Synthesis of novel pyrrolyl-indomethacin derivatives

Judith Serra Moreno; Dimitrios Agas; Maria Giovanna Sabbieti; Matteo Di Magno; Antonella Migliorini; M Antonietta Loreto

doi:10.1016/j.ejmech.2012.09.008

Synthesis of novel pyrrolyl-indomethacin derivatives

Eur J Med Chem. 2012 Nov:57:391-7. doi: 10.1016/j.ejmech.2012.09.008. Epub 2012 Sep 12.

Authors

Judith Serra Moreno¹, Dimitrios Agas, Maria Giovanna Sabbieti, Matteo Di Magno, Antonella Migliorini, M Antonietta Loreto

Affiliation

¹ Chemistry Department, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.

PMID: 23149256
DOI: 10.1016/j.ejmech.2012.09.008

Abstract

In the present work, we report the synthesis of the novel esters of indomethacin (IDMC) and an ester of reduced IDMC. For this purpose, IDMC is covalently bound by using a spacer chain to the pyrrole (Py) in the 3-position. The innovative pyrrole-indomethacin (3-Py-IDMC) derivates show no cytotoxic effects in primary calvarial osteoblasts. The designed IDMC derivates have been studied because they could be injected locally as a component of polymeric micro-particles. In fact, the new 3-Py-IDMC derivatives will assure their further polymerization since the 2- and 5-monomer positions are free.

Publication types

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

MeSH terms

Actins / chemistry
Animals
Animals, Newborn
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
Anti-Inflammatory Agents, Non-Steroidal / pharmacology
Cell Proliferation / drug effects
Cell Survival / drug effects
Delayed-Action Preparations / chemical synthesis*
Delayed-Action Preparations / pharmacology
Esters
Histocytochemistry
Indomethacin / chemistry*
Injections, Intra-Articular
Male
Mice
Osteoblasts / cytology
Osteoblasts / drug effects
Oxidation-Reduction
Primary Cell Culture
Pyrroles / chemistry*
Rats
Rats, Sprague-Dawley
Skull / cytology
Skull / drug effects

Substances

Actins
Anti-Inflammatory Agents, Non-Steroidal
Delayed-Action Preparations
Esters
Pyrroles
Indomethacin