Anahaenopeptins G (1) and H (2) were isolated from the cultured cyanobacterium Oscillatoria agardhii (NIES-595) as potent carboxypeptidase A (CPA) inhibitors. The gross structure of 1 and 2 were established by spectroscopic analysis including the 2D NMR technique and the absolute configurations of 1 and 2 were determined by the spectral and chemical methods. 1 and 2 inhibited CPA with IC50's of 0.0018 and 3.4 microg/mL, respectively.