title: Developments around the bioactive diketopiperazines: a patent review.
abstract: BACKGROUND
  2,5-Diketopiperazines (DKPs) are cyclic dipeptides from two amino acids with or without further structural modifications in DKP nucleus. These DKPs demonstrated attractive bioactive diversity and potential in drug discovery.
  
  
  METHODS
  This review summarized those bioactive DKPs in patents, and provided the analysis of the structure types (N-substitution, secondary cyclization, isopentenylation, S-substitution, dehydrogenation, and dimerization) and bioactivities including anti-tumor, neuroprotective, immune and metabolic regulatory, oxytocin inhibitory and anti-inflammatory effects, antibiotic activity, PAF inhibition, inhibition of plasminogen activator and T-cell mediated immunity, and insecticidal activity, etc.
  
  
  CONCLUSIONS
  Though DKPs did not show very complicated chemical structures, their rigid structure, chiral nature and varied side chains led to their various medicinal applications.
authors: Ocean University of China, School of Medicine and Pharmacy, Key Laboratory of Marine Drugs, Ministry of Education of China , Qingdao 266003 , People's Republic of China +86 532 82031268 ; +86 532 82031268 ; weimingzhu@ouc.edu.cn.
authors: Yi
authors: Y
authors: Wang
authors: Pei
authors: P
authors: Wang
authors: Hongguang
authors: H
authors: Ma
authors: Weiming
authors: W
authors: Zhu
mesh_terms: D043203:1-Alkyl-2-acetylglycerophosphocholine Esterase / Q000037:antagonists & inhibitors; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D003500:Cyclization; D054659:Diketopiperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans; D007166:Immunosuppressive Agents / Q000138:chemical synthesis / Q000494:pharmacology; D010330:Patents as Topic; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D054659:Diketopiperazines; D007166:Immunosuppressive Agents; D043203:1-Alkyl-2-acetylglycerophosphocholine Esterase