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. 2011 Dec 28;17(1):227-39.
doi: 10.3390/molecules17010227.

Synthesis and biological activity of some 3-(4-(substituted)-piperazin-1-yl)cinnolines

Eman D Awad  1 , Mustafa M El-Abadelah, Suzan Matar, Malek A Zihlif, Randa G Naffa, Ehab Q Al-Momani, Mohammad S Mubarak
Affiliations

Synthesis and biological activity of some 3-(4-(substituted)-piperazin-1-yl)cinnolines

Eman D Awad et al. Molecules. .

Abstract

A new series of 6-substituted-4-methyl-3-(4-arylpiperazin-1-yl)cinnolines 8-10 were synthesized as potential antifungal agents via intramolecular cyclization of the respective 1-(2-arylhydrazono)-1-(4-arylpiperazin-1-yl)propan-2-ones 5-7, mediated by polyphosphoric acid (PPA). The amidrazones themselves were synthesized via direct interaction of the appropriate hydrazonoyl chlorides 4a-d with the corresponding N-substituted piperazine in the presence of triethylamine. The structures of the new prepared compounds were confirmed by elemental analyses, (1)H-NMR, (13)C-NMR, and ESI-HRMS spectral data. The antitumor, antibacterial, and antifungal activity of the newly synthesized compounds was evaluated.

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Figures

Figure 1
Figure 1
Cinoxacine (1) and ICI-D-7569 (2).
Scheme 1
Scheme 1
The synthetic route for compounds 8–10.
See this image and copyright information in PMC

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