Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors
Publication type: Journal Article
Publication date: 2014-07-29
scimago Q2
wos Q3
SJR: 0.470
CiteScore: 5.1
Impact factor: 3.1
ISSN: 10542523, 15548120
Organic Chemistry
General Pharmacology, Toxicology and Pharmaceutics
Abstract
3-[(2-Chloroquinolin-3-yl) methylene]-5-phenylfuran-2(3H)-one derivatives (6a–j and 7a–j) have been synthesized and evaluated for their antimalarial activity. Three compounds 7d, 7f, and 7g showed excellent activity (0.50–0.72 µg/mL). In addition, six compounds were active in range below 5 µg/mL. A preliminary structure–activity relationship analysis of the series suggested that electropositive character is beneficial for antimalarial activity. Falcipain-2 was identified as potential target for the compounds by in silico studies. The docking studies of synthesized compounds on falcipain-2 revealed vital interactions and their binding conformation. Compound 7d and 7f could be used as lead to develop selective falcipain-2 inhibitors as they showed good inhibition of the enzyme in enzyme assay studies.
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24
Total citations:
24
Citations from 2024:
9
(37.5%)
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GOST
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Akhter M. et al. Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors // Medicinal Chemistry Research. 2014. Vol. 24. No. 2. pp. 879-890.
GOST all authors (up to 50)
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Akhter M., Saha R., Tanwar O., Mumtaz Alam M., Zaman M. Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors // Medicinal Chemistry Research. 2014. Vol. 24. No. 2. pp. 879-890.
Cite this
RIS
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TY - JOUR
DO - 10.1007/s00044-014-1139-1
UR - https://doi.org/10.1007/s00044-014-1139-1
TI - Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors
T2 - Medicinal Chemistry Research
AU - Akhter, Mymoona
AU - Saha, Rikta
AU - Tanwar, Omprakash
AU - Mumtaz Alam, Md
AU - Zaman, M.S.
PY - 2014
DA - 2014/07/29
PB - Springer Nature
SP - 879-890
IS - 2
VL - 24
SN - 1054-2523
SN - 1554-8120
ER -
Cite this
BibTex (up to 50 authors)
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@article{2014_Akhter,
author = {Mymoona Akhter and Rikta Saha and Omprakash Tanwar and Md Mumtaz Alam and M.S. Zaman},
title = {Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors},
journal = {Medicinal Chemistry Research},
year = {2014},
volume = {24},
publisher = {Springer Nature},
month = {jul},
url = {https://doi.org/10.1007/s00044-014-1139-1},
number = {2},
pages = {879--890},
doi = {10.1007/s00044-014-1139-1}
}
Cite this
MLA
Copy
Akhter, Mymoona, et al. “Synthesis and antimalarial activity of quinoline-substituted furanone derivatives and their identification as selective falcipain-2 inhibitors.” Medicinal Chemistry Research, vol. 24, no. 2, Jul. 2014, pp. 879-890. https://doi.org/10.1007/s00044-014-1139-1.