Semi-synthetic pyrazoline derivatives from polygonum senegalense chalcones and their anti-microbial activities
Date
2017Author
Kenanda, Evans O
Omosa, Leonidah K
Type
ArticleLanguage
enMetadata
Show full item recordAbstract
This paper describes the semi-synthesis and anti-microbial activity of novel
pyrazoline derivatives of
Polygonum senegalense
chalcones. The study
was carried out on the understanding that heterocycles with pyrazoline
ring systems are known to possess a broad spectrum of biological activities.
The derivatives were afforded by refluxing mixtures of chalcones and phen
-
ylhydrazine, hydrazine hydrate, and / or acetic acid in DMSO or ethanol
at low temperatures between 40-60°C in an oil-bath. The products were
characterized in by
1
H-NMR (200 or 400 MHz),
13
C-NMR spectroscopy
and ESI-HRMS. NMR data was described in detail for each derivative.
The compounds
6-15
have been screened for their
in vitro
anti-bacterial
activity against one gram positive bacteria (
S. aureus
) and anti-fungal activity
against five strains
C. krusei
,
C. neoformans,
and
C. glabrata.
They all
showed insignificant antimicrobial activities with lower IC
50
as compared
to positive control, except compound
7
that demonstrated moderate anti-
fungal activity with IC
50
values ranging between 8.01 - 13.74 μg/mL against C. krusei
,
C. neoformans
and
C. glabrata
. The compound also showed anti-
bacterial activity of IC
50
value 7.56μg/mL against
S. aureus
. Based on these
findings, we recommend that compound
7
should undergo further structural
modification in order to optimize its anti-microbial activity. Aromatic, Exudate, Heterocyclic, Pharmacologica
URI
http://phcogcommn.org/sites/default/files/10.5530pc.2017.1.8.pdfhttp://hdl.handle.net/11295/100478
Citation
Kenanda, Evans Okemwa, and Leonidah Kerubo Omosaa. "Semi-Synthetic Pyrazoline Derivatives from Polygonum senegalense Chalcones and their Anti-Microbial Activities." Pharmacognosy Communications 7.1 (2017).Publisher
University of Nairobi
Rights
Attribution-NonCommercial-NoDerivs 3.0 United StatesUsage Rights
http://creativecommons.org/licenses/by-nc-nd/3.0/us/Collections
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