Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents
Publication type: Journal Article
Publication date: 2021-01-07
scimago Q3
wos Q3
SJR: 0.349
CiteScore: 2.7
Impact factor: 1.3
ISSN: 00092363, 13475223
PubMed ID:
33431728
General Chemistry
Drug Discovery
General Medicine
Abstract
A series of 3-substituted-2-hydroxy-1,4-naphthoquinone derivatives with a variety of side chains were successfully synthesized by Mannich reaction of 2-hydroxy-1,4-naphthoquinone (lawsone) with selected amines and aldehydes. All substances (1-16) were evaluated for in-vitro antimalarial activity against strains of Plasmodium falciparum by microculture radioisotope technique. Bioassay data revealed that ten derivatives (1-8, 11 and 13) displayed significantly good activity with values of IC50 ranging from 0.77 to 4.05 µg/mL. The best biological profile (IC50 = 0.77 µg/mL) was observed in compound 1, possessing a n-butyl substituted aminomethyl group. Experimental results support the potential use of our active Mannich components as promising antimalarial agents in the fight against malaria infections and multidrug resistance problems.
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14
Total citations:
14
Citations from 2024:
8
(57.14%)
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GOST
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Paengsri W. et al. Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents // Chemical and Pharmaceutical Bulletin. 2021. Vol. 69. No. 3. pp. 253-257.
GOST all authors (up to 50)
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Paengsri W., Promsawan N., Baramee A. Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents // Chemical and Pharmaceutical Bulletin. 2021. Vol. 69. No. 3. pp. 253-257.
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RIS
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TY - JOUR
DO - 10.1248/cpb.c20-00770
UR - https://doi.org/10.1248/cpb.c20-00770
TI - Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents
T2 - Chemical and Pharmaceutical Bulletin
AU - Paengsri, Wanthani
AU - Promsawan, Napapha
AU - Baramee, Apiwat
PY - 2021
DA - 2021/01/07
PB - Pharmaceutical Society of Japan
SP - 253-257
IS - 3
VL - 69
PMID - 33431728
SN - 0009-2363
SN - 1347-5223
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2021_Paengsri,
author = {Wanthani Paengsri and Napapha Promsawan and Apiwat Baramee},
title = {Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents},
journal = {Chemical and Pharmaceutical Bulletin},
year = {2021},
volume = {69},
publisher = {Pharmaceutical Society of Japan},
month = {jan},
url = {https://doi.org/10.1248/cpb.c20-00770},
number = {3},
pages = {253--257},
doi = {10.1248/cpb.c20-00770}
}
Cite this
MLA
Copy
Paengsri, Wanthani, et al. “Synthesis and Evaluation of 2-Hydroxy-1,4-naphthoquinone Derivatives as Potent Antimalarial Agents.” Chemical and Pharmaceutical Bulletin, vol. 69, no. 3, Jan. 2021, pp. 253-257. https://doi.org/10.1248/cpb.c20-00770.