Synthesis, Characterization and Biological Activity of Some Dithiourea Derivatives

Novel dithiourea derivatives have been designed as HIV-1 protease inhibitors using Autodock 4.2, synthesized and characterized by spectroscopic methods and microanalysis. 1-(3-Bromobenzoyl)-3-[2-({[(3-bromophenyl)formamido]methanethioyl}amino)phenyl]thiourea ( 10 ) and 3-benzoyl-1{[(phenylformamido)methanethioyl]amino}thiourea ( 12 ) gave a percentage viability of 17.9±5.6% and 11.2±0.9% against Trypanosoma brucei. Single crystal X-ray diffraction analysis of 1-benzoyl-3-(5-methyl-2-{[(phenylformamido)methanethioyl]amino}phenyl)thiourea ( 1 ), 3-benzoyl-1-(2-{[(phenylformamido)methanethioyl]amino}ethyl)thiourea ( 11 ), 3-benzoyl-1-{[(phenylformamido)methanethioyl]amino}thiourea ( 12 ) and 3-benzoyl-1-(4-{[(phenylformamido)methanethioyl]amino}butyl)thiourea ( 14 ) have been presented. 1-(3-Bromobenzoyl)-3-[2-({[(3-bromophenyl)formamido]methanethioyl}amino)phenyl]thiourea ( 10 ) gave a percentage inhibition of 97.03±0.37% against HIV-1 protease enzyme at a concentration of 100 µM.