This work presents the positive effects of synthesized novel 3-cyano-N-pyridinyl acetamide derivatives on the wound healing process. This work also analyzes their putative action mechanism related to decreased lipid peroxidation and increased antioxidant effects of 3-cyano-N-pyridinyl acetamide derivatives during the wound healing process. We divided 30 Wistar rats into the following groups: control, untreated, and application groups of application groups of 3-cyano-N-pyrdinyl acetamide derivatives (5a-c). Incisional wounds were created in the untreated and application groups. In the application groups, 3-cyano-N-pyrdinyl acetamide derivatives (1 mg/mL) were applied topically to the wounds once a day for 7 days. The wound tissue nitric oxide (NOx), glutathione (GSH), thiobarbituric acid-reactive substances (TBARs), ascorbic acid (AA) levels were measured, and the wound lengths were calculated. The application of these three different substances increased the NOx levels compared to the untreated group. The wound tissue GSH level of the group treated with N-(3-cyano-4-(5-methylfuran-2-yl)-5,6,7,8-tetrahydraquinolin-2-yl)acetamide (5a) was found to be higher than the other groups. 3-Cyano-N-pyridinyl acetamide derivatives effectively reduced tissue lipid peroxidation. Moreover, these substances significantly accelerated wound closure compared to the untreated group. In light of experimental data, newly synthesized 3-cyano-N-pyridinyl acetamide derivatives seem to have the potential to promote both the healing process and antioxidant capacity of wound tissue. This treatment option may be valuable in clinical practice.