Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent
Girish D Hatnapure
1
,
Ashish P Keche
1
,
Atish H Rodge
2
,
Satish S Birajdar
1
,
Rajesh H Tale
2
,
Vandana M Kamble
3
1
Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India.
|
2
Dendrimer and Bio-organic Chemistry Laboratory, School of Chemical Science, S.R.T.M. University, Nanded, India
|
3
Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India
|
Publication type: Journal Article
Publication date: 2012-10-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
22981334
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A series of novel 6-methoxy-2-(piperazin-1-yl)-4H-chromen-4-one and 5,7-dimethoxy-2-(piperazin-1-ylmethyl)-4H-chromen-4-one derivatives of biological interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Among all the compound screened (5a-j and 10k-t), the compounds 5c, 5g, 5h, 10l, 10m, 10n and 10r found to have promising anti-inflammatory activity (up to 65-87% TNF-α and 70-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (71% TNF-a and 84% IL-6 inhibitory activities at 1 μM) while the compounds 5b, 5i, 5j, 10s and 10t found to be potent antimicrobial agent showing even 2 to 2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL.
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GOST
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Hatnapure G. D. et al. Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent // Bioorganic and Medicinal Chemistry Letters. 2012. Vol. 22. No. 20. pp. 6385-6390.
GOST all authors (up to 50)
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Hatnapure G. D., Keche A. P., Rodge A. H., Birajdar S. S., Tale R. H., Kamble V. M. Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent // Bioorganic and Medicinal Chemistry Letters. 2012. Vol. 22. No. 20. pp. 6385-6390.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2012.08.071
UR - https://doi.org/10.1016/j.bmcl.2012.08.071
TI - Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Hatnapure, Girish D
AU - Keche, Ashish P
AU - Rodge, Atish H
AU - Birajdar, Satish S
AU - Tale, Rajesh H
AU - Kamble, Vandana M
PY - 2012
DA - 2012/10/01
PB - Elsevier
SP - 6385-6390
IS - 20
VL - 22
PMID - 22981334
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
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@article{2012_Hatnapure,
author = {Girish D Hatnapure and Ashish P Keche and Atish H Rodge and Satish S Birajdar and Rajesh H Tale and Vandana M Kamble},
title = {Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2012},
volume = {22},
publisher = {Elsevier},
month = {oct},
url = {https://doi.org/10.1016/j.bmcl.2012.08.071},
number = {20},
pages = {6385--6390},
doi = {10.1016/j.bmcl.2012.08.071}
}
Cite this
MLA
Copy
Hatnapure, Girish D., et al. “Synthesis and biological evaluation of novel piperazine derivatives of flavone as potent anti-inflammatory and antimicrobial agent.” Bioorganic and Medicinal Chemistry Letters, vol. 22, no. 20, Oct. 2012, pp. 6385-6390. https://doi.org/10.1016/j.bmcl.2012.08.071.