Výsledky vyhledávání - "Yeeman K. Ramtohul"

Synthesis of α,α-Disubstituted Benzocyclobutane Amino Acids through [2+2] Annulation of Benzyne with Dehydroalanine

Autor: Stephane Ciblat, Audrey Picard, Yeeman K. Ramtohul

Publikováno v: Synlett. 31:507-511

A mild and general method for the synthesis of α,α-disubstituted benzocyclobutane amino acids through a [2+2] annulation of benzyne with dehydroalanine is described. Yields up to 88% of the constrained quaternary amino acids can be obtained and its

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a0ae60fbe405fd4e7ce892b6cc5b8bc2
https://doi.org/10.1055/s-0039-1691572

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Design and synthesis of potent, isoxazole-containing renin inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:2670-2674

The design and optimization of a novel isoxazole S(1) linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin inhibitor even in the presence of human pla

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::adb21bf0f8aa1b021cd6fbd529e12bdc
https://doi.org/10.1016/j.bmcl.2012.03.014

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Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series

Autor: Nicolas Lachance, Zheng Huang, Yeeman K. Ramtohul, Renata Oballa, Hao Wang, Chun Sing Li, Lei Zhang, Sébastien Guiral, Jean-Philippe Leclerc, Jin Wu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:623-627

Elevated levels of stearoyl-CoA desaturase (SCD) activity have been implicated in metabolic disorders such as obesity and type II diabetes. To circumvent skin and eye adverse events observed in rodents with systemically-distributed inhibitors, our re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6319a1d37bfc92fbe16a8a0ad1abd642
https://doi.org/10.1016/j.bmcl.2011.10.070

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Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: From systemic to liver-targeting inhibitors

Autor: Zheng Huang, Jocelyne Guay, Lei Zhang, David A. Powell, Joel Robichaud, Elise Isabel, Jean-Philippe Leclerc, Cameron Black, Serge Leger, Renata Oballa, Sébastien Guiral, Sheldon Crane, Chun Sing Li, Yeeman K. Ramtohul

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:5692-5696

Optimization of a lead thiazole amide MF-152 led to the identification of potent bicyclic heteroaryl SCD1 inhibitors with good mouse pharmacokinetic profiles. In a view to target the liver for efficacy and to avoid SCD1 inhibition in the skin and eye

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13063d6a227e069320283ad317f85e23
https://doi.org/10.1016/j.bmcl.2011.08.037

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2-Aryl benzimidazoles: Human SCD1-specific stearoyl coenzyme-A desaturase inhibitors

Autor: Yeeman K. Ramtohul, Sathesh Bhat, Lei Zhang, Zheng Huang, Kathryn Skorey, Paul Tawa, Jean-Pierre Falgueyret, David A. Powell, Renata Oballa, Sébastien Guiral, Marie-Eve Lebrun

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:6366-6369

A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. The compounds possess suitable cellular activity and pharmacokinetic properties which render them capable

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a093718a0739afc431d0c82cbad18ff
https://doi.org/10.1016/j.bmcl.2010.09.094

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SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors

Autor: Sheldon Crane, Lei Zhang, Jocelyne Guay, Sébastien Guiral, Chun Sing Li, Cameron Black, Lijing Xu, Yeeman K. Ramtohul, Renata Oballa, Zheng Huang, Chi-Chung Chan

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1593-1597

Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Compound 3j, a potent SCD inhibitor (human HepG2 IC50 = 1 nM) was identified from the optimization of a lead th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a8c151b313856c738d0112e7e037e0d
https://doi.org/10.1016/j.bmcl.2010.01.083

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A Multiplexed Cell Assay in HepG2 Cells for the Identification of Delta-5, Delta-6, and Delta-9 Desaturase and Elongase Inhibitors

Autor: Jocelyne Guay, Lei Zhang, Hao Wang, Yeeman K. Ramtohul, Sébastien Gagné, Zheng Huang, Angela Styhler

Publikováno v: SLAS Discovery. 15:169-176

A multiplexed cell assay has been optimized to measure the activities of fatty acyl-CoA elongase, delta-5 desaturase (Delta5D), delta-6 desaturase (Delta6D), and delta-9 desaturase (Delta9D) together using (14)C-labeled tracers in HepG2 cells, which

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea7d49eefbb4cc32f5b31cc225b30636
https://doi.org/10.1177/1087057109356208

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Thiazole analog as stearoyl-CoA desaturase 1 inhibitor

Autor: Zheng Huang, Lei Zhang, Liette Belair, Wayne Sturkenboom, Chun Sing Li, Yeeman K. Ramtohul, Jocelyne Guay, Renata Murgasva

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:5214-5217

SCD1 inhibition may represent a novel treatment for obesity, type-2 diabetes and related metabolic disorders. A prototype thiazole amide analog 13 (MF-152) was identified as an excellent tool in the study of SCD biology in animals.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::348930203ee59f6b0f5762c823d46d85
https://doi.org/10.1016/j.bmcl.2009.07.015

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