Results 1 to 10 of about 5,442 (212)

Bitter 2,5-Diketopiperazines From Cocoa Activate Human Bitter Taste Receptors. [PDF]

Mol Nutr Food Res
Thermal processing of protein‐containing food leads to the formation of cyclic dipeptides, called 2,5‐diketopiperazines (DKPs). These molecules often contribute to a bitter note in food. Despite the impact of DKPs on the taste of important food groups, their detection by human bitter taste receptors remained enigmatic.
Schaefer S, Luna A, Behrens M.
europepmc   +2 more sources

2,5-Diketopiperazine Derivatives as Potential Anti-Influenza (H5N2) Agents: Synthesis, Biological Evaluation, and Molecular Docking Study

Molecules, 2022
2,5-Diketopiperazine derivatives, consisting of benzylidene and alkylidene substituents at 3 and 6 positions, have been considered as a core structure for their antiviral activities.
Chanakan Winyakul, Weerachai Phutdhawong, Poomipat Tamdee, Jitnapa Sirirak, Thongchai Taechowisan, Waya S. Phutdhawong   +5 more
doaj   +2 more sources

The Chemistry and Pharmacology of the Alkaloid Barettin and Its Analogues from the Marine Sponge Geodia barretti: Progress and Perspectives [PDF]

Marine Drugs
The cold-water siliceous sponge Geodia barretti, largely present in the North Atlantic Ocean, notably around Scandinavian costs, plays important roles in carbon and silicon cycling in the deep-sea.
Christian Bailly
doaj   +2 more sources

Beyond Simple Mimicry: Next-Generation Geometric Architectures and Future Paradigms in Small-Molecule and Macrocyclic Peptidomimetics. [PDF]

Angew Chem Int Ed Engl
Peptide‐to‐Small Molecule Paradigm: Peptidomimetics have evolved from simple mimicry toward drug‐like scaffolds supported by increasing clinical successes. This Perspective highlights the geometric design principles—linear repetition, convergent fusion, and cyclization—defining the next‐generation peptidomimetic architectures capable of targeting ...
Lee J, Son S, Yoo JY, Lee JH, Chun M, Park SB.   +5 more
europepmc   +3 more sources

Four New Pairs of MetO-Containing Diketopiperazine Enantiomers: Isolation, Synthesis and Potential Anti-Parkinson’s Disease Activity [PDF]

Marine Drugs
Four new methionine sulfoxide-containing diketopiperazines, (+)-dysidmetsulfoxide A [(+)-1], (+)-dysidmetsulfoxide B [(+)-2], (+)-dysidmetsulfoxide C [(+)-3] and (−)-dysidmetsulfoxide C [(−)-3], were isolated from the South China Sea sponge Dysidea sp ...
Yu Lei, Zhenyu Yang, Daichun Li, Xiaojian Liao, Chamari Hettiarachchi, Bingxin Zhao, Shihai Xu   +6 more
doaj   +2 more sources

Computational and Cellular Evaluation of the Anti-Melanogenic Potential of Gancidin W: Integrating Network Pharmacology and Free-Energy Analyses [PDF]

Pharmaceuticals
Background/Objectives: Dysregulated melanogenesis underpins numerous hyperpigmentation disorders. Gancidin W, a naturally occurring diketopiperazine with diverse biological activities, has attracted interest as a potential bioactive compound; however ...
Yang Xu, Chang-Gu Hyun
doaj   +2 more sources

A New Prenylated Indole Diketopiperazine Alkaloid From Eurotium cristatum

Molecules, 2014
A new prenylated indole diketopiperazine alkaloid, cristatumin F (1), and four known metabolites, echinulin (2), dehydroechinulin (3), neoechinulin A (4) and variecolorin O (5), were isolated from the crude extract of the fungus Eurotium cristatum.
Xuan Liu, Jintian Tang, Xianwei Zou
exaly   +3 more sources

Unveiling an indole alkaloid diketopiperazine biosynthetic pathway that features a unique stereoisomerase and multifunctional methyltransferase

Nature Communications, 2023
The 2,5-diketopiperazines are a prominent class of bioactive molecules. The nocardioazines are actinomycete natural products that feature a pyrroloindoline diketopiperazine scaffold composed of two D-tryptophan residues functionalized by N- and C ...
Garrett Deletti, Sajan D. Green, Caleb Weber, Kristen N. Patterson, Swapnil S. Joshi, Tushar M. Khopade, Mathew Coban, James Veek-Wilson, Thomas R. Caulfield, Rajesh Viswanathan, Amy L. Lane   +10 more
doaj   +1 more source

Total Synthesis of the Four Stereoisomers of Cyclo(l-Trp-l-Arg) Raises Uncertainty of the Structures of the Natural Products and Invalidates Their Promising Antimicrobial Activities

Molecules, 2022
New therapeutic options to combat the growing incidence of antimicrobial resistance are urgently needed. A 2015 publication reported the isolation and biological evaluation of two diketopiperazine natural products, cyclo(l-Trp-l-Arg) (CDP 2) and cyclo(d ...
Dan Chen, Daniel J. Park, Melissa M. Cadelis, Hana Douafer, Marie Lise Bourguet-Kondracki, Jean Michel Brunel, Brent R. Copp   +6 more
doaj   +1 more source

Analysis of the isomerization of diketopiperazine consisting of proline and aromatic amino acid residues using nuclear magnetic resonance

Analytical Science Advances, 2022
Under different concentrations of the base potassium deuteroxide KOD, the progress of reactions, such as enolization, D‐substitution, isomerization, and conformational changes of diketopiperazine cyclo(L‐Pro‐L‐Xxx) and cyclo(D‐Pro‐L‐Xxx) (Xxx = Phe, Tyr)
Takashi Ishizu, Popuri Sato, Shiori Tsuyama, Ryosuke Nagao, Kanae Fujiki, Amia Yamaji   +5 more
doaj   +1 more source