SYNTHESIS
OF SOME NEW N,N-DISUBSTITUTED DITHIOCARBAMIC ACID 2-(6-ARYLHEXAHYDROPYRIMIDINE-2,4-DION-3-YL)ETHYL
ESTERS AND IN VITRO EVALUATION OF ANTIMICROBIAL ACTIVITIES
Ebubekir SEPTİOĞLU*, Mutlu Dilsiz AYTEMİR*, Ekrem KILIÇ**,
Meral ÖZALP**, Ünsal ÇALIŞ*,o
*Hacettepe University, Faculty of Pharmacy, Department of
Pharmaceutical Chemistry, 06100 Sıhhiye, Ankara, TURKEY.
oCorresponding Author
Summary
In this study, a number of novel dithiocarbamate derivatives
were synthesized for the evaluation of their antimicrobial
activities.
These compounds were originally prepared by the reaction
of potassium salts of N,N-disubstituted dithiocarbamic acids
with 3-(2-chloroethyl)-6-arylhexahydropyrimidine-2,4- diones.
The structures of the synthesized compounds were confirmed
by the spectral data (IR, 1H-NMR) and elemental analysis.
The antimicrobial activities of all of the compounds were
investigated by microdilution broth method using two Gram-positive
(Staphylococcus aureus ATCC 29213, Enterococcus faecalis
ATCC 29212) and two Gram-negative (Escherichia coli ATCC
25922, Pseudomonas aeruginosa ATCC 27853) bacteria and three
fungi (Candida albicans ATCC 90028, Candida krusei ATCC6258,
Candida parapsilosis ATCC 22019). Among the compounds tested
2-[6-(3-chlorophenyl) hexahydropyrimidine-2,4-dione-3-yl]ethyl
morpholine- 4-carbodithioate (compound 7c) showed the most
favorable antibacterial activity (MIC: 16 µg/mL).
Key Words :
Hexahydropyrimidine-2,4-diones, 6-arylhexahydropyrimidine-2,4-diones,
N,N-disubstituted carbamodithioic acid 3-ethyl-6-arylhexahydropyrimidine-2,4-dione
esters, carbamodithioic acid esters, synthesis, antimicrobial
activity, antibacterial activity, antifungal activity. |