Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 23, Issue 11, Pages 1415-1433Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543776.2013.828036
Keywords
2,5-diketopiperazines; bioactivities; chemical structure; patents
Categories
Funding
- 863 Program of China [2013AA092901]
- 973 program of China [2010CB833804]
- Special Fund for Marine Scientific Research in the Public Interest of China [2010418022-3]
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Introduction: 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. Areas covered: 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. Expert opinion: Though DKPs did not show very complicated chemical structures, their rigid structure, chiral nature and varied side chains led to their various medicinal applications.
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