Pyrazole, isoxazoline and bypyrimidine derivatives from polygonum senegalense and psiadia punctulata flavonoids and their anti- microbial activities
Date
2017Author
Kenanda, Evans O
Omosa, Leonidah K
Type
ArticleLanguage
enMetadata
Show full item recordAbstract
Currently, researchers have given special attention to the synthesis of hetero
cyclic compounds with nitrogen and oxygen five in five or six
membered
ring systems. This is mainly due to their wide range of biological activities.
Hence, in this study, isoxazoline, pyrazole and bypyrimidine derivatives were
synthesized from flavonoids, previously isolated from
Polygonum senega
-
lense
and
Psiadia panctulata,
and assessed for their antifungal activity.
A flavone was reacted with hydrazine hydrate to afford a pyrazole analogue
5methoxy
2(5(2,3,4,5tetramethoxyphenyl)1
H
pyrazol3yl)benzene1,3
diol (
1
) Two isoxazoline derivatives namely, 2(4,5dihydro5phenylisoxazol
3yl)5methoxybenzene1,3diol (
2
) and 2(4,5dihydro5phenylisoxazol
3yl)3,5dimethoxyphenol (
3
) were successfully synthesized by the reaction
of chalcones with hydroxylamine hydrochloride. An oxime derivative
(
4
) was also generated from a similar procedure. A reaction between a
chalcone and thiourea gave a bypyrimidine derivative, 4,5dihydro6(2,4
dihydroxy
3,6dimethoxyphenyl)4phenylpyrimidine2(1H)thione (
5
). The
products were then assessed for their antibacterial and antifungal activity. All compounds showed no significant activity except compound
2
that
demonstrated activity against standard antibacterial agent,
Streptococcus
aureus
with
IC
50
value of 7.56 and
antifungal
Candida neoformans, Candida
krusei
and
Candida glabrata
strains with IC
50
values 8.01, 8.11 and 13.74 μg/mL
respectively. We, therefore, recommend synthetic optimization of com
pound
2
as a potential antimicrobial agent.
Citation
Kenandaa, Evans Okemwa, and Leonidah Kerubo Omosab. "Pyrazole, Isoxazoline and Bypyrimidine Derivatives from Polygonum senegalense and Psiadia punctulata Flavonoids 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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