Aziz‐ur‐Rehman, I. Ahmad, M. Abbasi, S. Z. Siddiqui, K. Nafeesa, A. Sattar, Irshad Ahmed, S. Afzal
{"title":"N-(二甲基苯基取代)-N-乙基/苄基-4-氯苯磺酰胺衍生物的合成及生物学筛选","authors":"Aziz‐ur‐Rehman, I. Ahmad, M. Abbasi, S. Z. Siddiqui, K. Nafeesa, A. Sattar, Irshad Ahmed, S. Afzal","doi":"10.15228/2014.V04.I04.P01","DOIUrl":null,"url":null,"abstract":"In the undertaken research, a number of N-dimethylphenyl substituted derivatives of N-ethyl/benzyl-4-chlorobenzenesulfonamide, (6a-f & 7a-f) was synthesized and also estimated for their biological potential. The reaction of 4-chlorobenzenesulfonyl chloride with different dimethyl substituted phenyl amine (2a-f) in the presence of basic aqueous media yielded N-[(Dimethyl substituted) phenyl]-4-chlorobenzenesulfonamides (3a-f). The targeted compounds 6a-f & 7a-f were synthesized by the reaction of compounds 3a-f with electrophiles, ethyl bromide/benzyl chloride in the presence of base NaH and polar aprotic solvent (DMF). The structures of the compounds were elucidated through H-NMR, IR and mass spectral data. The synthesized compounds (6a-f & 7a-f) were screened against Gram-negative & Gram-positive bacteria and also subjected for enzyme inhibition potential against lipoxygenase and chymotrypsin enzymes and almost all the compounds exhibited moderate to good activities.","PeriodicalId":19815,"journal":{"name":"Pakistan Journal of Chemistry","volume":"95 1","pages":"153-160"},"PeriodicalIF":0.0000,"publicationDate":"2014-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Biological Screening of N-(Dimethylphenyl Substituted)-N-Ethyl/Benzyl-4-Chlorobenzenesulfonamide Derivatives\",\"authors\":\"Aziz‐ur‐Rehman, I. Ahmad, M. Abbasi, S. Z. Siddiqui, K. Nafeesa, A. Sattar, Irshad Ahmed, S. Afzal\",\"doi\":\"10.15228/2014.V04.I04.P01\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"In the undertaken research, a number of N-dimethylphenyl substituted derivatives of N-ethyl/benzyl-4-chlorobenzenesulfonamide, (6a-f & 7a-f) was synthesized and also estimated for their biological potential. The reaction of 4-chlorobenzenesulfonyl chloride with different dimethyl substituted phenyl amine (2a-f) in the presence of basic aqueous media yielded N-[(Dimethyl substituted) phenyl]-4-chlorobenzenesulfonamides (3a-f). The targeted compounds 6a-f & 7a-f were synthesized by the reaction of compounds 3a-f with electrophiles, ethyl bromide/benzyl chloride in the presence of base NaH and polar aprotic solvent (DMF). The structures of the compounds were elucidated through H-NMR, IR and mass spectral data. The synthesized compounds (6a-f & 7a-f) were screened against Gram-negative & Gram-positive bacteria and also subjected for enzyme inhibition potential against lipoxygenase and chymotrypsin enzymes and almost all the compounds exhibited moderate to good activities.\",\"PeriodicalId\":19815,\"journal\":{\"name\":\"Pakistan Journal of Chemistry\",\"volume\":\"95 1\",\"pages\":\"153-160\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2014-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pakistan Journal of Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.15228/2014.V04.I04.P01\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pakistan Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.15228/2014.V04.I04.P01","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and Biological Screening of N-(Dimethylphenyl Substituted)-N-Ethyl/Benzyl-4-Chlorobenzenesulfonamide Derivatives
In the undertaken research, a number of N-dimethylphenyl substituted derivatives of N-ethyl/benzyl-4-chlorobenzenesulfonamide, (6a-f & 7a-f) was synthesized and also estimated for their biological potential. The reaction of 4-chlorobenzenesulfonyl chloride with different dimethyl substituted phenyl amine (2a-f) in the presence of basic aqueous media yielded N-[(Dimethyl substituted) phenyl]-4-chlorobenzenesulfonamides (3a-f). The targeted compounds 6a-f & 7a-f were synthesized by the reaction of compounds 3a-f with electrophiles, ethyl bromide/benzyl chloride in the presence of base NaH and polar aprotic solvent (DMF). The structures of the compounds were elucidated through H-NMR, IR and mass spectral data. The synthesized compounds (6a-f & 7a-f) were screened against Gram-negative & Gram-positive bacteria and also subjected for enzyme inhibition potential against lipoxygenase and chymotrypsin enzymes and almost all the compounds exhibited moderate to good activities.