To synthesise a new series of 5-substituted-1,3,4-Oxadiazol-2yl-4-(morpholin-4yl
sulfonyl)benzyl sulfide and evaluate their antibacterial activity.
Different organic acids were converted consecutively into corresponding esters, hydrazides
and 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-e
). The targets, 6a-e
were synthesized by stirring 4a-e
with 4-(4-(bromomethyl)phenylsulfonyl) morpholine (5
) in the presence of N,N-dimethylformamide
(DMF) and sodium hydride (NaH). All the structures were elucidated by modern spectroscopic
techniques and screened against bacteria using standard procedure and ciprofloxacin drug as positive
The yield of the synthesized compounds (4a-e
) were moderate (65 - 90 %).
had antibacterial activity against
while some had activity against the other bacteria used. One of the compounds,
, exhibited significant activity against all the bacterial strains, i.e.,
(-), P. aeruginosa
(-), B. subtilis
(+) and S. aureus
(+) with MIC (μM) values of 11.01 ±
0.31, 15.37 ± 3.33, 16.11 ± 1.14, 9.70 ± 1.96, 10.01 ± 2.70 and 9.15 ± 0.29, respectively. However,
none of the compounds had any inhibitory activity against any bacteria as high as that of ciprofloxacin.
Five new compounds with antibacterial activities have been synthesized. Their potential
as therapeutic agents is, however, yet to be evaluated.