Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors
Claudia Cusan
1
,
Giampiero Spalluto
1
,
Maurizio Prato
1
,
M. C. Adams
2
,
Antje Bodensieck
2
,
R L Bauer
2
,
Aurelia Tubaro
3
,
Paolo Bernardi
4
,
Tatiana Da Ros
1
Publication type: Journal Article
Publication date: 2005-01-01
PubMed ID:
15652362
Drug Discovery
Pharmaceutical Science
Abstract
A new series of potential human 5-LOX inhibitors structurally related to the 1-phenyl-3-pyrazolidinone (phenidone, 2) has been synthesized and the activity against COX-1, COX-2, and human 5-LOX enzymes has been evaluated. In contrast with literature data, we observed that phenidone resulted to be inactive against human 5-LOX, while retains its activity against cyclooxygenases in a micromolar range. The present results suggest that the substitution of the amino function at the 4-position is detrimental in terms of activity toward COX-1 and COX-2, while the presence of a double bond at the 4,5-position does not alter the biological profile against COX. The absence of activity vs. human 5-LOX strongly suggests a re-consideration of phenidone and its analogs as 5-LOX inhibitors in humans.
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GOST
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Cusan C. et al. Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors // Il Farmaco. 2005. Vol. 60. No. 1. pp. 7-13.
GOST all authors (up to 50)
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Cusan C., Spalluto G., Prato M., Adams M. C., Bodensieck A., Bauer R. L., Tubaro A., Bernardi P., Da Ros T. Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors // Il Farmaco. 2005. Vol. 60. No. 1. pp. 7-13.
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RIS
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TY - JOUR
DO - 10.1016/j.farmac.2004.09.002
UR - https://doi.org/10.1016/j.farmac.2004.09.002
TI - Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors
T2 - Il Farmaco
AU - Cusan, Claudia
AU - Spalluto, Giampiero
AU - Prato, Maurizio
AU - Adams, M. C.
AU - Bodensieck, Antje
AU - Bauer, R L
AU - Tubaro, Aurelia
AU - Bernardi, Paolo
AU - Da Ros, Tatiana
PY - 2005
DA - 2005/01/01
PB - Elsevier
SP - 7-13
IS - 1
VL - 60
PMID - 15652362
SN - 0014-827X
ER -
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BibTex (up to 50 authors)
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@article{2005_Cusan,
author = {Claudia Cusan and Giampiero Spalluto and Maurizio Prato and M. C. Adams and Antje Bodensieck and R L Bauer and Aurelia Tubaro and Paolo Bernardi and Tatiana Da Ros},
title = {Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors},
journal = {Il Farmaco},
year = {2005},
volume = {60},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.farmac.2004.09.002},
number = {1},
pages = {7--13},
doi = {10.1016/j.farmac.2004.09.002}
}
Cite this
MLA
Copy
Cusan, Claudia, et al. “Synthesis and biological evaluation of new phenidone analogues as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors.” Il Farmaco, vol. 60, no. 1, Jan. 2005, pp. 7-13. https://doi.org/10.1016/j.farmac.2004.09.002.