K. Naik, Sivakumar Thangavel, A. Alam, Shailendra Kumar
{"title":"作为抗菌剂的黄酮类似物。","authors":"K. Naik, Sivakumar Thangavel, A. Alam, Shailendra Kumar","doi":"10.2174/1872213X11666170119094702","DOIUrl":null,"url":null,"abstract":"BACKGROUND\nMost of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity and side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective.\n\n\nOBJECTIVES\nThe aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity.\n\n\nMETHOD\nAn attempt was made to synthesize a newer series of 3-methyl flavanone derivatives together with the synthesis of a series of 3- hydroxyl flavone analogues. The structures of the test compounds were elucidated and established by UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were subjected for in vitro antimicrobial screening using cup plate methods, followed by the determination of zone of inhibitions.\n\n\nRESULT\nTwo series (each 10) of 3-methyl flavanone and 3-hydroxy flavone derivatives were synthesized. The structures of the test compounds were characterized and established by various spectroscopic methods. The synthesized compounds were screened for in vitro antibacterial and antifungal activity against different strains (3-Gram positive, 3-Gram negative and 2- fungal strains).\n\n\nCONCLUSION\nSome of the 3- hydroxyl flavones derivatives (1b, 3b, 4b, and 5b) and 3- methyl flavanone derivatives (3a, 1a, 2a and 4a) were found to elicit potent antimicrobial activity. The study revealed that 3-hydroxy flavone derivatives were found to be most active against Gram negative, while 3-methyl flavanone derivatives were active against Gram positive bacteria.","PeriodicalId":20960,"journal":{"name":"Recent patents on inflammation & allergy drug discovery","volume":null,"pages":null},"PeriodicalIF":4.2000,"publicationDate":"2017-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"6","resultStr":"{\"title\":\"Flavone Analogues as Antimicrobial Agents.\",\"authors\":\"K. Naik, Sivakumar Thangavel, A. Alam, Shailendra Kumar\",\"doi\":\"10.2174/1872213X11666170119094702\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"BACKGROUND\\nMost of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity and side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective.\\n\\n\\nOBJECTIVES\\nThe aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity.\\n\\n\\nMETHOD\\nAn attempt was made to synthesize a newer series of 3-methyl flavanone derivatives together with the synthesis of a series of 3- hydroxyl flavone analogues. The structures of the test compounds were elucidated and established by UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were subjected for in vitro antimicrobial screening using cup plate methods, followed by the determination of zone of inhibitions.\\n\\n\\nRESULT\\nTwo series (each 10) of 3-methyl flavanone and 3-hydroxy flavone derivatives were synthesized. The structures of the test compounds were characterized and established by various spectroscopic methods. The synthesized compounds were screened for in vitro antibacterial and antifungal activity against different strains (3-Gram positive, 3-Gram negative and 2- fungal strains).\\n\\n\\nCONCLUSION\\nSome of the 3- hydroxyl flavones derivatives (1b, 3b, 4b, and 5b) and 3- methyl flavanone derivatives (3a, 1a, 2a and 4a) were found to elicit potent antimicrobial activity. The study revealed that 3-hydroxy flavone derivatives were found to be most active against Gram negative, while 3-methyl flavanone derivatives were active against Gram positive bacteria.\",\"PeriodicalId\":20960,\"journal\":{\"name\":\"Recent patents on inflammation & allergy drug discovery\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":4.2000,\"publicationDate\":\"2017-01-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"6\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Recent patents on inflammation & allergy drug discovery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1872213X11666170119094702\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Recent patents on inflammation & allergy drug discovery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1872213X11666170119094702","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
BACKGROUND
Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity and side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective.
OBJECTIVES
The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity.
METHOD
An attempt was made to synthesize a newer series of 3-methyl flavanone derivatives together with the synthesis of a series of 3- hydroxyl flavone analogues. The structures of the test compounds were elucidated and established by UV, IR, 1H-NMR, 13C-NMR and mass spectrometry. The synthesized compounds were subjected for in vitro antimicrobial screening using cup plate methods, followed by the determination of zone of inhibitions.
RESULT
Two series (each 10) of 3-methyl flavanone and 3-hydroxy flavone derivatives were synthesized. The structures of the test compounds were characterized and established by various spectroscopic methods. The synthesized compounds were screened for in vitro antibacterial and antifungal activity against different strains (3-Gram positive, 3-Gram negative and 2- fungal strains).
CONCLUSION
Some of the 3- hydroxyl flavones derivatives (1b, 3b, 4b, and 5b) and 3- methyl flavanone derivatives (3a, 1a, 2a and 4a) were found to elicit potent antimicrobial activity. The study revealed that 3-hydroxy flavone derivatives were found to be most active against Gram negative, while 3-methyl flavanone derivatives were active against Gram positive bacteria.
期刊介绍:
Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.