V. V. Grigoriev, A. Yu. Aksinenko, T. V. Goreva, A. V. Gabrelyan, T. A. Epishina
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引用次数: 0
Abstract
New adamantane-containing derivatives of edaravone, one of two drugs used to treat amyotrophic lateral sclerosis, were synthesized. The pyrazolone ring and adamantane moiety in the new edaravone derivatives were conjugated by alkyl and azetidine linkers via amination of the corresponding alcohol mesylates. Some of the new compounds were found to be effective blockers of the allosteric NMDA receptor binding site in rats but exhibited little activity against the intrachannel NMDA receptor binding site. The structure–activity relationship between the ability to block the ifenprodil binding site and the structure of the linkers and substituents on the molecule was analyzed.
期刊介绍：
Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including:
methods of synthesis;
results of pharmacological, toxicological, and biochemical studies;
investigation of structure - activity relationships in prediction of new compounds;
methods and technical facilities used; and
problems associated with the development of ecologically safe and economically feasible methods of industrial production.
In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world.
Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April.
All articles are peer-reviewed.
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