Design, Synthesis and Antimycobacterial Activity of Some New Azaheterocycles: Phenanthroline with p-halo-benzoyl Skeleton. Part V

Title:Design, Synthesis and Antimycobacterial Activity of Some New Azaheterocycles: Phenanthroline with p-halo-benzoyl Skeleton. Part V

Volume: 12 Issue: 1

Author(s): Ramona Danac, Teofil Daniloaia, Vasilichia Antoci, Violeta Vasilache and Ionel I. Mangalagiu

Affiliation:

Keywords: Antimycobacterial, design, synthesis, N-alkylation, 1, 7-Phenanthroline, p-Halo-benzoyl, SAR.

Abstract: We report herein a feasible study concerning the design, synthesis, structure and in vitro antimycobacterial activity of new phenanthroline derivatives with p-halo-benzoyl skeleton. The preparation is straight and efficient, involving an N-alkylation reaction of 1,7- phenanthroline. The antimycobacterial agents have been prepared in good yields and purity. The antimycobacterial activity of the synthesized compounds was investigated against Mycobacterium tuberculosis H37Rv. Five from the eight tested compounds had activity against M. tuberculosis H37Rv under aerobic conditions. A certain influence of substituents from the para position of the benzoyl moiety was observed; thus, the 1,7- phenanthrolinium salts substituted with p-halo (Br, Cl)- benzoyl have shown the most pronounced antimycobacterial activity. SAR correlations have been done.

Cite this article as:

Danac Ramona, Daniloaia Teofil, Antoci Vasilichia, Vasilache Violeta and Mangalagiu I. Ionel, Design, Synthesis and Antimycobacterial Activity of Some New Azaheterocycles: Phenanthroline with p-halo-benzoyl Skeleton. Part V, Letters in Drug Design & Discovery 2015; 12 (1) . https://dx.doi.org/10.2174/1570180811666140819223501