Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives

Abstract

In this work, we prepared an excellent yield of (2-oxo-2H-pyrano[3,2-h] quinolin-4-yl) acetic acid; compound (1) and from the reaction of it with hydrazine hydrate (100%) we obtain 2-(2-oxo-2H-pyrano [3,2-h] quinolin-4-yl) aceto hydrazide (2) which is the starting material for the synthesis of several series of new compounds: such as schiff’s bases (3a-e) and compound (4) in good yields, hydrazide derivatives like compound (5), derivatives of mercapto oxadiazole as compound (6) and derivatives of pyrazolyl as compound (7). All these compounds were found to possess high antimicrobial activity against G⁺ and G^- bacteria and against antifungal as described in scheme (1). Anticancer activity was screened only for compound (1). The IC₅₀ value of it against breast cancer was found = 6.83 µM comparable with that of the drug of doxorubicin which has IC₅₀ = 5.6. As a result these newly compounds from (1) to (7) are considerable as potent compounds for various pharmacological activities.