One Pot Synthesis And Antifungal Activites Of Thiochromanones Derivatives

Thiochroman-4-one derivatives are a kind of high lipophilicity and low hydrophilcityheterocyclic compounds with Sulfur atom which has a wide range of biological activities. Itcan damage the structure and the function of the cell membrane and the wall of fungi, leadingfungi to death.19thiochromeno[4,3-c]pyrazole derivatives and15pyrano[3,2-c]thiochromanderivatives based on thiochroman-4-one were designed and synthesized in one-pot. Thestructures of new synthesized compounds were characterized by HRMS,1H NMR, and13CNMR. Antifungi activities of the target compounds were tested using double dilution method.3-carbaldehyde-thiochromanone were synthesized from substituted thiophenol as thestarting material. Then using the3-carbaldehyde-thiochromanone, phenacyl bromide andthiosemicarbazide as raw material react in order to get the target compounds.19targetcompounds were tested in vitro antifungal activity and the test results showed that some of thecompounds exhibited antifungal activity against C. Neoformans. And we compared the effectsof different solvent and reaction time for the yields of this reaction under reflux andultrasonic.Thiochromanones were synthesized through substituted reaction and cyclization reactionfrom the starting material thiophenol. Then using the substited thiochromanones,malononitrile and aromatic aldehydes as raw material to get the target compounds.15targetcompounds were tested in vitro antifungal activity and the test results showed that some of thecompounds exhibited weak antifungal activity against C. Neoformans.