MS - Master of Science |
| Thesis Type: |
Master's Thesis |
| Refereed: |
Yes |
| Uncontrolled Keywords: |
Lambert-Eaton myasthenic sydrome, (R)-roscovitine, Ca2+ channel agonist |
| Date Deposited: |
09 Jan 2015 21:18 |
| Last Modified: |
09 Jan 2020 06:15 |
| URI: |
http://d-scholarship.pitt.edu/id/eprint/22632 |
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