Herein we report the biological evaluation of new hybrids of 1,2,3,4-tetrahydroisoquinoline with ibuprofen. The hybrids are screened for their in vitro inhibition of albumin denaturation, antioxidant, and antitryptic activity. The tested compounds have shown significant results. The lipophilicity was established using both reversed-phase thin layer chromatography and in silico calculations