Synthesis, Characterization and Antimicrobial activity of protected dipeptides and their deprotected analogs

Gill, Jatinder Pal Kaur; Singh, Simranjeet; Sethi, Nidhi

doi:10.13005/ojc/310149

Cited by 3 publications

(1 citation statement)

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“…In the work of Kayser and Meisel (1996), Tyr-Gly was reported to reinforce the proliferation of peripheral blood lymphocytes. Peptides have also been reported as an antimicrobial (Jatinder et al, 2015), carbonic anhydrase I, II, IV, and XII inhibitor (Zehra Küçükbay et al, 2016;Küçükbay et al, 2019), antiplasmodial (Amit et al, 2015;Jatinder et al, 2015), and antihypertensive agent (Kitts and Weiler, 2003). In a continuation of our work, we synthesized novel Leu-Val dipeptide carboxamide scaffolds bearing sulfonamide moieties with potent antimalarial and antimicrobial properties.…”

Section: Introductionmentioning

confidence: 90%

Novel Leu-Val Based Dipeptide as Antimicrobial and Antimalarial Agents: Synthesis and Molecular Docking

et al. 2020

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The increase of antimicrobial resistance (AMR) and antimalarial resistance are complex and severe health issues today, as many microbial strains have become resistant to market drugs. The choice for the synthesis of new dipeptide-carboxamide derivatives is as a result of their wide biological properties such as antimicrobial, anti-inflammatory, and antioxidant activities. The condensation reaction of substituted benzenesulphonamoyl pentanamides with the carboxamide derivatives using peptide coupling reagents gave targeted products (8a-j). The in silico antimalarial and antibacterial studies showed good interactions of the compounds with target protein residues and a higher dock score in comparison with standard drugs. In the in vivo study, compound 8j was the most potent antimalarial agent with 61.90% inhibition comparable with 67% inhibition for Artemisinin. In the in vitro antimicrobial activity, compounds 8a and 8b (MIC 1.2 × 10−3 M and 1.1 × 10−3 M) were most potent against S. aureus; compound 8a, 8b, and 8j with MIC 6.0 × 10−3 M, 5.7 × 10−4 M, and 6.5 × 10−4 M, respectively, were the most active against B. subtilis; compound 8b (MIC 9.5 × 10−4 M) was most active against E.coli while 8a, 8b and 8d were the most active against S. typhi. Compounds 8c and 8h (MIC 1.3 × 10−3 M) each were the most active against C. albicans, while compound 8b (MIC 1.3 × 10−4 M) was most active against A. niger.

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