SYNTHESIS AND UTILITY OF NEW POLYCYCLIC COMPOUNDS A S POTENTIAL ANTIMICROBIALS BASED ON CHROMENE MOIETY
By: Abdelaziz, Mahmoud N
.
Contributor(s): Zarie, Eman S.
Publisher: M P Innovare Academic Sciences Pvt Ltd 2019Edition: Vol.11(9).Description: 49-56p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
International journal of pharmacy and pharmaceutical scienceSummary: Objective:
The present research aims to synthesize some new po
lycyclic compounds including chromene moiety and st
udy their antimicrobial activity.
Methods:
Several new polycyclic systems including chromene s
caffold incorporated with pyridine, pyrimidine, imi
dazopyrimidine, and
imidazodiazocine were achieved
via
condensation reaction of chromene derivative under
the proper condition with various reagents namely;
cyanothioacetamide, phenyl isothiocyanate, malononi
trile, carbon disulfide, benzaldehyde, triethylorth
oformate, and 1,4-dichlorobutane. Moreover,
a chlorodiazenyl chromene derivative was reacted wi
th some substances possessing active–CH
2
-bridge such as ethyl cyanoacetate and
malononitrile to end up with hydrazono compounds. S
uch compounds were eventually cyclized with hydrazi
ne hydrate to form pyrazole and
oxopyrazole derivatives. Moreover, compound 1
was treated with benzoyl acetone, and then followed
by cyclization with malononitrile to provide
the corresponding 2-amino14-(4-methoxyphenyl)-4-met
hy-5-phenyl-14H-benzo[5,6] chromeno [2,3H][1,6]napht
hyridine-3-carbonitrile (20).
Results:
The results of the antimicrobial screening
in vitro
revealed that the inhibition zone (mm) of the synt
hesized compounds 1-3, 5 and 8
implied their optimum antibacterial activity, while
the compounds 4, 6 and 9-13, 15 showed a moderate
to weak antibacterial activity against
multiple species of
B. subtilis, S. aureus, E. coli and P. aeruginosa
. In contrast, the compounds 1, 6, 11, 15 showed hi
gh antifungal activities against
different species of
A. flavinand C. albicans
, while the other compounds exhibit a moderate to p
oor antifungal activity.
Conclusion:
It is remarkable that a series of chromene derivati
ves synthesized by a simple and available method le
ads to a molecule of promising
antimicrobial activity. Further research is recomme
nded to approve the importance of polycyclic system
s for various applications.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2020873 |
Objective:
The present research aims to synthesize some new po
lycyclic compounds including chromene moiety and st
udy their antimicrobial activity.
Methods:
Several new polycyclic systems including chromene s
caffold incorporated with pyridine, pyrimidine, imi
dazopyrimidine, and
imidazodiazocine were achieved
via
condensation reaction of chromene derivative under
the proper condition with various reagents namely;
cyanothioacetamide, phenyl isothiocyanate, malononi
trile, carbon disulfide, benzaldehyde, triethylorth
oformate, and 1,4-dichlorobutane. Moreover,
a chlorodiazenyl chromene derivative was reacted wi
th some substances possessing active–CH
2
-bridge such as ethyl cyanoacetate and
malononitrile to end up with hydrazono compounds. S
uch compounds were eventually cyclized with hydrazi
ne hydrate to form pyrazole and
oxopyrazole derivatives. Moreover, compound 1
was treated with benzoyl acetone, and then followed
by cyclization with malononitrile to provide
the corresponding 2-amino14-(4-methoxyphenyl)-4-met
hy-5-phenyl-14H-benzo[5,6] chromeno [2,3H][1,6]napht
hyridine-3-carbonitrile (20).
Results:
The results of the antimicrobial screening
in vitro
revealed that the inhibition zone (mm) of the synt
hesized compounds 1-3, 5 and 8
implied their optimum antibacterial activity, while
the compounds 4, 6 and 9-13, 15 showed a moderate
to weak antibacterial activity against
multiple species of
B. subtilis, S. aureus, E. coli and P. aeruginosa
. In contrast, the compounds 1, 6, 11, 15 showed hi
gh antifungal activities against
different species of
A. flavinand C. albicans
, while the other compounds exhibit a moderate to p
oor antifungal activity.
Conclusion:
It is remarkable that a series of chromene derivati
ves synthesized by a simple and available method le
ads to a molecule of promising
antimicrobial activity. Further research is recomme
nded to approve the importance of polycyclic system
s for various applications.
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