Synthesis of new α aminophosphonate system bearing Indazole moiety and their biological activity

We are reporting herein for the first time the synthesis of α-aminophosphonates containing Indazole moiety in two steps. In the first step, imines of substituted N-benzylidene-1-methyl-1H-indazole-3-carbohydrazide are synthesized and in the next step it has converted to α-aminophosphonates using chlorotrimethylsilane (TMSCl) and triethyl phosphite. Some of the synthesized derivatives are evaluated for antibacterial activity against different bacterial strains.

Imines of substituted N-benzylidene-1-methyl-1H-indazole-3-carbohydrazide were synthesized and it was converted to α-aminophosphonates using chlorotrimethylsilane (TMSCl) and triethyl phosphite. Antibacterial activity against different bacterial strains were evaluated.Figure optionsDownload as PowerPoint slideHighlights
► A first time a new series of α-aminophosphonate derivatives containing highly bioactive Indazole moiety prepared in two steps.
► Some of the synthesized derivatives were then evaluated for antibacterial activity against different bacterial strains respect to agar disc method.
► The fluoro groups 1b and 1c has shown improved the antibacterial property as compared with the other derivatives of series 1. But the overall killing or inhibiting the growth of bacteria is inferior as compared with the standard Gentamicin and Kanamycin drugs.