The reaction of substituted 3-(4-nitrobenzoyl)hydrazonofuran-2(3 H )-ones with primary alcohols gave the corresponding 2-[2-(4-nitrobenzoyl)hydrazono]-4-oxobutanoates. Evaluation of anti-inflammatory activity and acute toxicity of the synthesized compounds revealed their pronounced anti-inflammatory effect. According to the toxicity classification the synthesized 2-[2-(4-nitrobenzoyl)hydrazono]-4-oxobutanoates belong to toxicity class V of practically nontoxic substances.