ISRN Organic ChemistryPub Date : 2011-03-06eCollection Date: 2011-01-01DOI: 10.5402/2011/184754
Dina A Bakhotmah, Reda M Abdul-Rahman, Mohammad S Makki, Mohamed A El-Zahabi, Mansor Suliman
{"title":"Synthesis, physiochemical properties, photochemical probe, and antimicrobial effects of novel norfloxacin analogues.","authors":"Dina A Bakhotmah, Reda M Abdul-Rahman, Mohammad S Makki, Mohamed A El-Zahabi, Mansor Suliman","doi":"10.5402/2011/184754","DOIUrl":"https://doi.org/10.5402/2011/184754","url":null,"abstract":"<p><p>The emerging resistance to antimicrobial drugs demands the synthesis of new remedies for microbial infections. Attempts have been made to prepare new compounds by modifications in the quinolone structure. An important method for the synthesis of new quinolone is using Vilsmeier approach but has its own limitations. The present work aimed to synthesize novel norfloxacin analogues using modified Vilsmeier approach and conduct preliminary investigations for the evaluation of their physicochemical properties, photochemical probe, and antimicrobial effects. In an effort to synthesize norfloxacin analogues, only 7-bromo-6-N-benzyl piperazinyl-4-oxoquinoline-3-carboxylic acid was isolated using Vilsmeier approach at high temperature, where N, N'-bis-(4-fluoro-3-nitrophenyl)-oxalamide and N, N'-bis-(3-chloro-4-fluorophenyl)-malonamide were obtained at low temperature. Correlation results showed that lipophilicity, molecular mass, and electronic factors might influence the activity. The synthesized compounds were evaluated for their antimicrobial effects against important pathogens, for their potential use in the inhibition of vitiligo. </p>","PeriodicalId":14730,"journal":{"name":"ISRN Organic Chemistry","volume":"2011 ","pages":"184754"},"PeriodicalIF":0.0,"publicationDate":"2011-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/184754","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31748425","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Malcolm J D'Souza, Anthony M Darrington, Dennis N Kevill
{"title":"A Study of Solvent Effects in the Solvolysis of Propargyl Chloroformate.","authors":"Malcolm J D'Souza, Anthony M Darrington, Dennis N Kevill","doi":"10.5402/2011/767141","DOIUrl":"https://doi.org/10.5402/2011/767141","url":null,"abstract":"<p><p>The specific rates of solvolysis of propargyl chloroformate (1) are analyzed in 22 solvents of widely varying nucleophilicity and ionizing power values at 25.0 °C using the extended Grunwald-Winstein equation. Sensitivities to solvent nucleophilicity (l) of 1.37 and to solvent ionizing power (m) of 0.47 suggest a bimolecular process with the formation of a tetrahedral intermediate. A plot of the rates of solvolysis of 1 against those previously reported for phenyl chloroformate (2) results in a correlation coefficient (R) of 0.996, a slope of 0.86, and an F-test value of 2161. The unequivocal correlation between these two substrates attest that the stepwise association-dissociation (A(N) + D(N)) mechanism previously proposed for 2 is also operative in 1.</p>","PeriodicalId":14730,"journal":{"name":"ISRN Organic Chemistry","volume":"2011 ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/767141","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30232711","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}