Design, synthesis, characterization and screening of thiophene derivatives for anti-inflammatory activity
A. Jerad Suresha*, K. Anithab and D. Vinodc
Journal Title:Journal of Chemical, Biological and physical sciences
A promising heterocyclic nucleus (Thiophene) which was prominently proved of exhibiting
different biological activities had been used to prepare a database which was then docked against
CYCLO OXYGENASE-2 for anti- inflammatory activity by using Glide software (Maestro 9.1).Extra
precision (XP) scoring function was utilised to rank order the compounds. The different derivatives of
thiophene were docked to the specific protein target site. The best compounds with top scores were
filtered. The top three compounds were synthesized, recrystallised and purity was conformed by TLC.
The characterization was carried out by UV, IR, NMR and MASS Spectroscopy. All synthesized compounds
were screened for anti -inflammatory activity by invitro Membrane stabilising method. The recorded
values showed significant anti-inflammatory activity compared with standard Diclofenac sodium. Toxicity
of the compounds was evaluated by acute toxicity study.