{"title":"作为潜在抗感染药物的头孢拉定席夫碱及其金属盐","authors":"Mohsin Ali, Obaid-ur-Rahman Abid, Wajid Rehman, Muhammad Shahid, Shumaila, Hifza Khan","doi":"10.2174/0122113525303362240429092531","DOIUrl":null,"url":null,"abstract":"\n\nA series of schiff bases(3-8) were synthesized by the reaction of cefradine with six different aldehydes/ketones.\n\n\n\nThese Schiff bases (3-8) were treated with different bases/salts (NaOH, KOH, Ca(OH)2, Ba(OH)2, Ag(NO)3) to get their metal salts. The structures of the products were as-certained by spectroscopic data. The synthesized compounds were tested for biological activities against Staphylococcus aureus (gram-positive bacterium) and Escherichia coli (gram-negative bacterium).\n\n\n\nIn general, low activities in most of the synthesized compounds were observed.\n\n\n\nA general reduction in the activities of most of the synthesized compounds in com-parison to cefradine can be linked to the unavailability of the free amino group of cefradine by its involvement in the synthesis of imine derivatives.\n\n\n\nAll the synthesized compounds were evaluated for anti-bacterial activity against two bacterial strains S.aureus and E.coli. Compound 23 shows the best activity against both the strains S. aureus and E.coli. Compounds 18, 5, 11 and 27 show good activity against S. aureus while compounds 5, 26, 27, 3, 13, 18, 19 show good activity against E. coli.\n\n\n\nReduced activities of most of the synthesized derivatives in comparison to cefradine can be linked to unavailability of free NH2 group of cefradine for any interaction by its involvement in derivatization.\n","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":"15 16","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Cefradine Schiff Bases and their Metal Salts as Potential Anti-Infective Agents\",\"authors\":\"Mohsin Ali, Obaid-ur-Rahman Abid, Wajid Rehman, Muhammad Shahid, Shumaila, Hifza Khan\",\"doi\":\"10.2174/0122113525303362240429092531\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nA series of schiff bases(3-8) were synthesized by the reaction of cefradine with six different aldehydes/ketones.\\n\\n\\n\\nThese Schiff bases (3-8) were treated with different bases/salts (NaOH, KOH, Ca(OH)2, Ba(OH)2, Ag(NO)3) to get their metal salts. The structures of the products were as-certained by spectroscopic data. The synthesized compounds were tested for biological activities against Staphylococcus aureus (gram-positive bacterium) and Escherichia coli (gram-negative bacterium).\\n\\n\\n\\nIn general, low activities in most of the synthesized compounds were observed.\\n\\n\\n\\nA general reduction in the activities of most of the synthesized compounds in com-parison to cefradine can be linked to the unavailability of the free amino group of cefradine by its involvement in the synthesis of imine derivatives.\\n\\n\\n\\nAll the synthesized compounds were evaluated for anti-bacterial activity against two bacterial strains S.aureus and E.coli. Compound 23 shows the best activity against both the strains S. aureus and E.coli. Compounds 18, 5, 11 and 27 show good activity against S. aureus while compounds 5, 26, 27, 3, 13, 18, 19 show good activity against E. coli.\\n\\n\\n\\nReduced activities of most of the synthesized derivatives in comparison to cefradine can be linked to unavailability of free NH2 group of cefradine for any interaction by its involvement in derivatization.\\n\",\"PeriodicalId\":7951,\"journal\":{\"name\":\"Anti-Infective Agents\",\"volume\":\"15 16\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-05-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Anti-Infective Agents\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/0122113525303362240429092531\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Anti-Infective Agents","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0122113525303362240429092531","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Medicine","Score":null,"Total":0}
Cefradine Schiff Bases and their Metal Salts as Potential Anti-Infective Agents
A series of schiff bases(3-8) were synthesized by the reaction of cefradine with six different aldehydes/ketones.
These Schiff bases (3-8) were treated with different bases/salts (NaOH, KOH, Ca(OH)2, Ba(OH)2, Ag(NO)3) to get their metal salts. The structures of the products were as-certained by spectroscopic data. The synthesized compounds were tested for biological activities against Staphylococcus aureus (gram-positive bacterium) and Escherichia coli (gram-negative bacterium).
In general, low activities in most of the synthesized compounds were observed.
A general reduction in the activities of most of the synthesized compounds in com-parison to cefradine can be linked to the unavailability of the free amino group of cefradine by its involvement in the synthesis of imine derivatives.
All the synthesized compounds were evaluated for anti-bacterial activity against two bacterial strains S.aureus and E.coli. Compound 23 shows the best activity against both the strains S. aureus and E.coli. Compounds 18, 5, 11 and 27 show good activity against S. aureus while compounds 5, 26, 27, 3, 13, 18, 19 show good activity against E. coli.
Reduced activities of most of the synthesized derivatives in comparison to cefradine can be linked to unavailability of free NH2 group of cefradine for any interaction by its involvement in derivatization.
期刊介绍:
Anti-Infective Agents publishes original research articles, full-length/mini reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. The scope of the journal covers all pre-clinical and clinical research on antimicrobials, antibacterials, antiviral, antifungal, and antiparasitic agents. Anti-Infective Agents is an essential journal for all infectious disease researchers in industry, academia and the health services.