Theobald CJ

References (3)

Title : The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2 - Blackie_2003_Bioorg.Med.Chem.Lett_13_1067
Author(s) : Blackie JA , Bloomer JC , Brown MJ , Cheng HY , Hammond B , Hickey DM , Ife RJ , Leach CA , Lewis VA , Macphee CH , Milliner KJ , Moores KE , Pinto IL , Smith SA , Stansfield IG , Stanway SJ , Taylor MA , Theobald CJ
Ref : Bioorganic & Medicinal Chemistry Lett , 13 :1067 , 2003
Abstract : Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency. Cyclopentyl fused derivative 21, SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man.
ESTHER : Blackie_2003_Bioorg.Med.Chem.Lett_13_1067
PubMedSearch : Blackie_2003_Bioorg.Med.Chem.Lett_13_1067
PubMedID: 12643913

Title : The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2 - Boyd_2001_Bioorg.Med.Chem.Lett_11_701
Author(s) : Boyd HF , Hammond B , Hickey DM , Ife RJ , Leach CA , Lewis VA , Macphee CH , Milliner KJ , Pinto IL , Smith SA , Stansfield IG , Theobald CJ , Whittaker CM
Ref : Bioorganic & Medicinal Chemistry Lett , 11 :701 , 2001
Abstract : Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A2, has given inhibitors of nanomolar potency and improved physicochemical properties. Compound 23 was identified as a potent, highly water soluble. CNS penetrant inhibitor suitable for intravenous administration.
ESTHER : Boyd_2001_Bioorg.Med.Chem.Lett_11_701
PubMedSearch : Boyd_2001_Bioorg.Med.Chem.Lett_11_701
PubMedID: 11266173

Title : 2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2 - Boyd_2000_Bioorg.Med.Chem.Lett_10_395
Author(s) : Boyd HF , Flynn ST , Hickey DM , Ife RJ , Jones M , Leach CA , Macphee CH , Milliner KJ , Rawlings DA , Slingsby BP , Smith SA , Stansfield IG , Tew DG , Theobald CJ
Ref : Bioorganic & Medicinal Chemistry Lett , 10 :395 , 2000
Abstract : Starting from two weakly active hits from high throughput screening, a novel series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivity for lipoprotein-associated phospholipase A2 has been designed. In contrast to previously known inhibitors, these have been shown to act by a non-covalent and substrate competitive mechanism.
ESTHER : Boyd_2000_Bioorg.Med.Chem.Lett_10_395
PubMedSearch : Boyd_2000_Bioorg.Med.Chem.Lett_10_395
PubMedID: 10714508