Literature DB >> 10890170

Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa.

G M Cingolani1, A Di Stefano, B Mosciatti, F Napolitani, G Giorgioni, M Ricciutelli, F Claudi.   

Abstract

The synthesis and in vitro chemical and enzymatic stability of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine (9) as L-Dopa prodrug are described. Prodrug 9 possesses a good lipophilicity (log P = 2.153 +/- 0.017), is stable in aqueous buffer solutions (pH 1.3 and 7.4), and in 80% rat and human plasma it is turned into L-Dopa.

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Year:  2000        PMID: 10890170     DOI: 10.1016/s0960-894x(00)00249-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  Cytogenetic and oxidative alterations after exposure of cultured human whole blood cells to lithium metaborate dehydrate.

Authors:  Fatih Çağlar Çelikezen; Başak Toğar; Fatma Betül Özgeriş; Mehmet Sait İzgi; Hasan Türkez
Journal:  Cytotechnology       Date:  2015-02-14       Impact factor: 2.058

2.  The carvacrol ameliorates acute pancreatitis-induced liver injury via antioxidant response.

Authors:  Murat Bakır; Fatime Geyikoglu; Suat Colak; Hasan Turkez; Tulay Ozhan Bakır; Mirkhalil Hosseinigouzdagani
Journal:  Cytotechnology       Date:  2015-09-08       Impact factor: 2.058

3.  Carvacrol modulates oxidative stress and decreases cell injury in pancreas of rats with acute pancreatitis.

Authors:  Yeliz Kılıç; Fatime Geyikoglu; Suat Çolak; Hasan Turkez; Murat Bakır; Mirkhalil Hsseinigouzdagani
Journal:  Cytotechnology       Date:  2015-06-21       Impact factor: 2.058

4.  The in vitro protective effect of salicylic acid against paclitaxel and cisplatin-induced neurotoxicity.

Authors:  Damla Cetin; Ahmet Hacımuftuoglu; Abdulgani Tatar; Hasan Turkez; Basak Togar
Journal:  Cytotechnology       Date:  2015-07-22       Impact factor: 2.058

5.  Carvacrol codrugs: a new approach in the antimicrobial plan.

Authors:  Ivana Cacciatore; Mara Di Giulio; Erika Fornasari; Antonio Di Stefano; Laura Serafina Cerasa; Lisa Marinelli; Hasan Turkez; Emanuela Di Campli; Soraya Di Bartolomeo; Iole Robuffo; Luigina Cellini
Journal:  PLoS One       Date:  2015-04-10       Impact factor: 3.240

Review 6.  Dopamine and Levodopa Prodrugs for the Treatment of Parkinson's Disease.

Authors:  Fatma Haddad; Maryam Sawalha; Yahya Khawaja; Anas Najjar; Rafik Karaman
Journal:  Molecules       Date:  2017-12-25       Impact factor: 4.411

Review 7.  Diketomorpholines: Synthetic Accessibility and Utilization.

Authors:  Lan Phuong Vu; Michael Gütschow
Journal:  ACS Omega       Date:  2021-12-22

Review 8.  Antiparkinson prodrugs.

Authors:  Antonio Di Stefano; Piera Sozio; Laura Serafina Cerasa
Journal:  Molecules       Date:  2008-01-16       Impact factor: 4.411

  8 in total

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