Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1

Autor: Teresa Brooks, Richard Faint, Sukhjit Sohal, Adrian Folkes, Golec Julian M C, Peter Charlton, Michael Bryan Roe

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:2589-2592

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC 50 =0.2 μM. The synthesis and SAR of these compounds are described

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::766e7b20a095c6f68d57e64459468757
https://doi.org/10.1016/s0960-894x(01)00508-x

ChemInform Abstract: Reversal of P-Glycoprotein Mediated Multidrug Resistance by Novel Anthranilamide Derivatives

Autor: Lal Chima, Pretswell Ian Andrew, Michael Bryan Roe, Wendy Dangerfield, Adrian Folkes, Ashworth Philip Anthony, Julie Elizabeth Brumwell, Hamish Ryder, Peter Charlton, Sukhjit Hunjan

Publikováno v: ChemInform. 30

We have synthesised and evaluated a series of anthranilamide based modulators of P-glycoprotein. These studies have identified XR9576(2), a potent inhibitor of P-glycoprotein in vitro and in vivo. The general synthesis and the SAR of these compounds

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1a42841f83497663539abd3bae642826
https://doi.org/10.1002/chin.199926274

New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists

Autor: James Barnett, Andy Sheppard, Andy J Baxter, Robert Haigh, Doreen Mary Ashworth, John Horton, Janice D Broadbridge, Michael Bryan Roe, Christine Elizabeth Allan, Richard Jeremy Franklin, Sally L Hampton, Peter A. Robson, Graeme San Diego Semple, Andy M Penson, Pierre Riviere, Rooker David Philip, Peter Hudson, Pitt Gary Robert William, Yea Christopher Martyn, Paul David Jenkins

Publikováno v: Journal of medicinal chemistry. 51(24)

Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desir

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5811e23f6391edc618cca30c4ed2af9b
https://pubmed.ncbi.nlm.nih.gov/19053774

Solid and solution phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728

Autor: Nicolas Willand, Jean-Claude Gesquiere, André Tartar, Michael Bryan Roe, Jurgen Joossens, D.Michael Evans

Publikováno v: Tetrahedron
Tetrahedron, Elsevier, 2002, 58, pp.5741-5746. ⟨10.1016/S0040-4020(02)00536-7⟩
Tetrahedron, 2002, 58, pp.5741-5746. ⟨10.1016/S0040-4020(02)00536-7⟩

DPP-IV inhibitors have been suggested as potential new treatments for type-II diabetes and 2-cyanopyrrolidides have been reported as potent DPP-IV inhibitors. Alternative synthetic approaches to one such compound, NVP-DPP728, are investigated here. O

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4590918b7dcbfada999969bc47798906
https://www.hal.inserm.fr/inserm-00110441/document

Nonpeptide oxytocin agonists

Autor: Celine Marguerite Simone Heeney, Peter A. Robson, Regent Laporte, Robert Haigh, Pierre Broqua, Andrzej Roman Batt, André Tartar, Peter Hudson, Rooker David Philip, Chris Yea, Michael Bryan Roe, Pitt Gary Robert William, Doreen Mary Ashworth, Andrew John Baxter, Andrew M. Penson

Publikováno v: Drugs of the Future. 31:345

Oxytocin is a neurohypophyseal hormone that acts at the oxytocin receptor localized both peripherally and centrally and is particularly highly expressed in the pregnant human myometrium. Synthetic oxytocin has long been used to induce labor and oxyto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7c9a35c1fd8fb3d616cdec730b4ad6b8
https://doi.org/10.1358/dof.2006.031.04.980655