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Abstract

BIOLOGICAL EVALUATION OF AZA-HETEROCYCLIC DERIVATIVES AND THEIR INTERMEDIATES

Erum Dilshad, Bushra Mirza*, Muhammad Shabbir, Zia-ul- Haq, Zareen Akhter

ABSTRACT

The objective of present study was to carry out biological evaluation of
aza-heterocyclic derivatives including methoxy, phenoxy, alkyl and
aryl derivatives of pyrazoles and their intermediates i.e. diketones. All
of the compounds were evaluated to find their potential as
antimicrobial, antioxidant and antitumor agents. Antimicrobial
screening was done by finding the bactericidal and fungicidal activity
of the test compounds using agar well diffusion and agar tube dilution
methods. Antioxidant potential was examined by DPPH free radical
scavenging and DNA damage assays. Whereas antitumor findings
were based on the potato disc tumor assy. Among all the tested
compounds, 2-(5-(4-hydroxyphenyl)-1-phenyl-1Hpyrazol-
3-yl)phenol (IX), a pyrazole having three phenyl groups has shown the highest
antimicrobial, antitumor, and DNA protective activity while the compound 1-(2-
hydroxyphenyl)-3-(2 methoxyphenyl)propane-1,3-dione (I) has shown the best antioxidant
potential. Data obtained from these experiments indicated the possible biological activities of
these compounds and enabled us to compare these compounds as antimicrobial, antioxidant
and antitumor agents. On the basis of these findings, efforts for the pharmacological
applications of these heterocyclic compounds can be initiated.

Keywords: Heterocyclic derivatives, pyrazoles, intermediates of pyrazoles, diketones, biological evaluation.


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