Examining barbiturate scaffold for the synthesis of new agents with biological interest
Sotirios Katsamakas
1
,
Anastasios G Papadopoulos
2
,
Maria G Kouskoura
3
,
Catherine K Markopoulou
3
,
Dimitra Hadjipavlou-Litina
1
Publication type: Journal Article
Publication date: 2019-09-20
scimago Q3
wos Q2
SJR: 0.501
CiteScore: 4.8
Impact factor: 3.4
ISSN: 17568919, 17568927
PubMed ID:
31538521
Drug Discovery
Pharmacology
Molecular Medicine
Abstract
Aim: Barbiturates have a long history of being used as drugs presenting wide varieties of biological activities (antimicrobial, anti-urease and antioxidant). Reactive oxygen species are associated with inflammation implicated in cancer, atherosclerosis and autoimmune diseases. Multitarget agents represent a powerful approach to the therapy of complicated inflammatory diseases. Results: A novel series of barbiturates has been synthesized and evaluated in several in vitro assays. Compound 16b (lipoxygenases inhibitor, 55.0 μM) was found to be a cyclooxygenase-2 inhibitor (27.5 μM). Compound 8b was profiled as a drug-like candidate. Conclusion: The barbiturate core represents a new scaffold for lipoxygenases inhibition, and the undertaken derivatives show promise as multiple-target agents to combat inflammatory diseases.
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14
Total citations:
14
Citations from 2025:
2
(14.29%)
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GOST
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Katsamakas S. et al. Examining barbiturate scaffold for the synthesis of new agents with biological interest // Future Medicinal Chemistry. 2019. Vol. 11. No. 16. pp. 2063-2079.
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Katsamakas S., Papadopoulos A. G., Kouskoura M. G., Markopoulou C. K., Hadjipavlou-Litina D. Examining barbiturate scaffold for the synthesis of new agents with biological interest // Future Medicinal Chemistry. 2019. Vol. 11. No. 16. pp. 2063-2079.
Cite this
RIS
Copy
TY - JOUR
DO - 10.4155/fmc-2018-0541
UR - https://doi.org/10.4155/fmc-2018-0541
TI - Examining barbiturate scaffold for the synthesis of new agents with biological interest
T2 - Future Medicinal Chemistry
AU - Katsamakas, Sotirios
AU - Papadopoulos, Anastasios G
AU - Kouskoura, Maria G
AU - Markopoulou, Catherine K
AU - Hadjipavlou-Litina, Dimitra
PY - 2019
DA - 2019/09/20
PB - Taylor & Francis
SP - 2063-2079
IS - 16
VL - 11
PMID - 31538521
SN - 1756-8919
SN - 1756-8927
ER -
Cite this
BibTex (up to 50 authors)
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@article{2019_Katsamakas,
author = {Sotirios Katsamakas and Anastasios G Papadopoulos and Maria G Kouskoura and Catherine K Markopoulou and Dimitra Hadjipavlou-Litina},
title = {Examining barbiturate scaffold for the synthesis of new agents with biological interest},
journal = {Future Medicinal Chemistry},
year = {2019},
volume = {11},
publisher = {Taylor & Francis},
month = {sep},
url = {https://doi.org/10.4155/fmc-2018-0541},
number = {16},
pages = {2063--2079},
doi = {10.4155/fmc-2018-0541}
}
Cite this
MLA
Copy
Katsamakas, Sotirios, et al. “Examining barbiturate scaffold for the synthesis of new agents with biological interest.” Future Medicinal Chemistry, vol. 11, no. 16, Sep. 2019, pp. 2063-2079. https://doi.org/10.4155/fmc-2018-0541.