B. Sahoo, B. Banik, Mazaharunnisa, N. Rao, B. Raju
{"title":"微波辅助下苯并咪唑衍生物的绿色合成及其抗惊厥活性评价","authors":"B. Sahoo, B. Banik, Mazaharunnisa, N. Rao, B. Raju","doi":"10.2174/2213335606666190429124745","DOIUrl":null,"url":null,"abstract":"\n\nBenzimidazole is the fused heterocyclic aromatic compound. It is an essential\npharmacophore and privileged structure for the development of new drug molecules. These are\nbioactive molecules present in various anthelmintic drugs such as albendazole, mebendazole, parbendazole,\ntriclabendazole etc.\n\n\n\nBenzimidazole derivatives are synthesized by reaction between orthophenylene diamine\nand anthranillic acid followed by acetylation in the presence of acetic anhydride. Finally, the acetylated\nproducts undergo Claisen-Schimdt condensation with various substituted benzaldehydes to produce\ncorresponding benzimidazole derivatives or chalcones. Both conventional and microwave irradiation\ntechnology are followed to get the titled compounds. The titled compounds are screened for\ntheir anticonvulsant and neurotoxicity activity.\n\n\n\nBy the help of microwave synthesis, the yield of product was increased in less reaction time.\nSo, it follows Green chemistry approach by making above reactions eco-friendly. Some of the compounds\nexhibited significant anticonvulsant activity as compared to standard drug.\n\n\n\nIn the present investigation, we have synthesized novel benzimdazole derivatives with\nchalone moiety to improve the biological activity. The compounds were obtained under microwave\nreaction with high yield in a short reaction time.\n","PeriodicalId":43539,"journal":{"name":"Current Microwave Chemistry","volume":" ","pages":""},"PeriodicalIF":0.9000,"publicationDate":"2019-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/2213335606666190429124745","citationCount":"15","resultStr":"{\"title\":\"Microwave Assisted Green Synthesis of Benzimidazole Derivatives and Evaluation of Their Anticonvulsant Activity\",\"authors\":\"B. Sahoo, B. Banik, Mazaharunnisa, N. Rao, B. Raju\",\"doi\":\"10.2174/2213335606666190429124745\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nBenzimidazole is the fused heterocyclic aromatic compound. It is an essential\\npharmacophore and privileged structure for the development of new drug molecules. These are\\nbioactive molecules present in various anthelmintic drugs such as albendazole, mebendazole, parbendazole,\\ntriclabendazole etc.\\n\\n\\n\\nBenzimidazole derivatives are synthesized by reaction between orthophenylene diamine\\nand anthranillic acid followed by acetylation in the presence of acetic anhydride. Finally, the acetylated\\nproducts undergo Claisen-Schimdt condensation with various substituted benzaldehydes to produce\\ncorresponding benzimidazole derivatives or chalcones. Both conventional and microwave irradiation\\ntechnology are followed to get the titled compounds. The titled compounds are screened for\\ntheir anticonvulsant and neurotoxicity activity.\\n\\n\\n\\nBy the help of microwave synthesis, the yield of product was increased in less reaction time.\\nSo, it follows Green chemistry approach by making above reactions eco-friendly. Some of the compounds\\nexhibited significant anticonvulsant activity as compared to standard drug.\\n\\n\\n\\nIn the present investigation, we have synthesized novel benzimdazole derivatives with\\nchalone moiety to improve the biological activity. The compounds were obtained under microwave\\nreaction with high yield in a short reaction time.\\n\",\"PeriodicalId\":43539,\"journal\":{\"name\":\"Current Microwave Chemistry\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2019-10-24\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.2174/2213335606666190429124745\",\"citationCount\":\"15\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Microwave Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/2213335606666190429124745\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Microwave Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/2213335606666190429124745","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Microwave Assisted Green Synthesis of Benzimidazole Derivatives and Evaluation of Their Anticonvulsant Activity
Benzimidazole is the fused heterocyclic aromatic compound. It is an essential
pharmacophore and privileged structure for the development of new drug molecules. These are
bioactive molecules present in various anthelmintic drugs such as albendazole, mebendazole, parbendazole,
triclabendazole etc.
Benzimidazole derivatives are synthesized by reaction between orthophenylene diamine
and anthranillic acid followed by acetylation in the presence of acetic anhydride. Finally, the acetylated
products undergo Claisen-Schimdt condensation with various substituted benzaldehydes to produce
corresponding benzimidazole derivatives or chalcones. Both conventional and microwave irradiation
technology are followed to get the titled compounds. The titled compounds are screened for
their anticonvulsant and neurotoxicity activity.
By the help of microwave synthesis, the yield of product was increased in less reaction time.
So, it follows Green chemistry approach by making above reactions eco-friendly. Some of the compounds
exhibited significant anticonvulsant activity as compared to standard drug.
In the present investigation, we have synthesized novel benzimdazole derivatives with
chalone moiety to improve the biological activity. The compounds were obtained under microwave
reaction with high yield in a short reaction time.