{"title":"新型肉桂碱融合曼尼希碱的合成:抗菌、镇痛和抗炎活性的药理评价","authors":"G. Kalyani, S. Bethi, K. V. Sastry, V. Kuchana","doi":"10.25258/IJPCR.V9I7.8784","DOIUrl":null,"url":null,"abstract":"In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensation\nreaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures of\ncompounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newly\nsynthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), and\nEeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which are\nhaving larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli when\ncompared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120\nmins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantly\nhigher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar antiinflammatory\nactivity when compared with celecoxib (20 mg/kg).","PeriodicalId":19889,"journal":{"name":"药学与临床研究","volume":"7 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2017-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"4","resultStr":"{\"title\":\"Synthesis of Novel Cinnoline Fused Mannich Bases: Pharmacological Evaluation of Antibacterial, Analgesic and Anti-Inflammatory Activities\",\"authors\":\"G. Kalyani, S. Bethi, K. V. Sastry, V. Kuchana\",\"doi\":\"10.25258/IJPCR.V9I7.8784\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensation\\nreaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures of\\ncompounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newly\\nsynthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), and\\nEeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which are\\nhaving larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli when\\ncompared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120\\nmins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantly\\nhigher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar antiinflammatory\\nactivity when compared with celecoxib (20 mg/kg).\",\"PeriodicalId\":19889,\"journal\":{\"name\":\"药学与临床研究\",\"volume\":\"7 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-07-25\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"药学与临床研究\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.25258/IJPCR.V9I7.8784\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"药学与临床研究","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.25258/IJPCR.V9I7.8784","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis of Novel Cinnoline Fused Mannich Bases: Pharmacological Evaluation of Antibacterial, Analgesic and Anti-Inflammatory Activities
In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensation
reaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures of
compounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newly
synthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), and
Eeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which are
having larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli when
compared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120
mins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantly
higher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar antiinflammatory
activity when compared with celecoxib (20 mg/kg).