Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase
G. Forlani
1
,
Łukasz Berlicki
2
,
Mattia Duò
1
,
Gabriela Dziedzioła
2
,
Samuele Giberti
1
,
Michele Bertazzini
1
,
P Kafarski
2
Publication type: Journal Article
Publication date: 2013-07-03
scimago Q1
wos Q1
SJR: 1.215
CiteScore: 9.3
Impact factor: 6.2
ISSN: 00218561, 15205118
PubMed ID:
23790100
General Chemistry
General Agricultural and Biological Sciences
Abstract
Analogues of previously studied phenyl-substituted aminomethylene-bisphosphonic acids were synthesized and evaluated as inhibitors of Arabidopsis thaliana δ1-pyrroline-5-carboxylate reductase. With the aim of improving their effectiveness, two main modifications were introduced into the inhibitory scaffold: the aminomethylenebisphosphonic moiety was replaced with a hydroxymethylenebisphosphonic group, and the length of the molecule was increased by replacing the methylene linker with an ethylidene chain. In addition, chlorine atoms in the phenyl ring were replaced with various other substituents. Most of the studied derivatives showed activity in the micromolar to millimolar range, with two of them being more effective than the lead compound, with concentrations inhibiting 50% of enzyme activity as low as 50 μM. Experimental evidence supporting the ability of these inhibitors to interfere with proline synthesis in vivo is also shown.
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55
Total citations:
55
Citations from 2025:
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(5.45%)
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GOST
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Forlani G. et al. Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase // Journal of Agricultural and Food Chemistry. 2013. Vol. 61. No. 28. pp. 6792-6798.
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Forlani G., Berlicki Ł., Duò M., Dziedzioła G., Giberti S., Bertazzini M., Kafarski P. Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase // Journal of Agricultural and Food Chemistry. 2013. Vol. 61. No. 28. pp. 6792-6798.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/jf401234s
UR - https://doi.org/10.1021/jf401234s
TI - Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase
T2 - Journal of Agricultural and Food Chemistry
AU - Forlani, G.
AU - Berlicki, Łukasz
AU - Duò, Mattia
AU - Dziedzioła, Gabriela
AU - Giberti, Samuele
AU - Bertazzini, Michele
AU - Kafarski, P
PY - 2013
DA - 2013/07/03
PB - American Chemical Society (ACS)
SP - 6792-6798
IS - 28
VL - 61
PMID - 23790100
SN - 0021-8561
SN - 1520-5118
ER -
Cite this
BibTex (up to 50 authors)
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@article{2013_Forlani,
author = {G. Forlani and Łukasz Berlicki and Mattia Duò and Gabriela Dziedzioła and Samuele Giberti and Michele Bertazzini and P Kafarski},
title = {Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase},
journal = {Journal of Agricultural and Food Chemistry},
year = {2013},
volume = {61},
publisher = {American Chemical Society (ACS)},
month = {jul},
url = {https://doi.org/10.1021/jf401234s},
number = {28},
pages = {6792--6798},
doi = {10.1021/jf401234s}
}
Cite this
MLA
Copy
Forlani, G., et al. “Synthesis and Evaluation of Effective Inhibitors of Plant δ1-Pyrroline-5-carboxylate Reductase.” Journal of Agricultural and Food Chemistry, vol. 61, no. 28, Jul. 2013, pp. 6792-6798. https://doi.org/10.1021/jf401234s.