Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Pitt Gary Robert William"'
Autor:
Alastair Logan, James T Palmer, B. Narasinga Rao, Neil R. Stokes, Ian Collins, Tarun Shukla, James M. Bennett, Anil K Srivastava, Paul Lancett, Leigh Ford, Pitt Gary Robert William, Helena Thomaides-Brears, Lorraine C. Axford, Stephanie Barker, Anju Yadav, Amit Kumar Singh, David T. Davies, Michael Blair, Craig J. Morton, David J. Haydon, Carlie T. Gannon, Daniel A. Offermann, Christopher J. Lunniss
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4215-4222
A series of dual-targeting, alcohol-containing benzothiazoles has been identified with superior antibacterial activity and drug-like properties. Early lead benzothiazoles containing carboxylic acid moieties showed efficacy in a well-established in vi
Autor:
Ian Collins, Pramod K. Chauhan, Neil R. Stokes, Anu Mahajan, Anil K Srivastava, Mahipal Singh, Anju Yadav, James M. Bennett, Leanne MacLeod, Paul Lancett, Yashodanand Nandan Nayal, David T. Davies, Narendra Nayal, Maruti Gavade, David J. Haydon, Rebecca Macdonald, Nicola Baker, Jeffrey Peter Mitchell, Lloyd George Czaplewski, Pitt Gary Robert William, Dushyant Kumar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:353-359
The design, synthesis and structure-activity relationships of a series of oxazole-benzamide inhibitors of the essential bacterial cell division protein FtsZ are described. Compounds had potent anti-staphylococcal activity and inhibited the cytokinesi
Autor:
Pitt Gary Robert William, Rooker David Philip, Robert Haigh, Andrew M. Penson, Andrzej Roman Batt, André Tartar, Peter A. Robson, Julie E. Trim, Michael Bryan Roe, Yea Christopher Martyn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4585-4589
A library of compounds targeted to the vasopressin/oxytocin family of receptors was screened for activity at a cloned human oxytocin receptor using a reporter gene assay. Potency and selectivity were optimised to afford compound 39, EC50 = 33 nM. Thi
Autor:
Pitt Gary Robert William, Andrzej Roman Batt, Paul D. Jenkins, Graeme Semple, Rooker David Philip, Andrew John Baxter, Doreen M. Ashworth, Peter Hudson, D.Michael Evans, David W.M. Benzies, Franklin Richard Jeremy, Yasuo Isomura, Satoshi Yamamoto, Lucy H. Elliot
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:959-964
Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE
Autor:
Ian Collins, Anil K Srivastava, Piyush K. Agarwal, John Frederick Atherall, Paul Lancett, Amit Kumar Singh, Pitt Gary Robert William, David T. Davies, Laura Andrau, Christopher Richard Steele, James M. Bennett, Stephanie Barker, James T Palmer, Mahipal Singh, Lorraine C. Axford, Carlie T. Gannon, Dushyant Kumar, David J. Haydon, Nicholas John Palmer, Daniel J. Price, Tarun Shukla, Daniel A. Offermann, Edward M. Tyndall, David G. Watson, Michael Blair, Helena Thomaides-Brears, Kelly Helen Anderson, Dale Robert Mitchell, Neil R. Stokes, Lloyd George Czaplewski, Stéphanie Pommier, Christopher J. Lunniss, Alastair Logan, Rashmi Saxena, B. Narasinga Rao
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent acti
Autor:
Y. Isomura, Lucy H. Elliot, Andrew John Baxter, Peter Hudson, S. Yamamoto, Paul D. Jenkins, Andrzej Roman Batt, Doreen M. Ashworth, Graeme Semple, Andrew Sheppard, Michael Szelke, Graham R. Baker, Pitt Gary Robert William, David Michael Evans, David W.M. Benzies, Franklin Richard Jeremy, Rooker David Philip
Publikováno v:
ChemInform. 28
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
Autor:
Pitt, Gary Robert William
Whether your liver is infected with a virus, injured by chemicals or under attack from your own immune system, the damage to your liver is likely to progress in a similar way. In the early stages of liver disease, your liver becomes inflamed. If left
Externí odkaz:
http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.496095
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
Autor:
D. Michael Evans, Pitt Gary Robert William, D. Michael Jones, Javier Sueiras-Diaz, Hoakan Olsson, Doreen Mary Ashworth, John Horton, M. Szelke
Publikováno v:
Immunopharmacology. 32:115-116
Based on a tetrapeptide fragment [Pro387-Ser390] of HK we have developed a series of potent low molecular weight (5-600 Da) inhibitors of PK which are stable to the enzyme. These inhibitors show good selectivity for PK versus tissue kallikrein, throm