The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists

JA Jablonowski, CA Grice, W Chai… - Journal of medicinal …, 2003 - ACS Publications
Following the discovery of the human histamine H 4 receptor, a high throughput screen of our
corporate compound collection identified compound 6 as a potential lead. Investigation of …

Identification of ABX-1431, a selective inhibitor of monoacylglycerol lipase and clinical candidate for treatment of neurological disorders

…, RAB Ezekowitz, GP O'Neill, CA Grice - Journal of medicinal …, 2018 - ACS Publications
The serine hydrolase monoacylglycerol lipase (MGLL) converts the endogenous cannabinoid
receptor agonist 2-arachidonoylglycerol (2-AG) and other monoacylglycerols into fatty …

Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides:  Potent Human Histamine H4 Antagonists

…, H Cai, W Chai, CA Dvorak, CA Grice… - Journal of medicinal …, 2005 - ACS Publications
Three series of H 4 receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones,
have been synthesized and their structure−activity relationships evaluated for …

Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis

…, ST Motley, KJ Shaw, R Wolin, CA Grice… - Bioorganic & medicinal …, 2007 - Elsevier
In an attempt to search for a new class of antibacterial agents, we have discovered a series
of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram-…

Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton

…, F Coles, JP Riley, KN Williams, CA Grice… - … of Pharmacology and …, 2007 - ASPET
Leukotriene A 4 hydrolase (LTA 4 H) catalyzes production of the proinflammatory lipid
mediator, leukotriene (LT) B 4 , which is implicated in a number of inflammatory diseases. We …

Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains

…, RM Goldschmidt, KJ Shaw, TK Jones, CA Grice - Bioorganic & medicinal …, 2007 - Elsevier
We have previously reported a novel class of tetrahydroindazoles that display potency against
a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type …

Identification of a Potent, Selective, and Orally Active Leukotriene A4 Hydrolase Inhibitor with Anti-Inflammatory Activity

CA Grice, KL Tays, BM Savall, J Wei… - Journal of medicinal …, 2008 - ACS Publications
LTA 4 H is a ubiquitously distributed 69 kDa zinc-containing cytosolic enzyme with both
hydrolase and aminopeptidase activity. As a hydrolase, LTA 4 H stereospecifically catalyzes the …

Monoacylglycerol lipase inhibition in human and rodent systems supports clinical evaluation of endocannabinoid modulators

…, ML Cunningham, TK Jones, IP Fraser, CA Grice… - … of Pharmacology and …, 2018 - ASPET
Monoacylglycerol lipase (MGLL) is the primary degradative enzyme for the endocannabinoid
2-arachidonoylglycerol (2-AG). The first MGLL inhibitors have recently entered clinical …

Discovery of a novel series of selective HCN1 blockers

…, N Hawryluk, JG Breitenbucher, CA Grice - Bioorganic & medicinal …, 2011 - Elsevier
The discovery of a series of novel, potent, and selective blockers of the cyclic nucleotide-modulated
channel HCN1 is disclosed. Here we report an SAR study around a series of …

Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors

…, RL Thurmond, S Sun, L Karlsson, CA Grice… - Bioorganic & Medicinal …, 2010 - Elsevier
A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide
functional groups were prepared with the goal of improving upon the cellular activity of …