From Chemistry Towards Technology Step-By-Step From Chemistry Towards Technology Step-By-Step От химии к технологии шаг за шагом 2782-1900 81671 10.52957/27821900_2022_04_93 Научные статьи Scientific articles Научные статьи Development and synthesis of amino acid derivatives of N-methyl analogue of procaine and benzocaine based on pharmacophore fusion strategy Development and synthesis of amino acid derivatives of N-methyl analogue of procaine and benzocaine based on pharmacophore fusion strategy Красникова Наталия Владимировна Krasnikova Natalia Vladimirovna

кандидат химических наук;

candidate of chemical sciences;

 Красников Сергей Владиславович Krasnikov Sergey Vladislavovich

доктор химических наук;

doctor of chemical sciences;

 Ярославский государственный технический университет Yaroslavl State Technical University ОАО НИИ «Ярсинтез», Ярославль, Россия Ярославль Россия OAO NII (Research Institute) "Yarsintez" Yaroslavl Russian Federation 23 12 2022 23 12 2022 3 4 93 101 08 11 2022 09 12 2022 https://chemintech.ru/en/nauka/article/81671/view

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.

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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