Medicinal Chemistry

Author(s): Ana Maria Zbancioc, Anca Miron, Cristina Tuchilus, Pincu Rotinberg, Cosmin Teodor Mihai, Ionel I. Mangalagiu and Gheorghita Zbancioc

DOI: 10.2174/15734064113096660070

Synthesis and In vitro Analysis of Novel Dihydroxyacetophenone Derivatives with Antimicrobial and Antitumor Activities

Page: [476 - 483] Pages: 8

  • * (Excluding Mailing and Handling)

Abstract

Herein we report a feasible study concerning the design, syntheses and in vitro antimicrobial and antitumoral activities of some novel compounds with dihydroxyacetophenone (DA) moiety. An efficient and general method for the preparation of diazine with dihydroxyacetophenone (DDA) skeleton under conventional thermal heating (TH), microwave (MW) and ultrasounds (US) irradiation is presented. Antimicrobial and antitumoral tests prove that some dihydroxyacetophenone compounds (the brominated derivatives BrDA 3) have a significant biological activity. It is also to be pointed out that, basically all the dihydroxyacetophenone derivatives proved to have a powerful antibacterial activity against drug resistant Gram-negative strain Pseudomonas aeruginosa ATCC 27853. Of particular interest could be the excellent antibacterial activity of our dihydroxyacetophenone compounds against drug resistant Gram-negative strain Pseudomonas aeruginosa.

Keywords: Antimicrobial, antitumoral, dihydroxyacetophenone, microwaves, phthalazine, pyridazine, ultrasounds.

Graphical Abstract