Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Valentina V. Jeliazkova-Mecheva"'
Autor:
Hugh Nuthall, Lily Y. Moy, Candia M. Kenific, Sean P. Ahearn, Damaris Diaz, Elizabeth Helen Kelley, Bethany Hughes, Armetta D. Hill, Adam J. Schell, Nadya Smotrov, Valentina V. Jeliazkova-Mecheva, Chris Moxham, Hua Zhou, Sanjiv J. Shah, Andrew Rosenau, Alexey Rivkin, Sam Kattar, Joey L. Methot, Richard G. Ball, William Brown, Mark S. Shearman, Chaomin Li, Christian Fischer, Alexander A. Szewczak, Sujal V. Deshmukh, Dawn M. Mampreian, Thomas A. Miller, Benito Munoz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3495-3500
The triazolyl amide γ-secretase modulators are potent alternatives to the cinnamyl amides that have entered the clinic for the treatment of Alzheimer's disease. Herein we build on the lead benzoazepinones described in our prior communication with im
Autor:
Richard E. Middleton, Valentina V. Jeliazkova-Mecheva, Damaris Diaz, Candia M. Kenific, George N. Nikov, Sanjiv J. Shah, Adam J. Schell, Bethany Hughes, Nadja Smotrov, Alexander A. Szewczak, Melanie Bouthillette, Hugh Nuthall, Deborah Walker, W. Colby Brown, Mark S. Shearman, Hua Zhou, Benito Munoz, Christian Fischer, Dan F. Savage, Joey L. Methot, Jonathan C. Cruz, Susan L. Zultanski, Nathan Bays, Dawn M. Mampreian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4083-4087
Synthesis, SAR, and evaluation of aryl triazoles as novel gamma secretase modulators (GSMs) are presented in this communication. Starting from the literature and in-house leads, we evaluated a range of five-membered heterocycles as replacements for o
Autor:
Sujal V. Deshmukh, Susan L. Zultanski, George N. Nikov, Christopher M. Moxham, Armetta D. Hill, Lily Y. Moy, Nadya Smotrov, Christian Fischer, Hua Zhou, Joey L. Methot, Maria S. Michener, Bethany Hughes, Damaris Diaz, Zhenhua Wu, Jacquelynn J. Cook, Sanjiv J. Shah, Benito Munoz, Jonathan C. Cruz, Flobert Tanga, Nathan Bays, Melanie Bouthillette, Bo-Sheng Pan, Valentina V. Jeliazkova-Mecheva, Ikuo Hayashi, Mark S. Shearman, Candia M. Kenific, Deborah Walker
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of Aβ42 led to the discover
Publikováno v:
Microvascular Research. 71:108-114
Heat shock was imposed on an in vitro model of the blood-brain barrier (BBB) by submersion into prewarmed growth medium. Transendothelial electrical resistance (TEER) was used to assess the functional integrity of the endothelial barrier. Consequence
Publikováno v:
Brain Research Protocols. 12:91-98
A method for the isolation of porcine atrocytes as a simple extension of a previously described procedure for isolation of brain capillary endothelial cells from adolescent pigs [Methods Cell Sci. 17 (1995) 2] is described. The obtained astroglial cu
Autor:
George N. Nikov, Flobert Tanga, Chris Moxham, Ziping Yang, Chaomin Li, Richard G. Ball, Joshua Close, Richard W. Heidebrecht, Gloria Y. Kwei, Lin Xu, Laura Surdi, Xiaoliu Geng, Candia Kenefic, Sanjiv J. Shah, Dan F. Savage, Valentina V. Jeliazkova-Mecheva, Jennifer Chapnick, Julie Elizabeth Burke, Solomon Kattar, Bethany Hughes, Lily Y. Moy, Sujal V. Deshmukh, Paul Moses, Damaris Diaz, John Kevin Leach, Paul Tempest, John Hendrix, Amanda Markarewicz, Nadya Smotrov, Ilona Kariv, Michael J. McNevin, Ben Munoz, Mark S. Shearman, Thomas A. Miller
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(9)
Alzheimer’s disease is a major unmet medical need with pathology characterized by extracellular proteinaceous plaques comprised primarily of β-amyloid. γ-Secretase is a critical enzyme in the cellular pathway responsible for the formation of a ra
Autor:
Lin Xu, Laird A. Trimble, Bruce Adams, Valentina V. Jeliazkova-Mecheva, Andreas Harsch, Gloria Y. Kwei
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 36(4)
Three novel conjugation metabolites of colchicine were identified in rat bile facilitated by enhanced on-line liquid chromatography-accurate radioisotope counting. The known 2- and 3-demethylcolchicines (DMCs) underwent O-sulfate conjugation in addit
Autor:
Wolf B, Jeliazkova-Mecheva V, Del Rio-Espinola A, Boisclair J, Walker D, Cochin De Billy B, Flaherty M, Flandre T
Publikováno v:
Toxicological sciences : an official journal of the Society of Toxicology [Toxicol Sci] 2022 Jan 24; Vol. 185 (2), pp. 246.
Autor:
Wolf B; Novartis Institutes for BioMedical Research, Preclinical Safety, 4002 Basel, Switzerland., Jeliazkova-Mecheva V; Novartis Institutes for BioMedical Research, Preclinical Safety, Cambridge, Massachusetts 02139, USA., Del Rio-Espinola A; Novartis Institutes for BioMedical Research, Preclinical Safety, 4002 Basel, Switzerland., Boisclair J; Novartis Institutes for BioMedical Research, Preclinical Safety, 4002 Basel, Switzerland., Walker D; Novartis Institutes for BioMedical Research, Preclinical Safety, Cambridge, Massachusetts 02139, USA., Cochin De Billy B; Novartis Institutes for BioMedical Research, Preclinical Safety, 4002 Basel, Switzerland., Flaherty M; Novartis Institutes for BioMedical Research, Preclinical Safety, Cambridge, Massachusetts 02139, USA., Flandre T; Novartis Institutes for BioMedical Research, Preclinical Safety, 4002 Basel, Switzerland.
Publikováno v:
Toxicological sciences : an official journal of the Society of Toxicology [Toxicol Sci] 2021 Dec 28; Vol. 185 (1), pp. 89-104.
Autor:
Close J; Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. joshua_close@merck.com, Heidebrecht R Jr, Hendrix J, Li C, Munoz B, Surdi L, Kattar S, Tempest P, Moses P, Geng X, Hughes B, Smotrov N, Moxham C, Chapnick J, Kariv I, Nikov G, Burke JE, Deshmukh S, Jeliazkova-Mecheva V, Leach JK, Diaz D, Xu L, Yang Z, Kwei G, Moy L, Shah S, Tanga F, Kenefic C, Savage D, Shearman M, Ball RG, McNevin MJ, Markarewicz A, Miller T
Publikováno v:
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3203-7. Date of Electronic Publication: 2012 Mar 17.