Simone Belshaw | AMiner学者主页

1Discovery Of Selective Cyp11b2 Inhibitors As Potential Treatments For Resistant Hypertension

Scott Hoyt,Whitney Petrilli,Min Park,Jerry Taylor,Clare London,Andrew Cooke,Jiaqiang Cai,Emma Carswell,John Robinson,John Maclean,Lindsay Brown,Simone Belshaw,

2017ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2017）

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2Discovery of Benzimidazole Cyp11b2 Inhibitors with in Vivo Activity in Rhesus Monkeys

Scott B. Hoyt,Min K. Park,Clare London,Yusheng Xiong,Jim Tata,D. Jonathan Bennett,Andrew Cooke,Jiaqiang Cai,Emma Carswell,John Robinson,John MacLean,Lindsay Brown,

We report the discovery of a benzimidazole series of CYP11B2 inhibitors. Hit-to-lead and lead optimization studies identified compounds such as 32, which displays potent CYP11B2 inhibition, high selectivity versus related CYP targets, and good pharmacokinetic properties in rat and rhesus. In a rhesus pharmacodynamic model, 32 produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels.

2015ACS MEDICINAL CHEMISTRY LETTERS（2015）引用：29

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3Discovery Of A Benzimidazole Lead Class: Selective Aldosterone Synthase Inhibitors For The Treatment Of Hypertension

Scott B. Hoyt,Min K. Park,Clare London,Yusheng Xiong,Jim Tata,D. Jonathan Bennett,Andrew Cooke,Jaiqiang Cai,Emma Carswell,John Robinson,John Maclean,Lindsay Brown,

2014ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2014）

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41H-Imidazo[4,5-c]pyridine-4-carbonitrile As Cathepsin S Inhibitors: Separation of Desired Cellular Activity from Undesired Tissue Accumulation Through Optimization of Basic Nitrogen Pka

Wullie Arbuckle,Mark Baugh,Simone Belshaw,D. Jonathan Bennett,John Bruin,Jiaqiang Cai,Kenneth S. Cameron,Chris Claxton,Maureen Dempster,Kathryn Everett,Xavier Fradera,William Hamilton,

Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pk(a) of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pk(a) 6-8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.

2011Bioorganic & Medicinal Chemistry Letters引用：9

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5Trifluoromethylphenyl As P2 for Ketoamide-Based Cathepsin S Inhibitors

Jiaqiang Cai,John Robinson,Simone Belshaw,Kathryn Everett,Xavier Fradera,Mario van Zeeland,Leon van Berkom,Peter van Rijnsbergen,Lucy Popplestone,Mark Baugh,Maureen Dempster,John Bruin,

The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of the torsion angle between the P2 phenyl ring and the attached secondary amide by adding a small Cl, F, or Me group at the 2-position.

2010BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2010）引用：23

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