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

Journal Title: JOURNAL OF ADVANCES IN CHEMISTRY - Year 2014, Vol 9, Issue 2

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. 

Authors and Affiliations

Mona A. Hosny, Wafaa A. Mokbe, Emtithal A. El-Sawi

Keywords

Related Articles

Electronegativity, Hardness and Atomic number: Mutual relationships explored via novel isoelectronic series methodology

The novel isoelectronic methodology proposed recently, reveals electronic configuration dependent relationship between the hardness and atomic number, and electronegativity and hardness.  In eight out of the first ten i...

Synthesis and Antimicrobial Evaluation of Some New Benzoxazinone and Quinazolinone Derivatives

Ring opening reactions of benzoxazinone (2) with nitrogen and oxygen nucleophiles gave the corresponding benzamides (3)&(4) and benzoates (5).Quinazolinone derivatives (6) and (7) were obtained upon treatment of (2)...

Calcium, Zinc and Phytate Interrelationships in Four Lesser-Known African Seeds Processed into Food Condiments

The calcium (Ca), zinc (Zn) and phytate contents of raw, boiled, and boiled plus 72 h fermented samples of four lesser-known African seeds – Citrullus colocynthis, Cucumeropsis edulis, Ricinus communis  and Prosopis a...

ANN MODELLING OF SMALL HOLE DRILLING ON MONEL METAL BY USING ELECTRICAL DISCHARGE MACHINING

The selection of best combination of the process parameters in small hole drilling by Electrical Discharge Machining for an optimum material removal rate with a reduced tool wear rate can reduce machining time and yield...

Reactivity of Hydrazine, Some Hydrazine derivatives and Diamines toward Ethyl 2,2-Dicyano-1-aryl (or alkyl)vinylcarbamate

A series of pyrimidinone and dipyrimidinone derivatives 2a-c, 4a-e and 6a-f has been synthesized via the reaction between ethyl 2,2-dicyano-1-aryl(or alkyl)vinylcarbamate derivatives 1a-d and hydrazine derivatives or  d...

Download PDF file
  • EP ID EP652670
  • DOI 10.24297/jac.v9i2.2341
  • Views 133
  • Downloads 0

How To Cite

Mona A. Hosny, Wafaa A. Mokbe, Emtithal A. El-Sawi (2014). Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives. JOURNAL OF ADVANCES IN CHEMISTRY, 9(2), 1892-1899. https://europub.co.uk/articles/-A-652670