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The engine of chemical biology
Medicinal chemistry
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Whether making chemical probes or new drugs, managing efficient chemistry programmes is a key component of success. Effectively bridging the disciplines of biology & chemistry is the core of CBVs Â
service. Providing project review & mentoring to maximise progress versus activity; to present alternative views to work through & around problems & to support project outsourcing & progression into scale-up, preclinical development & beyond, CBVÂ can add value & pace to your portfolio.
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Lloyd Czaplewski, a biologist by training and a Fellow of the Royal Society of Chemistry , recognising his ability to work across disciplines, has a strong track record of delivering successful projects, generating & managing intellectual property. and has worked with a variety of synthetic and natural product scaffolds including imidazolopyridines, triazolopyridines, benzothiazoles, benzamides, aminocoumarins & various lactams. He has directed projects based on structure-based design, traditional medicinal chemistry and novel approaches driven by neural net technology. His inputs including iterative compound design, route development to the kilo scale & selection of service providers & collaborators have had direct impact on project progression and delivery.
Reference Link:
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Haydon DJ, Stokes NR, Ure R, Galbraith G, Bennett JM, Brown D, Baker PJ, Barynin VV, Rice DW, Sedelnikova SE, Heal JR, Sheridan JM, Aiwale ST, Chauhan PK, Srivastava A, Taneja A, Collins I, Errington J, Czaplewski LG. A novel inhibitor of FtsZ with potent and selective anti-staphylococcal activity. Science 321, 1673-1675.
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Czaplewski LG, Collins I, Boyd EA, Brown D, East SP, Gardiner M, Fletcher R, Haydon DJ, Henstock V, Ingram P, Jones C, Noula C, Kennison L, Rockley C, Rose V, Thomaides HB, Ure R, Whittaker M Stokes NR. Antibacterial alkyloxybenzamide inhibitors of the essential bacterial cell division protein FtsZ. Bioorganic Medicinal Chemistry Letters 2009;19(2):524-7.
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East SP. Bantry White C, Barker O, Barker S, Bennett J, Brown D, Boyd EA, Brennamn C, Chowdhury C, Collins I, Covers-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. (2009) DNA gyrase (GyrB)/Topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity. Bioorganic Medicinal Chemistry Letters 19, 894-899.
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Haydon DJ, , Bennett JM, Brown D, Collins I, Lancett P, Stokes NR, Macdonald R, Chauhan PK, Sutariya JK, Nayal N, Srivastava A, Beanland J, Hall R, Henstock V, Noula C, Rockley C, Czaplewski LG. (2010). Building an antibacterial with in vivo efficacy: synthesis and characterisation of potent inhibitors of the bacterial cell-division protein FtsZ with improved pharmaceutical properties. J. Med Chem. 53, 3927-3936.
Compounds selected from published patents eg US 2009/0197877 & East et al
