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Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa.
Bioorg Med Chem Lett. 2000 Jun 19; 10(12):1385-8.BM

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.

Authors+Show Affiliations

Dipartimento di Scienze Chimiche, Università di Camerino, Italy. giemmeci@camserv.unicam.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

10890170

Citation

Cingolani, G M., et al. "Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as Potential Prodrug of L-dopa." Bioorganic & Medicinal Chemistry Letters, vol. 10, no. 12, 2000, pp. 1385-8.
Cingolani GM, Di Stefano A, Mosciatti B, et al. Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa. Bioorg Med Chem Lett. 2000;10(12):1385-8.
Cingolani, G. M., Di Stefano, A., Mosciatti, B., Napolitani, F., Giorgioni, G., Ricciutelli, M., & Claudi, F. (2000). Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa. Bioorganic & Medicinal Chemistry Letters, 10(12), 1385-8.
Cingolani GM, et al. Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as Potential Prodrug of L-dopa. Bioorg Med Chem Lett. 2000 Jun 19;10(12):1385-8. PubMed PMID: 10890170.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa. AU - Cingolani,G M, AU - Di Stefano,A, AU - Mosciatti,B, AU - Napolitani,F, AU - Giorgioni,G, AU - Ricciutelli,M, AU - Claudi,F, PY - 2000/7/13/pubmed PY - 2001/2/28/medline PY - 2000/7/13/entrez SP - 1385 EP - 8 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 10 IS - 12 N2 - 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. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/10890170/Synthesis_of_L__+__3__3_hydroxy_4_pivaloyloxybenzyl__25_diketomorpholine_as_potential_prodrug_of_L_dopa_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(00)00249-3 DB - PRIME DP - Unbound Medicine ER -