1-(2,4-Dichlorophenyl)Butan-1-Ol置于chromium(Vi) Oxide,硫酸体系中,用 丙酮 作为反应溶剂,化学反应 0.5H,以90%的收率获得产物2,4-二氯苯丁酮
参考文献:Synthesis,Antifungal Activity,And Molecular Modeling Studies Of New Inverted Oxime Ethers Of Oxiconazole
标题:Synthesis,Antifungal Activity,And Molecular Modeling Studies Of New Inverted Oxime Ethers Of Oxiconazole
摘要:Some New Oxime Ethers Of Types 7 And 8,In Which The Methyleneaminoxy Group,C=n-O,Of Oxiconazole 6 Is In An Inverted Atomic Sequence,Were Synthesized And Tested For Their Antifungal Activities. Among Them,The Type 7 Compounds,Such As The N-Ethoxy-Morpholino-Substituted Derivatives 71-O (Table 1),Showed Good Antifungal Properties Against The Candida Strains Tested,With Minimum Inhibitory Concentration (Mic) Values Similar To Those Of The Reference Drug 6. A Remarkable Result Was Obtained With These Types Of Azoles,Which Had Shown A Cidal Character Against Candida Albicans,While The Reference Drug Oxiconazole Was Only Fungistatic In The Same Tests. This Fact May Be Seen From A Comparison Of The Mic Values With Those Of The Minimum Fungicidal Concentration (Mfc) Values For Most Of The Type 7 Compounds Assayed That Have Shown Differences Between The Mic And The Mfc,Which Are Lower Than Three Double Diluitions. A Simple Molecular Modeling Of The P450 14-Alpha-Sterol Demethylase From C. Albicans (Candida P450Dm) Was Built In Order To Understand How The Structural Differences Between Type 7 Compounds And Oxiconazole 6 Can Induce Different Antifungal Profiles. The Results Of This Work Seem To Confirm That It Is Possible To Reverse The Atomic Sequence Of The Methyleneaminoxy Group,C=n-O,Of 6,Obtaining New Imidazoles Possessing Good Antifungal Properties.
DOI:10.1021/jm020980T