{"title":"新型β-内酰胺类化合物对黄嘌呤氧化酶活性的体外影响。","authors":"Arlinda Bytyqi-Damoni, Hayriye Genç, Mustafa Zengin, Serap Beyaztas, Nahit Gençer, Oktay Arslan","doi":"10.3109/10731199.2012.678943","DOIUrl":null,"url":null,"abstract":"<p><p>Carbazole substituted imines (2a-l) were prepared from N-methyl-3-amino carbazole with different aldehydes. The imines compounds undergo (2+2) cycloaddition reactions with in situ ketenes to produce β-lactam compounds (3a-l). The β-lactam compounds were tested as inhibitors of the xanthine oxidase (XO) purified from bovine milk. The results show that these compounds exhibit inhibitory effects on XO at low concentrations with IC(50) values ranging from 21.65 to 58.04 µM. The most effective compound for XO was 4-(4-chlorophenyl)-1-(9-ethyl-9H-carbazol-3-yl)-3-phenylazetidin-2-one with IC(50) of 21.65 μM. The lactams investigated here showed effective XO inhibitory effects, in the same range as the clinically used allopurinol.</p>","PeriodicalId":8413,"journal":{"name":"Artificial cells, blood substitutes, and immobilization biotechnology","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2012-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10731199.2012.678943","citationCount":"17","resultStr":"{\"title\":\"In vitro effect of novel β-lactam compounds on xanthine oxidase enzyme activity.\",\"authors\":\"Arlinda Bytyqi-Damoni, Hayriye Genç, Mustafa Zengin, Serap Beyaztas, Nahit Gençer, Oktay Arslan\",\"doi\":\"10.3109/10731199.2012.678943\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Carbazole substituted imines (2a-l) were prepared from N-methyl-3-amino carbazole with different aldehydes. The imines compounds undergo (2+2) cycloaddition reactions with in situ ketenes to produce β-lactam compounds (3a-l). The β-lactam compounds were tested as inhibitors of the xanthine oxidase (XO) purified from bovine milk. The results show that these compounds exhibit inhibitory effects on XO at low concentrations with IC(50) values ranging from 21.65 to 58.04 µM. The most effective compound for XO was 4-(4-chlorophenyl)-1-(9-ethyl-9H-carbazol-3-yl)-3-phenylazetidin-2-one with IC(50) of 21.65 μM. The lactams investigated here showed effective XO inhibitory effects, in the same range as the clinically used allopurinol.</p>\",\"PeriodicalId\":8413,\"journal\":{\"name\":\"Artificial cells, blood substitutes, and immobilization biotechnology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2012-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.3109/10731199.2012.678943\",\"citationCount\":\"17\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Artificial cells, blood substitutes, and immobilization biotechnology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3109/10731199.2012.678943\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2012/6/6 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Artificial cells, blood substitutes, and immobilization biotechnology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3109/10731199.2012.678943","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2012/6/6 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
In vitro effect of novel β-lactam compounds on xanthine oxidase enzyme activity.
Carbazole substituted imines (2a-l) were prepared from N-methyl-3-amino carbazole with different aldehydes. The imines compounds undergo (2+2) cycloaddition reactions with in situ ketenes to produce β-lactam compounds (3a-l). The β-lactam compounds were tested as inhibitors of the xanthine oxidase (XO) purified from bovine milk. The results show that these compounds exhibit inhibitory effects on XO at low concentrations with IC(50) values ranging from 21.65 to 58.04 µM. The most effective compound for XO was 4-(4-chlorophenyl)-1-(9-ethyl-9H-carbazol-3-yl)-3-phenylazetidin-2-one with IC(50) of 21.65 μM. The lactams investigated here showed effective XO inhibitory effects, in the same range as the clinically used allopurinol.