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Concept

Prodrug

Related publications (9)

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK

Stewart Cole

Mycobacterium tuberculosis, the etiological agent of the infectious disease tuberculosis, kills approximately 1.5 million people annually, while the spread of multidrug-resistant strains is of great global concern. Thus, continuous efforts to identify new ...

Nature Research2018

A Smart Europium-Ruthenium Complex as Anticancer Prodrug: Controllable Drug Release and Real-Time Monitoring under Different Light Excitations

Jean-Claude Bünzli

A unique, dual-function, photoactivatable anticancer prodrug, RuEuL, has been tailored that features a ruthenium(II) complex linked to a cyclen-europium chelate via a pi-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes ph ...

Amer Chemical Soc2017

p,t-[Ru(CO)(PR3)(tren)](2+) [R=Ph or p-tol; tren=tris(2-aminoethyl)amine], Ru(II) complexes bearing a simple tripodal tetradentate amine: synthesis, characterization, and antimicrobial activity

Paul Joseph Dyson, Rosario Scopelliti, Francisco Dinis Fagundes

Complexes with general formula p,t-[Ru(CO)(PR3)(tren)]X-2 [R=Ph (1) or p-tol (2); tren=tris(2-aminoethyl)amine; X=Cl- or PF6-] were prepared from [RuCl2(CO)(dmf)(PR3)] by direct reaction with tren. The complexes were fully characterized by NMR (H-1, P-31{H ...

Taylor & Francis2016

Inhibition of Sepiapterin Reductase through Formation of a Ternary Complex with Sulfasalazine or other Sulfa Drugs and NADP+

Miriam Grønlund Pedersen

The mechanism of action of sulfasalazine, an anti-inflammatory drug used against inflammatory bowel diseases and rheumatoid arthritis is, despite its medical importance, still not well understood. Recently, it was shown that sulfasalazine and its metabolit ...

EPFL2014

Extracellular matrix binding mixed micelles for drug delivery applications

Jeffrey Alan Hubbell, Jutta Christine Wandrey, Davide Demurtas

Received 5 January 2009 Accepted 22 March 2009 Available online 27 March 2009 Keywords: Mixed micelles Drug delivery Block copolymers Sirolimus Extracellular matrix We present the formation of collagen-binding mixed micelles and their potential suitability ...

2009

Nouvelles approches synthétiques de prodrogues de cyclosporine A et d'analogues antiviraux

Jérémy Bérard

The cyclosporins comprise a family of cyclic 11-peptides containing seven N-methylated, hydrophobic amino acids. Cyclosporine A (CsA) representing the major member of this family is widely used as immunosuppressive agent in organ transplantations. The biol ...

EPFL2008

Water-soluble prodrugs of cyclosporine A with tailored conversion rates

Arnaud Hamel

A novel type of water-soluble prodrugs of cyclosporine A (CsA) is described, featuring a modular system of an enzyme-cleavable group, a solubilizing moiety and a chemodegradable spacer attached to the hydroxyl function of (4R)-4-[(E)-2-butenyl]-4-,N-dimeth ...

2005

Cyclosporin analogues : potential HIV inhibitors and water-soluble prodrug systems

Arnaud Hamel

Cyclosporins are a family of hydrophobic cyclic undecapeptides produced by the fungus Tolypocladium niveum. The main metabolite cyclosporin A (CsA, see Scheme, R = R' = H) is the first line drug currently used to prevent rejection of organ transplants. Its ...

EPFL2005

Synthèse, structure et propriétés physicochimiques des cyclosporines

Olivier Turpin

Cyclosporin is a cyclic undecapeptide useful as drug for organ transplantation due to its immunosuppressive properties. Ten years ago, an anti-viral activity was discovered, incompatible with immunosuppression. These two activities originate in the presenc ...

EPFL2004