Yaroslavl, Yaroslavl, Russian Federation
Yaroslavl, Yaroslavl, Russian Federation
We have developed a rational method for the synthesis of amino acid derivatives of N-methyl analogue of procaine and benzocaine using N,N-carbonyl diimidazole method in solutions. Using the PASS software package, we predicted the biological activity of a series of hybrid compounds produced by the fusion of aminoether and aminoanilide anaesthetics. All hybrid compounds have a potential lack of significant hepatotoxicity with an increased median lethal dose for both intraperitoneal and subcutaneous injection routes when the pharmocophor is fused. The synthesised compounds are of interest as potential therapeutic agents with local anaesthetic activity and low toxicity.
benzocaine, Boc-α-amino acids, N,N-carbonyldiimidazole, 4-aminobenzoic acid, local anaesthetics
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