Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Christopher, Baccei"'
Autor:
Daniel S. Lorrain, Ariana O Lorenzana, Alexander Broadhead, Christopher Baccei, Xiong Yifeng, Thomas O. Schrader, Michael M Poon, Karin J. Stebbins
Publikováno v:
ACS Medicinal Chemistry Letters. 12:155-161
The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M1 antagonist, linker replacement and structure-activity relationship investiga
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::430b568160efae9b410358b8f2bedc3b
https://doi.org/10.1021/acsmedchemlett.0c00626
https://doi.org/10.1021/acsmedchemlett.0c00626
Autor:
Kim Fischer, Bryan Laffitte, Jason D. Jacintho, Christopher Baccei, Catherine Lee, Karin J. Stebbins, Alex R. Broadhead, Davorka Messmer, Lucia Correa, Daniel S. Lorrain, Peppi Prasit, Austin Chen, Nicholas Simon Stock, Yalda Bravo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:503-508
We previously published on the design and synthesis of novel, potent and selective PPARα antagonists suitable for either i.p. or oral in vivo administration for the potential treatment of cancer. Described herein is SAR for a subsequent program, whe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86e1852f2be64898c0f9b88e9a60a368
https://doi.org/10.1016/j.bmcl.2018.12.045
https://doi.org/10.1016/j.bmcl.2018.12.045
Autor:
Thomas O, Schrader, Yifeng, Xiong, Ariana O, Lorenzana, Alexander, Broadhead, Karin J, Stebbins, Michael M, Poon, Christopher, Baccei, Daniel S, Lorrain
Publikováno v:
ACS Med Chem Lett
[Image: see text] The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M(1) antagonist, linker replacement and structure–activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::3fa8ec81843f4909dda2e384fce0b703
https://pubmed.ncbi.nlm.nih.gov/33488977
https://pubmed.ncbi.nlm.nih.gov/33488977
Autor:
Jason D. Jacintho, Richard Bundey, Nicholas Simon Stock, Alex R. Broadhead, Karin J. Stebbins, Austin Chen, Ryan C. Clark, Lucia Correa, Yalda Bravo, Christopher Baccei, Peppi Prasit, Davorka Messmer, Daniel S. Lorrain
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2267-2272
The discovery and SAR of a novel series of potent and selective PPARα antagonists are herein described. Exploration of replacements for the labile acyl sulfonamide linker led to a biaryl sulfonamide series of which compound 33 proved to be suitable
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0831ca0312667de4945e3418afd1045
https://doi.org/10.1016/j.bmcl.2014.03.090
https://doi.org/10.1016/j.bmcl.2014.03.090
Autor:
Peppi Prasit, Daniel S. Lorrain, Davorka Messmer, Karin J. Stebbins, Lucia Correa, Austin Chen, Richard Bundey, Geraldine Cabrera, Alex R. Broadhead, Nicholas Simon Stock, Christopher Baccei, Yalda Bravo
Publikováno v:
European journal of pharmacology. 809
Peroxisome-proliferator activated receptors (PPAR) are members of the nuclear hormone receptor superfamily which regulate gene transcription. PPARα is a key regulator of lipid homeostasis and a negative regulator of inflammation. Under conditions of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d81a51b31cebff203d417e655669f24
https://pubmed.ncbi.nlm.nih.gov/28483457
https://pubmed.ncbi.nlm.nih.gov/28483457
Autor:
Charles Chapman, Alex R. Broadhead, Peppi Prasit, Christopher Baccei, Nicholas Simon Stock, Yiwei Li, Jeffrey Roger Roppe, Angelina M. Santini, Dan Lorrain, Lucia Correa, Gretchen Bain, Jasmine Eleanor Zunic, Jeannie Ziff, Christopher D. King, Catherine Lee, Pat Prodanovich, Janice Darlington, Haojing Rong, Jilly F. Evans, Hutchinson John H
Publikováno v:
Journal of Medicinal Chemistry. 54:8013-8029
The potent 5-lipoxygenase-activating protein (FLAP) inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid 11cc is described (AM803, now GSK2190915). Building upo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fbf179f44ba2592906663a125ace36d
https://doi.org/10.1021/jm2008369
https://doi.org/10.1021/jm2008369
Autor:
Christopher Baccei, Jilly F. Evans, Daniel S. Lorrain, Yen Troung, Hutchinson John H, Peppi Prasit, Janice Darlington, Gretchen Bain, Brian Andrew Stearns, Christopher D. King, Catherine Lee, Karin J. Stebbins, Alex R. Broadhead, Angelina M. Santini, Pat Prodanovich
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 338:290-301
The prostaglandin D(2) (PGD(2)) receptor type 2 (DP2) is a G protein-coupled receptor that has been shown to be involved in a variety of allergic diseases, including allergic rhinitis, asthma, and atopic dermatitis. In this study, we describe the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6712b393e7da1ebfb64225ffc12e7bfe
https://doi.org/10.1124/jpet.111.180430
https://doi.org/10.1124/jpet.111.180430
Autor:
Timothy Parr, Jeffrey Roger Roppe, Christopher Baccei, Gretchen Bain, Janice Darlington, Nicholas Simon Stock, Charles Chapman, Lucia Correa, Alex R. Broadhead, Hutchinson John H, Daniel S. Lorrain, Brian Andrew Stearns, Christopher D. King, Angelina M. Santini, Catherine Lee, Karin J. Stebbins, Pat Prodanovich, Peppi Prasit, Jilly F. Evans, Deborah Volkots
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1036-1040
Compound 21 (AM432) was identified as a potent and selective antagonist of the DP2 receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c61da34684106e4141e51f6fe39171d6
https://doi.org/10.1016/j.bmcl.2010.12.016
https://doi.org/10.1016/j.bmcl.2010.12.016
Autor:
Nicholas Simon Stock, Jilly F. Evans, Angelina M. Santini, Patricia Prodanovich, Hutchinson John H, Daniel S. Lorrain, Yen Pham Truong, Alex R. Broadhead, Jill Melissa Scott, Peppi Prasit, Christopher Baccei, Patrick Fagan, Heather Coate, Brian Andrew Stearns, Christopher D. King, Karin J. Stebbins, Gretchen Bain
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 332:764-775
Prostaglandin D(2) (PGD(2)) is one of a family of biologically active lipids derived from arachidonic acid via the action of COX-1 and COX-2. PGD(2) is released from mast cells and binds primarily to two G protein-coupled receptors, namely DP1 and DP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2f1afd08e1dd668bba850e22f16b979
https://doi.org/10.1124/jpet.109.161919
https://doi.org/10.1124/jpet.109.161919
Autor:
Ryan C. Clark, Daniel S. Lorrain, Gretchen Bain, Jill Melissa Scott, Hutchinson John H, Alex R. Broadhead, Brian A. Stearns, Nicholas Simon Stock, Patrick Fagan, Yen Pham Truong, Angelina M. Santini, Heather Coate, Christopher Baccei, Christopher D. King, Jilly F. Evans, Catherine Lee, Peppi Prasit, Pat Prodanovich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4647-4651
The synthesis of a series of tricyclic antagonists for the prostaglandin D(2) receptor DP2 (CRTH2) is disclosed. The activities of the compounds were evaluated in a human DP2 binding assay and a human whole blood eosinophil shape change assay. Potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3c1e4e6de423e3948f39109431fbe4d
https://doi.org/10.1016/j.bmcl.2009.06.085
https://doi.org/10.1016/j.bmcl.2009.06.085