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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Acetaminophen Prodrug: Microwave-Assisted Synthesis and in vitro Metabolism Evaluation by Mass Spectrometry

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Author(s):
Murie, Valter E. [1] ; Marques, Lucas M. M. [1] ; Souza, Gloria E. P. [2] ; Oliveira, Anderson R. M. [3] ; Lopes, Norberto P. [1] ; Clososki, Giuliano C. [1, 3]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Nucleo Pesquisa Prod Nat & Sintet, Ave Cafe S-N, BR-14040903 Ribeirao Preto, SP - Brazil
[2] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Grp Farmacol, Ave Cafe S-N, BR-14040903 Ribeirao Preto, SP - Brazil
[3] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, Dept Quim, Ave Cafe S-N, BR-14040903 Ribeirao Preto, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: Journal of the Brazilian Chemical Society; v. 27, n. 6, p. 1121-1128, JUN 2016.
Web of Science Citations: 2
Abstract

Propacetamol is an acetaminophen prodrug of intravenous administration used to control fever and pain of perioperative period in multimodal analgesia therapy. After injection, it is completely converted by plasma esterases into N,N-diethylglycine and acetaminophen, its active metabolite whose mechanism of action is the inhibition of prostaglandin synthesis. Herein, we report an improved protocol for the synthesis of propacetamol hydrochloride that allows the isolation of the active pharmaceutical ingredient (API) with high purity and yield. In addition, the in vitro metabolism of propacetamol in a microssomal reaction was evaluated by ion trap tandem mass spectrometry. (AU)

FAPESP's process: 13/17658-9 - Development and validation of chromatographic and electrophoretic methods for subsequent application in studies of in vitro metabolism and biotransformation - phase 2
Grantee:Anderson Rodrigo Moraes de Oliveira
Support Opportunities: Regular Research Grants
FAPESP's process: 15/12811-9 - DIRECTED FUNCTIONALIZATION OF ARENES AND HETEROARENES AIMIMNG THE SYNTHESIS OF SUBSTANCES OF MEDICINAL INTEREST
Grantee:Giuliano Cesar Clososki
Support Opportunities: Regular Research Grants
FAPESP's process: 14/50265-3 - Distribution and metabolism of natural and synthetic xenobiotics: from the comprehension of reactional process to tissue imaging generation
Grantee:Norberto Peporine Lopes
Support Opportunities: BIOTA-FAPESP Program - Thematic Grants