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 ofaza-heterocyclic derivatives including methoxy, phenoxy, alkyl andaryl derivatives of pyrazoles and their intermediates i.e. diketones. Allof the compounds were evaluated to find their potential asantimicrobial, antioxidant and antitumor agents. Antimicrobialscreening was done by finding the bactericidal and fungicidal activityof the test compounds using agar well diffusion and agar tube dilutionmethods. Antioxidant potential was examined by DPPH free radicalscavenging and DNA damage assays. Whereas antitumor findingswere based on the potato disc tumor assy. Among all the testedcompounds, 2-(5-(4-hydroxyphenyl)-1-phenyl-1Hpyrazol-3-yl)phenol (IX), a pyrazole having three phenyl groups has shown the highestantimicrobial, antitumor, and DNA protective activity while the compound 1-(2-hydroxyphenyl)-3-(2 methoxyphenyl)propane-1,3-dione (I) has shown the best antioxidantpotential. Data obtained from these experiments indicated the possible biological activities ofthese compounds and enabled us to compare these compounds as antimicrobial, antioxidantand antitumor agents. On the basis of these findings, efforts for the pharmacologicalapplications of these heterocyclic compounds can be initiated.

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