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Synthesis of (R)-Roscovitine Analogs as Potential Treatments for Lambert-Eaton Myasthenic Syndrome

Frasso, Michael (2015) Synthesis of (R)-Roscovitine Analogs as Potential Treatments for Lambert-Eaton Myasthenic Syndrome. Master's Thesis, University of Pittsburgh. (Unpublished)

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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
Status: Unpublished
Creators/Authors:
CreatorsEmailPitt UsernameORCID
Frasso, Michaelmaf174@pitt.eduMAF174
ETD Committee:
TitleMemberEmail AddressPitt UsernameORCID
Committee ChairWipf, Peterpwipf@pitt.eduPWIPF
Committee MemberHorne, W. Sethhorne@pitt.eduHORNE
Committee MemberKoide, Kazunorikoide@pitt.eduKOIDE
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: 15 Nov 2016 14:22
URI: http://d-scholarship.pitt.edu/id/eprint/22632

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