Search Results - "HICKEY, Deirdre M. B"
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The discovery of GSK221149A: A potent and selective oxytocin antagonist
Published in Bioorganic & medicinal chemistry (2008)“…Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has…”
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Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor
Published in Bioorganic & medicinal chemistry letters (15-03-2007)“…The discovery, solid phase synthesis and structure–activity relationships of novel carboxylic acid agonists for the GPR40 receptor are described. The…”
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Synthesis and properties of macrolones characterized by two ether bonds in the linker
Published in Bioorganic & medicinal chemistry (01-09-2010)“…In this paper synthesis of macrolones 1– 18 starting from azithromycin is reported. Two key steps in the construction of the linker between macrolide and…”
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Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat
Published in American journal of physiology. Regulatory, integrative and comparative physiology (01-07-2007)“…Spontaneous and induced uterine contractions in the rat were found to be inhibited by a novel and selective oxytocin receptor antagonist GSK221149A…”
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5-Aryl-pyrazolo[3,4- b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)
Published in Bioorganic & medicinal chemistry letters (05-05-2003)“…A novel series of pyrazolo[3,4- b]pyridines has been identified that are potent inhibitors of glycogen synthase kinase-3 (GSK-3). A novel series of…”
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The identification of clinical candidate SB-480848 : A potent inhibitor of lipoprotein-associated phospholipase A2
Published in Bioorganic & medicinal chemistry letters (24-03-2003)“…Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated…”
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5-Aryl-pyrazolo[3,4- b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)
Published in Bioorganic & medicinal chemistry letters (05-05-2003)“…Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4- b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition…”
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Inhibitors of CoA-independent transacylase block the movement of arachidonate into 1-ether-linked phospholipids of human neutrophils
Published in Biochemistry (Easton) (25-04-1995)“…The enzyme CoA-independent transacylase (CoA-IT) has been proposed to mediate the movement of arachidonate between phospholipid subclasses and influence the…”
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Lipoprotein-associated phospholipase A2, platelet-activating factor acetylhydrolase, generates two bioactive products during the oxidation of low-density lipoprotein: use of a novel inhibitor
Published in Biochemical journal (01-03-1999)“…A novel and potent azetidinone inhibitor of the lipoprotein-associated phospholipase A2 (Lp-PLA2), i.e. platelet-activating factor acetylhydrolase, is…”
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Potent, orally active inhibitors of lipoprotein-associated phospholipase A2: 1-(biphenylmethylamidoalkyl)-pyrimidones
Published in Bioorganic & medicinal chemistry letters (07-01-2002)Get full text
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Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones
Published in Bioorganic & medicinal chemistry letters (07-01-2002)“…A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A(2) with…”
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N-1 substituted pyrimidin-4-ones: Novel, orally active inhibitors of lipoprotein-associated phospholipase A2
Published in Bioorganic & medicinal chemistry letters (20-11-2000)“…From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human…”
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1-(Arylpiperazinylamidoalkyl)-pyrimidones : Orally active inhibitors of lipoprotein-associated phospholipase A2
Published in Bioorganic & medicinal chemistry letters (23-07-2001)Get full text
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The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man
Published in Bioorganic & medicinal chemistry letters (16-09-2002)“…The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant…”
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The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2
Published in Bioorganic & medicinal chemistry letters (12-03-2001)“…Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase…”
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Lipoprotein-associated PLA2 inhibition : a novel, non-lipid lowering strategy for atherosclerosis therapy
Published in Farmaco (Società chimica italiana : 1989) (01-03-2001)“…Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a serine lipase that is associated with low density lipoprotein (LDL) in human plasma. Substrates include…”
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BASE INDUCED REACTION OF AN AZETIDIN-2-ONE: FORMATION OF A NOVEL [1,4]-DIAZEPINEDIONE
Published in Synthetic communications (01-01-2001)“…A mild, base mediated conversion of an azetidin-2-one to the [1,4]-diazapinedione system is reported and a putative mechanistic pathway is proposed…”
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SK&F 97426-A: a novel bile acid sequestrant with higher affinities and slower dissociation rates for bile acids in vitro than cholestyramine
Published in Journal of pharmaceutical sciences (01-01-1997)“…SK&F 97426-A is a novel bile acid sequestrant that is threefold more potent than cholestyramine at increasing bile acid excretion in the hamster. SK&F 97426-A…”
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