Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Laufersweiler Michael Christopher"'
Publikováno v:
Regulatory toxicology and pharmacology : RTP. 127
The Threshold of Toxicological Concern (TTC) for non-genotoxic substances, a risk assessment tool to establish safe exposure levels for chemicals with insufficient toxicological data, is based on the 5th percentile of cumulated distributions of Point
Autor:
Atish Patel, Laufersweiler Michael Christopher, Susan P. Felter, A.M. Api, Jane Rose, Kaushal Joshi
Publikováno v:
Regulatory toxicology and pharmacology : RTP. 116
The use of threshold of toxicological concern (TTC) supports the safety assessment of exposure to low levels of chemicals when toxicity data are limited. The Research Institute for Fragrance Materials (RIFM) delivers safety assessments for fragrance
Publikováno v:
Regulatory toxicology and pharmacology : RTP. 92
Structure activity relationships (SAR) and read-across are widely used animal alternative approaches for filling toxicological data gaps. A framework describing the use of expert judgment in evaluating analogs for SAR has been published and widely ci
Autor:
Jorge M. Naciff, Cathy Lester, Karen Blackburn, Laufersweiler Michael Christopher, Shengde Wu, George P. Daston, Joan Fisher
Publikováno v:
Chemical Research in Toxicology. 26:1840-1861
Developmental and reproductive toxicity (DART) end points are important hazard end points that need to be addressed in the risk assessment of chemicals to determine whether or not they are the critical effects in the overall risk assessment. These ha
Autor:
Karen Blackburn, George P. Daston, Gregory J. Carr, Alison Willis, Irene M. Baskerville-Abraham, Anthony R. Scialli, Andrew Maier, Bernard Gadagbui, Susan P. Felter, Laufersweiler Michael Christopher
Publikováno v:
Regulatory Toxicology and Pharmacology. 62:160-182
In the absence of toxicological data on a chemical, the threshold of toxicological concern (TTC) approach provides a system to estimate a conservative exposure below which there is a low probability of risk for adverse health effects. The original to
Autor:
Steven V. O’Neil, Biswanath De, Christopher D. Ellis, Charles A. Cruze, Mark William Baize, Thomas P. Demuth, Laufersweiler Michael Christopher, Maria Buchalova, Wei Lu, Richard L. Wang, Marina Belkin, Amy N. Fancher, Maureen K. Suchanek, John August Wos, David Lindsey Soper, William P. Schwecke, Kofi A. Oppong, Yili Wang
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:1311-1322
Peptidomimetic compounds possessing a caprolactam ring constraint were prepared and evaluated as interleukin-1beta converting enzyme (ICE) inhibitors. The caprolactam ring was used to constrain the P3 region of our inhibitors. This strategy proved to
Autor:
Thomas P. Demuth, Maria E. Petrey, Maria Kontoyianni, Laufersweiler Michael Christopher, Matthew Pokross, Yili Wang, R.L. Walter, Jeffrey Tupper Roesgen, Eloise C. Richardson, Artem G. Evdokimov, Marlene Mekel, Georgios Sabatakos, Corey R. Hopkins, Steven V. O’Neil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5659-5663
The synthesis and structure-activity relationships of a novel series of N-sulfonyl-2-indole carboxamides that bind to peroxisome proliferator-activated receptor gamma (PPAR-gamma) are reported. Chemical optimization of the series led to the identific
Autor:
David Lindsey Soper, John August Wos, Kofi A. Oppong, Richard L. Wang, Biswanath De, Laufersweiler Michael Christopher, Thomas P. Demuth, Wei Lu, Steven V. O’Neil, Maureen K. Suchanek, Christopher D. Ellis, Amy N. Fancher, Yili Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4728-4732
A series of monocyclic thiazepine inhibitors of interleukin-1β converting enzyme (ICE) were synthesized in eight steps from commercially available intermediates. In vitro biological evaluation showed the thiazepines to be moderately potent ICE inhib
Autor:
Amy N. Fancher, Mark William Baize, Thomas P. Demuth, Kofi A. Oppong, Yili Wang, David Lindsey Soper, Steven V. O’Neil, Richard L. Wang, Wei Lu, Christopher D. Ellis, Maureen K. Suchanek, John August Wos, Gregory K. Bosch, Laufersweiler Michael Christopher, Biswanath De
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5434-5438
Two novel 8,6-fused bicyclic peptidomimetic ring systems were synthesized utilizing olefin metathesis as the key reaction for the formation of the eight-membered ring. Both peptidomimetic scaffolds were further elaborated into potent ICE inhibitors,
Autor:
Mark William Baize, Thomas P. Demuth, Yili Wang, Steven V. O’Neil, Maureen K. Suchanek, John August Wos, David Lindsey Soper, Wei Lu, Laufersweiler Michael Christopher, Kofi A. Oppong, Christopher D. Ellis, Amy N. Fancher, Richard L. Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4322-4326
The application of a tricyclic pyrrolopyrimidinone scaffold for the synthesis of peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE) is reported. The synthesis of the tricyclic scaffold and conversion of it to a variety of target ICE