ANTIMICROBIAL ACTIVITY OF AMINO ACID DERIVATIVES OF MEMANTINE
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2022-01-01
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Abstract
Memantine is adamantane derivative used in medicinal practice. It is well-proven inhibitors of the M2 ion channel of influenza virus. In addition, it is applied for treatment of patients with Alzheimer’s disease. Herein, we report the antimicrobial activity of specifically designed memantine derivatives containing spatially compact (Gly, Ala, β-Ala) and bulky (Val and Phe) amino acids. New compounds were synthesized in a solution using 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethylaminium tetrafluoroborate (TBTU) as a coupling agent. All derivatives were obtained with good yields. Newly synthesized molecules at concentration 100 mM were tested for their antimicrobial activity using model strains of Gram-positive (Bacillus subtilis NBIMCC 3562), Gram-negative (Escherichia coli NBIMCC K12 407) microorganisms and fungal strain Candida albicans NBIMCC 74. The active compounds against model G+ microorganism are Val-MEM followed by Ala-MEM and Gly-MEM. All compounds show good activity against model G-microorganism. Introducing of bulky amino acid Phe, containing aromatic core, and Val, containing aliphatic core, leads to good antifungal activity