{"title":"三氟烷基-N, N ' -二取代硫脲的合成及体外抑菌活性研究","authors":"M. Sanhoury","doi":"10.19080/omcij.2019.09.555770","DOIUrl":null,"url":null,"abstract":"A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"32 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2020-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Synthesis, In vitro Antibacterial and Antifungal Activities of Trifluoroalkyl-N, N’-Disubstituted Thioureas\",\"authors\":\"M. Sanhoury\",\"doi\":\"10.19080/omcij.2019.09.555770\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.\",\"PeriodicalId\":19547,\"journal\":{\"name\":\"Organic & Medicinal Chemistry International Journal\",\"volume\":\"32 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-07-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Organic & Medicinal Chemistry International Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.19080/omcij.2019.09.555770\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic & Medicinal Chemistry International Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.19080/omcij.2019.09.555770","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis, In vitro Antibacterial and Antifungal Activities of Trifluoroalkyl-N, N’-Disubstituted Thioureas
A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.