Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships the side-chain

Dimitrov Ivaylo V.; Harvey Martyn G.; Voss Logan J.Sleigh James W.Bickerdike Michael J.Denny William A.

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Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships the side-chain

机译：Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships the side-chain

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N-Aliphatic ester analogues of the non-opioid ketamine (1) retain effective anaesthetic/analgesic properties while minimising ketamine's psychomimetic side-effects. We show that the anaesthetic/analgesic properties of these ester analogues depend critically on the length (from 2 to 4 carbons), polarity and steric cross-section of the aliphatic linker chain. More stable amide and ethylsulfone analogues generally showed weaker anaesthetic/analgesic activity. There was no correlation between the anaesthetic/analgesic properties of the compounds and their binding affinities for the N-methyl-D-aspartate (NMDA) receptor.

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来源
《Bioorganic and medicinal chemistry》 |2019年第7期|1226-1231|共6页
作者
Dimitrov Ivaylo V.; Harvey Martyn G.; Voss Logan J.Sleigh James W.Bickerdike Michael J.Denny William A.;
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作者单位

Univ Auckland, Sch Med Sci, Auckland Canc Soc, Res Ctr, Auckland, New Zealand;

Univ Auckland, Waikato Clin Sch, Auckland, New Zealand;

Kea Therapeut Ltd, Auckland, New Zealand;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Ketamine; Esters; Anaesthesia; Short-acting; Structure-activity relationship;

Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships the side-chain

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