Editor-in-Chief
Hatice Kübra Elçioğlu
Vice Editors
Levent Kabasakal
Esra Tatar
Online ISSN
2630-6344
Publisher
Marmara University
Frequency
Bimonthly (Six issues / year)
Abbreviation
J.Res.Pharm.
Former Name
Marmara Pharmaceutical Journal
Journal of Research in Pharmacy
2020 , Vol 24 , Issue 6
Synthesis, characterization, antituberculosis activity and computational studies on novel Schiff bases of 1,3,4-thiadiazole derivatives
A series of novel Schiff bases were designed and synthesized by the condensation of 1,3,4-thiadiazoles
that contain aromatic primary amine and variously substituted benzaldehydes. The synthesized compounds were
screened for their antituberculosis activity against Mycobacterium tuberculosis H37Rv using BACTEC 460 radiometric
system. Among the tested compounds, 2-(4-nitrophenyl)amino-5-[4-(3-(4-phenoxy))benzylideneaminophenyl]-1,3,4-
thiadiazole (3n) showed the highest inhibitory activity (80%). The activities of the newly synthesized Schiff bases
were higher in comparison to those of intermediate products 2-(4-aminophenyl)-5-aryl/alkylamino-1,3,4-
thiadiazoles (2a-l). The computational studies were also performed to estimate drug-like profile of the compounds
by using QikProp analysis.
Keywords :
Schiff bases; 1,3,4-thiadiazoles; antituberculosis activity; Mycobacterium tuberculosis H37Rv; ADME