Synthesis and biological activities of a-sulfamido/ a-amino phosphonate dervatives of N-heterocycle

Abstract

In this study, we describe a simple one-pot synthesis of novel α-aminophosphonates via the Kabachnik-Fields reaction bearing N-Sulfamoyl aminopyridine 3a-7a and 3b-4b and 5 (ethylthio)-1, 3, 4-thiadiazol-2-yl) α-aminophosphonate derivatives. The synthesized molecules were rationally designed and synthesized according to the principle of synergic bioactive substructures. The synthesized compounds were obtained with a moderate yield without chromatographic work-up and were characterized by the usual spectroscopic methods: 1H NMR,13C NMR, HSQC, and HMBC. Some compounds were evaluated for in vitro antioxidant (DPPH and SPF) and anti inflammatory activity in order to demonstrate the potential spectrum of the obtained α aminophosphonates.