Background: In our previous work, several piperazine derived bis(dialkylaminethiocarbonyl)
disulfides and disulfide esters of dithiocarbamic acid have been synthesized and
evaluated for their spermicidal and microbicidal efficacy. These studies have provided some promising
compounds for developing a dually active vaginal microbicidal contraceptive which is under
Objective: The main objective of this study was the design synthesis and biological evaluation of
bis(dialkylaminethiocarbonyl) disulfides (4–15) and 2,2’-disulfanediylbis (3-(substituted-1-yl)
propane-2,1-diyl) disubstituted-1-carbodithioates (19-28) as non-surfactant molecules capable of
eliminating Trichomonas vaginalis as well as irreversibly immobilizing 100% human sperm
Method: Spermicidal, anti-trichomonas, cytotoxicity and biocompatibility study of the synthesized
compounds was done as per the reported methodologies.
Result: Among bis(dialkylaminethiocarbonyl) disulfides (4-15, Table 1), compound 4 (MEC 0.02
mM) was found to be the most desirable for spermicidal activity as it was 40 times more active
than Nonoxynol-9 (N-9), and also active against Trichomonas vaginalis (MIC 0.02 &1.10 mM). 2,
2’-disulfanediylbis (3-(substituted- 1-yl) propane-2, 1-diyl) disubstituted-1-carbodithioates (19-28,
Table 2), and compounds (19, 22, 23, and 24 MEC 0.05 mM) were sixteen times more active than
N-9 with promising Trichomonacidal activity.
Conclusion: This study suggested that the disulfide linkage alone and dithiocarbamate along with
disulfide group within the same chemical entity impart the desired multiple activities of compounds.