Reaction and Antimicrobial Activity of 1‐Arylethylene Benzofuranyl Ketone Derivatives.

Abstract

Fused pyrimidine derivativesFused pyrimidine derivatives R 0515 Reaction and Antimicrobial Activity of 1-Arylethylene Benzofuranyl Ketone Derivatives. -Benzalvisnaginone and khellinone derivatives (I) are transformed into various pyrimidine, cyclohexanone and pyranone derivatives. Some products are evaluated for their antimicrobial activity: derivatives (V) and (VII) show significant antibacterial effects. -(MICKY*, J. A. A.; SALEH, N. M.; MOHAMED, S. M.; MOHAMED, S. A.; SALEM, M. M.; Indian J. Chem., Sect. B: Org. Chem. Incl. Med.

Significance and Biological Importance of Pyrimidine in the Microbial World

“…Another prominent work was reported by Micky et al who synthesized the 1-arylethylene benzofuranyl ketone derivatives having pyrimidine moiety and tested their in vitro antibacterial activity. The compounds ( 105 ) and ( 106 ) due to the presence of pyrimidine-2-thione moiety were found to show moderate activity against two strains of bacteria B. cerens (Gram positive) and E. coli (Gram negative) by agar diffusion technique [ 134 ]. Patel and Gorgamwala reported the synthesis of 2-(pyrazine-2-carboxamido)-4-(2– o -aminobenzene sulfonamide-4,6–dimehylpyrimidine)-6-arylthiouredio)-s-triazine derivatives and screened them for in vitro antibacterial activity against S. aureus and E. coli .…”

A simple approach to fused pyrido[2,3-d]pyrimidines incorporating khellinone and trimethoxyphenyl moieties as new scaffolds for antibacterial and antifungal agents

“…The interesting biological activity of khellinone derivatives [19] prompted us to continue our investigation of pyrido [2,3-d]pyrimidine incorporating 4,7-dimethoxy-1-benzofuran-5-ol moiety or trimethoxyphenyl moiety. A facile synthesis of 2-amino-3-cyanopyridine derivatives in a one-pot reaction was achieved using aromatic aldehyde, methyl ketone, malononitrile and ammonium acetate [20] or by preparing α,β-unsaturated ketone followed by reaction with malononitrile in the presence of ammonium acetate [21,22].…”