Výsledky vyhledávání - "Claudette Mookherjee"

In vivo activity of an azole series of CCR2 antagonists

Autor: Steve P. Watson, Nicola Bevan, Kitty Moores, Joanne Philp, Claudette Mookherjee, Val Piercy, Mara Zippoli, Chris A. Smethurst, Amanda Emmons, Carl Brooks, Simon Peace, Peter J. Gough

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7252-7255

Optimisation of a series of biaryl sulphonamides resulted in the identification of compound 14 [corrected] which demonstrated dose-dependent and strain-specific inhibition of monocyte recruitment in a thioglycollate-induced peritonitis model of infla

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7a9e166fe0a91c917c4e12740769694
https://doi.org/10.1016/j.bmcl.2012.09.020

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N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators

Autor: Kevin M. Thewlis, Simon E. Ward, Beatrice Oliosi, Mark H Harries, Claudette Mookherjee, Laura Aldegheri

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:7116-7119

A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::453510f26dffd06f49d33b6ffe79f3e0
https://doi.org/10.1016/j.bmcl.2010.09.062

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The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists

Autor: Paul W. Smith, Ian Thomson Forbes, Andrea M. Bradford, Graham Walker, Graham Murkitt, Wyman Paul Adrian, Graeme Irvine Stevenson, Dale James Johnson, Jeannette M. Watson, Steve P. Watson, Adam J. Lucas, Claudette Mookherjee, Fiona Brown, Vincenzo Garzya, Sean Thomas Flynn, Jane Gartlon, Harminder Mudhar

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:5434-5438

A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M 1 agonists. By control of the physicochemical characteristics of the series, particularly the lipophi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59cc3a2c45eff04cbd38a044e1b10476
https://doi.org/10.1016/j.bmcl.2010.07.097

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The PPARδ agonist GW0742X reduces atherosclerosis in LDLR−/− mice

Autor: Claudette Mookherjee, Lisa Patel, Colin N. A. Palmer, Tracey L. Graham, Keith E. Suckling

Publikováno v: Atherosclerosis. 181:29-37

Several lines of evidence suggest a biological role for peroxisome proliferator-activated receptor (PPARdelta) in the pathogenesis of atherosclerosis. Administration of synthetic PPARdelta agonists to obese rhesus monkeys elevates serum high-density

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0a51d28948cb90ad7c4033e11387446
https://doi.org/10.1016/j.atherosclerosis.2004.12.028

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Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators

Publikováno v: Journal of medicinal chemistry. 54(1)

A novel series of AMPAR positive modulators is described that were identified by high throughput screening. The molecules of the series have been optimized from a high quality starting point hit to afford excellent developability, tolerability, and e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f968ae85bfba5e74967880d1ee4d863
https://pubmed.ncbi.nlm.nih.gov/21128618

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Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator

Publikováno v: Journal of medicinal chemistry. 53(15)

A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS pen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::154b627b7254de36c15c9e847ad6636c
https://pubmed.ncbi.nlm.nih.gov/20614889

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Identification of a sulfonamide series of CCR2 antagonists

Autor: Simon Peace, Robert J. Ife, Kitty Moores, Claudette Mookherjee, Joanne Philp, Chris A. Smethurst, Carl Brooks, Mara Zippoli, Steve P. Watson, Val Piercy, Simon Gaines

Publikováno v: Bioorganicmedicinal chemistry letters. 20(13)

A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64cae2e02cf27bec7e4593b9f7adde93
https://pubmed.ncbi.nlm.nih.gov/20627722

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