1. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.

    PLoS ONE 9(5):e97139 (2014) PMID 24858947 PMCID PMC4032240

    Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importance of glucose control. Glucokinase converts gl...
  2. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.

    PLoS ONE 9(5):e97139 (2014) PMID 24858947 PMCID PMC4032240

    Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importance of glucose control. Glucokinase converts gl...
  3. Corrigendum to “The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus” [Bioorg. Med. Chem. Lett. 22 (2012) 7100–7105]

    Bioorganic & Medicinal Chemistry Letters 23(17):5022 (2013)

  4. Corrigendum to “The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus” [Bioorg. Med. Chem. Lett. 22 (2012) 7100–7105]

    Bioorganic & Medicinal Chemistry Letters 23(17):5022 (2013)

  5. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.

    Bioorganic & Medicinal Chemistry Letters 22(23):7100 (2012) PMID 23089526

    Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyrid...
  6. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus

    Bioorganic & Medicinal Chemistry Letters 22(23):7100 (2012)

  7. Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.

    Bioorganic & Medicinal Chemistry Letters 22(2):901 (2012) PMID 22209458

    We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration ...
  8. Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity

    Bioorganic & Medicinal Chemistry Letters 22(2):901 (2012)

    VER-156084 ( 1) shows dose-dependant in vivo FAAH inhibition in an anandamide-loading study in the rat.
  9. Are doctors justified in taking industrial action in defence of their pensions? Yes.

    British Medical Journal (Abstracts) 344:e3242 (2012) PMID 22569869

  10. Are doctors justified in taking industrial action in defence of their pensions? Yes.

    British Medical Journal (Abstracts) 344:e3242 (2012) PMID 22569869

  11. Evidence-based drainage of infected hydronephrosis secondary to ureteric calculi.

    Journal of Endourology 24(2):185 (2010) PMID 20063999

    The obstructed, infected kidney is a urological emergency. It has been accepted that the management of infected hydronephrosis secondary to ureteric stones is through prompt decompression of the collecting system. However, the optimal method of decompression has yet to be established. A PubMed a...
  12. Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas

    Bioorganic & Medicinal Chemistry Letters 19(15):4241 (2009)

  13. An unusual cause of syncope.

    BMJ Case Reports 2009 (2009) PMID 22171228 PMCID PMC3027396

    We present an unusual cause of recurrent syncope in a man in his 50s. He worked as a metallurgist and suffered syncopal events in his poorly ventilated workshop. A detailed history revealed that he used several solvents and chemicals at work and often kept workplace windows closed; he also smoke...
  14. Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas

    Bioorganic & Medicinal Chemistry Letters 19(15):4241 (2009)

  15. The effect of linkage on limits to artificial selection.

    PMID 18976519

  16. Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

    Bioorganic & Medicinal Chemistry Letters 16(5):1353 (2006) PMID 16325401

    Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example ...
  17. Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.

    Bioorganic & Medicinal Chemistry Letters 16(5):1353 (2006) PMID 16325401

    Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example ...
  18. Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: Protein structure-guided design and SAR

    Bioorganic & Medicinal Chemistry Letters 16(5):1353 (2006)

    Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3β (GSK-3β). One example h...
  19. Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

    Bioorganic & Medicinal Chemistry Letters 15(4):863 (2005) PMID 15686876

    The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3beta and o...
  20. Structure-guided design of pyrazolo[1,5-a]pyrimidines as inhibitors of human cyclin-dependent kinase 2.

    Bioorganic & Medicinal Chemistry Letters 15(4):863 (2005) PMID 15686876

    The protein structure guided design of a series of pyrazolo[1,5-a]pyrimidines with high potency for human cyclin-dependent kinase 2 (CDK2) is described. Some examples were shown to inhibit the growth of human colon tumour cells, were equipotent for CDK1 and were selective against GSK-3beta and o...