Synthesis and in vitro antibacterial activity of new oxoethylthio-1, 3, 4-oxadiazole derivatives

Abstract EN

In the present investigation, a series of 2(4-pyridyl)-5[(aryl/heteroarylamino)-1-oxoethyl] thio-1, 3, 4-oxadiazole were synthesized using isonicotinohydrazide and substituted aryl / heteroaryl amines using pyridine as solvent.

Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system.

Among the synthesized compounds, compounds 2(4-pyridyl)-5((2-nitrophenylamino)- 1-oxoethyl)thio-1, 3, 4-oxadiazole (5e), 2(4-pyridyl)-5((4-nitrophenylamino)-1-oxoethyl)thio- 1, 3, 4-oxadiazole (5g) and 2(4-pyridyl)-5((2-pyrrolylamino)-1-oxoethyl)thio-1, 3, 4-oxadiazole (5k) produced highest efficacy and exhibited > 90 % inhibition at a concentration of 0.0077, 0.0052 and 0.0089 lM, respectively.

All the new compounds were pharmacologically evaluated for their in vitro Antimicrobial activity.