G. V. Mokrov, T. Yu. Vorobieva, V. E. Birukova, A. S. Pantileev, E. I. Barchukova, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko, S. A. Kryzhanovskiy, T. A. Gudasheva, V. L. Dorofeev
{"title":"N1-苄基-N2-{2-[(2,3,4-三甲氧基苄基)氨基]-乙基}乙烷-1,2-二胺的设计、合成和强心特性","authors":"G. V. Mokrov, T. Yu. Vorobieva, V. E. Birukova, A. S. Pantileev, E. I. Barchukova, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko, S. A. Kryzhanovskiy, T. A. Gudasheva, V. L. Dorofeev","doi":"10.1007/s11094-024-03198-8","DOIUrl":null,"url":null,"abstract":"<p>A new group of unsymmetrical ALM-802 analogs, <i>N</i><sup>1</sup>-benzyl-<i>N</i><sup>2</sup>-{2-[(2,3,4-trimethoxybenzyl)amino]-ethyl}ethane-1,2-diamines of general formula <b>1</b>, in which one of the aromatic groups was changed, was studied. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their ADME characteristics were analyzed. The 2,3,4-trimethoxyphenyl group used as one of the aromatic pharmacophores was shown to play a key role in the activity of compounds of this type. The presence of a second aromatic group was also important since its removal led to the disappearance of cardiotropic activity. However, its structure had significantly less impact on the activity of the corresponding compounds because a rather wide variation of substituents in this group did not change the activity in most arrhythmia and ischemia models.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.8000,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, and Cardiotropic Properties of N1-Benzyl-N2-{2-[(2,3,4-Trimethoxybenzyl)Amino]-Ethyl}Ethane-1,2-Diamines\",\"authors\":\"G. V. Mokrov, T. Yu. Vorobieva, V. E. Birukova, A. S. Pantileev, E. I. Barchukova, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko, S. A. Kryzhanovskiy, T. A. Gudasheva, V. L. Dorofeev\",\"doi\":\"10.1007/s11094-024-03198-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>A new group of unsymmetrical ALM-802 analogs, <i>N</i><sup>1</sup>-benzyl-<i>N</i><sup>2</sup>-{2-[(2,3,4-trimethoxybenzyl)amino]-ethyl}ethane-1,2-diamines of general formula <b>1</b>, in which one of the aromatic groups was changed, was studied. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their ADME characteristics were analyzed. The 2,3,4-trimethoxyphenyl group used as one of the aromatic pharmacophores was shown to play a key role in the activity of compounds of this type. The presence of a second aromatic group was also important since its removal led to the disappearance of cardiotropic activity. However, its structure had significantly less impact on the activity of the corresponding compounds because a rather wide variation of substituents in this group did not change the activity in most arrhythmia and ischemia models.</p>\",\"PeriodicalId\":19990,\"journal\":{\"name\":\"Pharmaceutical Chemistry Journal\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.8000,\"publicationDate\":\"2024-09-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Chemistry Journal\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s11094-024-03198-8\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Chemistry Journal","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s11094-024-03198-8","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Design, Synthesis, and Cardiotropic Properties of N1-Benzyl-N2-{2-[(2,3,4-Trimethoxybenzyl)Amino]-Ethyl}Ethane-1,2-Diamines
A new group of unsymmetrical ALM-802 analogs, N1-benzyl-N2-{2-[(2,3,4-trimethoxybenzyl)amino]-ethyl}ethane-1,2-diamines of general formula 1, in which one of the aromatic groups was changed, was studied. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their ADME characteristics were analyzed. The 2,3,4-trimethoxyphenyl group used as one of the aromatic pharmacophores was shown to play a key role in the activity of compounds of this type. The presence of a second aromatic group was also important since its removal led to the disappearance of cardiotropic activity. However, its structure had significantly less impact on the activity of the corresponding compounds because a rather wide variation of substituents in this group did not change the activity in most arrhythmia and ischemia models.
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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