Synthesis, Characterization and Biological Activity of Some Dithiourea Derivatives

Abstract

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.

Keywords

• dithiourea
• cytotoxicity
• hiv-1 protease inhibition
• plasmodium falciparum activity
• trypanosoma brucei activity