Abstract: A series of novel tetrahydrocarboline derivatives was designed and synthesized in order to discover more potent peroxisome proliferator-activated receptor (PPAR) α/γ dual regulators. The structures of these compounds were confirmed by ¹H NMR and HR-MS; their PPAR-regulating activities were evaluated in vitro. Compounds 6h, 6n, 6p and 6q exhibited more potent PPARα agonistic activities than the control drug WY14643, while compounds 6o, 6g, 6i and 6q exhibited more potent PPARγ agonistic activities than the control drug rosiglitazone. Compound 6q was discovered as a potent PPARα/γ dual agonist and deserves further investigation.