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Synthesis and biological activity of peptide derivatives of 1,2-dihydro-3- methyl-2-oxoquinoxaline-6-carboxylic acid | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Abstract

Synthesis and biological activity of peptide derivatives of 1,2-dihydro-3- methyl-2-oxoquinoxaline-6-carboxylic acid

Author(s): Sachin Chaudhary a,b* and Sushil Kumar

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 nov el 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, 1 HNMR spectral data. All the synthesized peptide der ivatives were screened for their antibacterial, ant ifungal and anthelmintic activity against four pathogenic bacte ria, fungus strains and three earthworm species. Th e newly synthesized peptide derivatives had shown moderate to good anthelmintic activity against three earthwo rm species Megascoplex konkanensis, Pontoscotex corethruses an d Eudrilus eugeniea and exhibited potent bioactivit y against gram negative-bacteria Pseudomonas aeruginosa and K lebsiella pneumonia and fungal strains of Candida a lbicans and Aspergillus niger


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