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Items: 7


Development and Characterization of a Human Hepatocyte Low Intrinsic Clearance Assay for Use in Drug Discovery.

Lancett P, Williamson B, Barton P, Riley RJ.

Drug Metab Dispos. 2018 Aug;46(8):1169-1178. doi: 10.1124/dmd.118.081596. Epub 2018 Jun 7.


Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors.

Palmer JT, Axford LC, Barker S, Bennett JM, Blair M, Collins I, Davies DT, Ford L, Gannon CT, Lancett P, Logan A, Lunniss CJ, Morton CJ, Offermann DA, Pitt GR, Rao BN, Singh AK, Shukla T, Srivastava A, Stokes NR, Thomaides-Brears HB, Yadav A, Haydon DJ.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4215-22. doi: 10.1016/j.bmcl.2014.07.037. Epub 2014 Jul 19.


Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.

Stokes NR, Baker N, Bennett JM, Chauhan PK, Collins I, Davies DT, Gavade M, Kumar D, Lancett P, Macdonald R, Macleod L, Mahajan A, Mitchell JP, Nayal N, Nayal YN, Pitt GR, Singh M, Yadav A, Srivastava A, Czaplewski LG, Haydon DJ.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):353-9. doi: 10.1016/j.bmcl.2013.11.002. Epub 2013 Nov 13.


Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors.

Axford LC, Agarwal PK, Anderson KH, Andrau LN, Atherall J, Barker S, Bennett JM, Blair M, Collins I, Czaplewski LG, Davies DT, Gannon CT, Kumar D, Lancett P, Logan A, Lunniss CJ, Mitchell DR, Offermann DA, Palmer JT, Palmer N, Pitt GR, Pommier S, Price D, Narasinga Rao B, Saxena R, Shukla T, Singh AK, Singh M, Srivastava A, Steele C, Stokes NR, Thomaides-Brears HB, Tyndall EM, Watson D, Haydon DJ.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6598-603. doi: 10.1016/j.bmcl.2013.10.058. Epub 2013 Nov 4.


Biological evaluation of benzothiazole ethyl urea inhibitors of bacterial type II topoisomerases.

Stokes NR, Thomaides-Brears HB, Barker S, Bennett JM, Berry J, Collins I, Czaplewski LG, Gamble V, Lancett P, Logan A, Lunniss CJ, Peasley H, Pommier S, Price D, Smee C, Haydon DJ.

Antimicrob Agents Chemother. 2013 Dec;57(12):5977-86. doi: 10.1128/AAC.00719-13. Epub 2013 Sep 16.


Creating an antibacterial with in vivo efficacy: synthesis and characterization of potent inhibitors of the bacterial cell division protein FtsZ with improved pharmaceutical properties.

Haydon DJ, Bennett JM, Brown D, Collins I, Galbraith G, Lancett P, Macdonald R, Stokes NR, Chauhan PK, Sutariya JK, Nayal N, Srivastava A, Beanland J, Hall R, Henstock V, Noula C, Rockley C, Czaplewski L.

J Med Chem. 2010 May 27;53(10):3927-36. doi: 10.1021/jm9016366.


DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity.

East SP, White CB, Barker O, Barker S, Bennett J, Brown D, Boyd EA, Brennan C, Chowdhury C, Collins I, Convers-Reignier E, Dymock BW, Fletcher R, Haydon DJ, Gardiner M, Hatcher S, Ingram P, Lancett P, Mortenson P, Papadopoulos K, Smee C, Thomaides-Brears HB, Tye H, Workman J, Czaplewski LG.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):894-9. doi: 10.1016/j.bmcl.2008.11.102. Epub 2008 Dec 3. Erratum in: Bioorg Med Chem Lett. 2009 May 1;19(9):2606.


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