Synthesis and biological evaluation of novel PDMP analogues

Bioorganic & Medicinal Chemistry
Ulrik HillaertS Van Calenbergh

Abstract

A new series of hybrid PDMP analogues, based both on PDMP and styryl analogues of natural ceramide, has been synthesized from D-serine. The synthetic route was developed such that future introduction of different aryl groups is straightforward. Biological evaluation, both in vitro on rat liver Golgi fractions as well as in HEK-293 and COS-7 cells, revealed two lead compounds with comparable inhibitory potency as PDMP, which could be elaborated to more potent inhibitors.

References

Jan 1, 1992·Methods in Enzymology·A H Futerman, R E Pagano
Apr 1, 1980·Chemistry and Physics of Lipids·R R Vunnam, N S Radin
May 1, 1983·Proceedings of the National Academy of Sciences of the United States of America·N G Lipsky, R E Pagano
Apr 1, 1996·Glycoconjugate Journal·N S Radin
Jul 20, 1999·Journal of Medicinal Chemistry·I Van OvermeireP Herdewijn
May 16, 2002·The Journal of Biological Chemistry·Sarah Spiegel, Sheldon Milstien
May 16, 2002·The Journal of Biological Chemistry·Yusuf A Hannun, Lina M Obeid
May 16, 2002·The Journal of Biological Chemistry·Alfred H Merrill
May 16, 2002·The Journal of Biological Chemistry·Gerrit van Meer, Quirine Lisman
Apr 5, 2003·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Rosaria Buccoliero, Anthony H Futerman
Aug 1, 1959·Canadian Journal of Biochemistry and Physiology·E G BLIGH, W J DYER
Mar 10, 2004·Bioorganic & Medicinal Chemistry Letters·Jacob P SlavishRobin Polt
Jul 3, 2004·Nature Reviews. Molecular Cell Biology·Anthony H Futerman, Gerrit van Meer
Aug 4, 2004·EMBO Reports·Anthony H Futerman, Yusuf A Hannun
Aug 6, 2004·The Journal of Biological Chemistry·Akira AbeJames A Shayman
Dec 2, 2004·Brain Research. Brain Research Reviews·Laura Colombaioni, Mercedes Garcia-Gil

❮ Previous
Next ❯

Citations

Aug 8, 2013·Future Medicinal Chemistry·Jiawang LiuMaryam Foroozesh
Jun 1, 2007·Expert Opinion on Drug Discovery·Norman S Radin
Oct 29, 2009·Angewandte Chemie·Tom WennekesJohannes M F G Aerts
Jun 6, 2008·Bioorganic & Medicinal Chemistry Letters·Karin ThevissenIsabelle E J A François
Oct 24, 2015·ChemMedChem·Richard J B H N van den BergJohannes M F G Aerts
Jan 26, 2007·ChemMedChem·Antonio DelgadoGemma Fabriás
Sep 6, 2011·Organic Letters·María MorenoAntoni Riera
Mar 20, 2014·The Journal of Organic Chemistry·Anna Alcaide, Amadeu Llebaria
Feb 10, 2011·ACS Medicinal Chemistry Letters·Amar GhisaidoobeRichard J B H N van den Berg

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Clinical and Experimental Dermatology
D J BibelH R Shinefield
Bioorganic & Medicinal Chemistry Letters
Teiichi MurakamiMasazumi Nishikawa
© 2022 Meta ULC. All rights reserved