W Nawrocka, H Liszkiewicz, A Nawojski, M Wilimowski, L Kedzierska-Goździk, J Barczyńska, W Wojewódzki, E Duś, A Szelag, M Rutkowska
{"title":"1,5-苯二氮卓类药物的酰化衍生物。第二部分。","authors":"W Nawrocka, H Liszkiewicz, A Nawojski, M Wilimowski, L Kedzierska-Goździk, J Barczyńska, W Wojewódzki, E Duś, A Szelag, M Rutkowska","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>Acylated derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one (1) and of 2-methyl-4-phenyl-1H-tetrahydro-1,5-benzodiazepino-2-carboxylic acid ethyl ester (10) were synthesized and preliminarily tested on their central activity. Acylation was carried out with alpha, beta-unsaturated acid chlorides, dicarboxylic acid monoester monochlorides, and dicarboxylic acid dichlorides. Compounds 2, 3, 11 and 12 had analgesic, compounds 4, 11 and 12--anticonvulsant, and compounds 3 and 11--antiaggressive properties.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"43 6","pages":"495-503"},"PeriodicalIF":0.0000,"publicationDate":"1991-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Acylated derivatives of 1,5-benzodiazepines. Part II.\",\"authors\":\"W Nawrocka, H Liszkiewicz, A Nawojski, M Wilimowski, L Kedzierska-Goździk, J Barczyńska, W Wojewódzki, E Duś, A Szelag, M Rutkowska\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Acylated derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one (1) and of 2-methyl-4-phenyl-1H-tetrahydro-1,5-benzodiazepino-2-carboxylic acid ethyl ester (10) were synthesized and preliminarily tested on their central activity. Acylation was carried out with alpha, beta-unsaturated acid chlorides, dicarboxylic acid monoester monochlorides, and dicarboxylic acid dichlorides. Compounds 2, 3, 11 and 12 had analgesic, compounds 4, 11 and 12--anticonvulsant, and compounds 3 and 11--antiaggressive properties.</p>\",\"PeriodicalId\":20276,\"journal\":{\"name\":\"Polish journal of pharmacology and pharmacy\",\"volume\":\"43 6\",\"pages\":\"495-503\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1991-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Polish journal of pharmacology and pharmacy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Polish journal of pharmacology and pharmacy","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Acylated derivatives of 1,5-benzodiazepines. Part II.
Acylated derivatives of 4-methyl-1H-tetrahydro-1,5-benzodiazepin-2-one (1) and of 2-methyl-4-phenyl-1H-tetrahydro-1,5-benzodiazepino-2-carboxylic acid ethyl ester (10) were synthesized and preliminarily tested on their central activity. Acylation was carried out with alpha, beta-unsaturated acid chlorides, dicarboxylic acid monoester monochlorides, and dicarboxylic acid dichlorides. Compounds 2, 3, 11 and 12 had analgesic, compounds 4, 11 and 12--anticonvulsant, and compounds 3 and 11--antiaggressive properties.