Synthesis of Some New Maleamic Acid and Maleimide Derivatives of Trimethoprim (TMP), with Evaluating their Biological Activity

Abstract

Some new Maleamic acid derivatives of trimethoprim and their maleimide derivatives,In first step we obtained Amic which converted to Malimide in second step (cyclization).

This work includes three different parts as shown below:

The present work involved synthesis of series of new heterocyclic derivatives containing:

First part: This part included the synthesis of trimethoprim derivatives, and produced AMIC compounds.

Second Part: This part including transfer the Amic acid in second step to maleimide via using of sodium acetate and acetic anhydride. See in scheme I.

Third Part:This part includes the evaluating of the antibacterial activities for some of the synthesized compounds. These activities has been specified against   E.coli and Staph Areus for Gram strain, the results that has been obtained exhibited measurable activities, which is seen in Table 3-6.