Synthesis and biological activity of peptide derivatives of 1,2-dihydro-3- methyl-2-oxoquinoxaline-6-carboxylic acid
1,2-dihydro-3-methyl-2-oxoquinoxaline-6-carboxylic acid (S1) was prepared by interaction of pyruvic acid and 3,4- diaminobenzoic acid in presence of rectified spirit. Coupling of (S1) with different amino acids methyl ester hydrochlorides/dipeptide methyl esters afforded novel quinoxalopeptide derivatives (S1a-f). Selected peptide ester derivatives (S1a-f) were further hydrolyzed by using lithium hydroxide (LiOH) to afford the corresponding derivatives S2a-f. The chemical structure of all newly synthesized compounds were confirmed on the basis of IR, 1HNMR spectral data. All the synthesized peptide derivatives were screened for their antibacterial, antifungal and anthelmintic activity against four pathogenic bacteria, fungus strains and three earthworm species. The newly synthesized peptide derivatives had shown moderate to good anthelmintic activity against three earthworm species Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugeniea and exhibited potent bioactivity against gram negative-bacteria Pseudomonas aeruginosa and Klebsiella pneumonia and fungal strains of Candida albicans and Aspergillus niger.
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