Nineteen new compounds containing tetrazole and/or cyanamide moiety have been designed and synthesised. Their structures were confirmed using spectroscopic methods and elemental analyses. Anti-inflammatory activity for all the synthesised compounds was evaluated
in vivo
. The most active compounds
4c
,
5a
,
5d–f
,
8a
and
b
and
9a
and
b
were further investigated for their ulcerogenic liability and analgesic activity. Pyrazoline derivatives
9b
and
8b
bearing trimethoxyphenyl part and SO
2
NH
2
or SO
2
Me pharmacophore showed equal or nearly the same ulcerogenic liability (UI: 0.5, 0.75, respectively), to celecoxib (UI: 0.50). Most of tested compounds showed potent central and/or peripheral analgesic activities. Histopathological investigations were done to evaluate test compounds effect on rat's gastric tissue. The obtained results were in consistent with the
in vitro
data on COX evaluation. Docking study was also done for all the target compounds inside COX-2-active site.