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Updated: May 8, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines

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Published on: June 23, 2019

Developments around the bioactive diketopiperazines: a patent review.

Yi Wang¹, Pei Wang, Hongguang Ma

¹Ocean 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.

Expert Opinion on Therapeutic Patents

|August 22, 2013

Summary

2,5-Diketopiperazines (DKPs) are cyclic dipeptides with diverse structures and significant potential in drug discovery. This review highlights their various medicinal applications, including anti-tumor and neuroprotective effects.

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A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products

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Published on: October 4, 2019

Area of Science:

Medicinal Chemistry
Organic Chemistry
Drug Discovery

Background:

2,5-Diketopiperazines (DKPs) are cyclic dipeptides derived from amino acids.
DKPs exhibit diverse bioactivities and hold promise for drug discovery.

Purpose of the Study:

To review bioactive DKPs reported in patents.
To analyze DKP structural modifications and their associated bioactivities.

Main Methods:

Literature review of patents concerning DKPs.
Analysis of structural variations (e.g., N-substitution, cyclization, dimerization).
Categorization of bioactivities (e.g., anti-tumor, neuroprotective, anti-inflammatory).

Main Results:

DKPs encompass various structural types, including N-substituted, cyclized, and dimerized forms.
Reported bioactivities include anti-tumor, neuroprotective, immune and metabolic regulation, and anti-inflammatory effects.
Other activities include antibiotic, oxytocin inhibitory, PAF inhibitory, and insecticidal properties.

Conclusions:

Despite relatively simple chemical structures, DKPs possess rigid, chiral frameworks with diverse side chains.
These structural features contribute to their wide range of medicinal applications.