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Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues
In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-16...
| Autores principales: | , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2012
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268254/ https://www.ncbi.nlm.nih.gov/pubmed/23192189 http://dx.doi.org/10.3390/molecules171214126 |
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| author | de Miranda, Amanda Silva Júnior, Walfrido Bispo da Silva, Yolanda Karla Cupertino Alexandre-Moreira, Magna Suzana Castro, Rosane de Paula Sabino, José Ricardo Lião, Luciano Morais Lima, Lídia Moreira Barreiro, Eliezer J. |
| author_facet | de Miranda, Amanda Silva Júnior, Walfrido Bispo da Silva, Yolanda Karla Cupertino Alexandre-Moreira, Magna Suzana Castro, Rosane de Paula Sabino, José Ricardo Lião, Luciano Morais Lima, Lídia Moreira Barreiro, Eliezer J. |
| author_sort | de Miranda, Amanda Silva |
| collection | PubMed |
| description | In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 μM. |
| format | Online Article Text |
| id | pubmed-6268254 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2012 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-62682542018-12-14 Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues de Miranda, Amanda Silva Júnior, Walfrido Bispo da Silva, Yolanda Karla Cupertino Alexandre-Moreira, Magna Suzana Castro, Rosane de Paula Sabino, José Ricardo Lião, Luciano Morais Lima, Lídia Moreira Barreiro, Eliezer J. Molecules Article In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 μM. MDPI 2012-11-28 /pmc/articles/PMC6268254/ /pubmed/23192189 http://dx.doi.org/10.3390/molecules171214126 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
| spellingShingle | Article de Miranda, Amanda Silva Júnior, Walfrido Bispo da Silva, Yolanda Karla Cupertino Alexandre-Moreira, Magna Suzana Castro, Rosane de Paula Sabino, José Ricardo Lião, Luciano Morais Lima, Lídia Moreira Barreiro, Eliezer J. Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title | Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title_full | Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title_fullStr | Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title_full_unstemmed | Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title_short | Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues |
| title_sort | design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268254/ https://www.ncbi.nlm.nih.gov/pubmed/23192189 http://dx.doi.org/10.3390/molecules171214126 |
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