Title of article :
Synthesis and in vitro antibacterial activity of new oxoethylthio-1,3,4-oxadiazole derivatives
Author/Authors :
Raval, Jignesh P. Ashok Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences - Department of Pharmaceutical Chemistry, India , Akhaja, Tarunkumar N. Ashok Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences - Department of Pharmaceutical Chemistry, India , Jaspara, Dhaval M. Ashok Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences - Department of Pharmaceutical Chemistry, India , Myangar, Kruti N. Ashok Rita Patel Institute of Integrated Study and Research in Biotechnology and Allied Sciences - Department of Pharmaceutical Chemistry, India , Patel, Nilesh H. EMCURE Pharmaceuticals USA INC, USA
Abstract :
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 μM, respectively. All the new compounds were pharmacologically evaluated for their in vitro Antimicrobial activity.
Keywords :
Isonicotinohydrazide , 1,3,4 , oxadiazole , Oxoethylthio , 1,3,4 , oxadiazole , Anti , tubercular , Mycobacterium tuberculosis
Journal title :
Journal of Saudi Chemical Society
Journal title :
Journal of Saudi Chemical Society