Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Grace Reyes-Manalo"'
Autor:
Theodore M, Kamenecka, Céline, Bonnefous, Steven, Govek, Jean-Michel, Vernier, John, Hutchinson, Janice, Chung, Grace, Reyes-Manalo, Jeffery J, Anderson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4350-4353
Modulation of the metabotropic glutamate subtype 5 (mGlu5) receptor may be useful in the treatment of a variety of central nervous system disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amines as small
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6adaf2149ac25773b2a8c81552c49696
https://doi.org/10.1016/j.bmcl.2005.06.059
https://doi.org/10.1016/j.bmcl.2005.06.059
Autor:
Janice Chung, Hutchinson John H, Celine Bonnefous, Jean-Michel Vernier, Theodore M. Kamenecka, Grace Reyes-Manalo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1197-1200
The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amides as small molecules mGluR5 antagonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a87a6a4c4f0dcf7c05beec254b749d98
https://doi.org/10.1016/j.bmcl.2004.11.078
https://doi.org/10.1016/j.bmcl.2004.11.078
Autor:
Benito Munoz, Jeffrey Roger Roppe, Jeffery J. Anderson, Edwin J. Schweiger, Janice Chung, Merryl Cramer, Grace Reyes-Manalo, Lida Tehrani, Xiaohui Jiang, Nicholas D. P. Cosford, Bowei Wang, Theodore M. Kamenecka, Jesse Brodkin, Dehua Huang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3993-3996
Structure-activity relationship studies leading to the discovery of a new, orally active mGlu5 receptor antagonist are described. The title compound, 5-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine, is highly potent in vitro, has good in vivo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0ed6369ce4ac35bdb8054a29f2c002b
https://doi.org/10.1016/j.bmcl.2004.05.037
https://doi.org/10.1016/j.bmcl.2004.05.037
Autor:
Grace Reyes-Manalo, Edwin J. Schweiger, Mitchell D. Green, Janice Chung, Christopher D. King, Johnny Yasuo Nagasawa, Nicholas D. P. Cosford, Peter C. Chua, Jeffrey Anderson, Merryl Cramer, Lida Tehrani, Benito Munoz, Leo Bleicher
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(20)
Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bf2af7dcd707b2687a6250d8287bd3d
https://pubmed.ncbi.nlm.nih.gov/16115767
https://pubmed.ncbi.nlm.nih.gov/16115767
Autor:
Steven F Poon, Brian W. Eastman, Chixu Chen, Nicholas D. P. Cosford, Nicholas D. Smith, Grace Reyes-Manalo, Benito Munoz, Janice Chung
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(22)
The SAR of the lead compounds 2a and 2b was rapidly explored. Utilizing a parallel solution-phase Suzuki coupling approach, in tandem with strong cation exchange resin (SCX) purification afforded the desired focused library. The library was evaluated
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d8e254cf946fe442a0301a63ca5ef98
https://pubmed.ncbi.nlm.nih.gov/15482909
https://pubmed.ncbi.nlm.nih.gov/15482909