Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Michael Robert Peel"'
Autor:
Dongfang Meng, Dann L. Parker, Robin Kirwan, M A Powles, Jennifer Nielsen Kahn, James M. Apgar, Fred Racine, Paul A. Liberator, Amy M. Flattery, Andrew Galgoci, Kingsley H. Nelson, James M. Balkovec, Andrew S. Misura, Weiming Fan, Donald M. Sperbeck, Michael Robert Peel, Robert A. Giacobbe, Mark L. Greenlee, Ahmed Mamai, Jasminka Dragovic, Kenneth J. Wildonger, Hao Liu, Robert R. Wilkening, Mary Motyl, Shu Lee, Ming-Jo Hsu, Charles Gill, George K. Abruzzo
Publikováno v:
Bioorganicmedicinal chemistry letters. 32
We previously reported medicinal chemistry efforts that identified MK-5204, an orally efficacious β-1,3-glucan synthesis inhibitor derived from the natural product enfumafungin. Further extensive optimization of the C2 triazole substituent identifie
Autor:
James M. Balkovec, Robert A. Giacobbe, Jennifer Nielsen Kahn, Ming Jo Hsu, Weiming Fan, Ahmed Mamai, Michael Robert Peel, James M. Apgar, Amy M. Flattery, Paul A. Liberator, Fred Racine, Bahanu Habulihaz, Mary Motyl, Kingsley H. Nelson, Robert R. Wilkening, Robin Kirwan, M A Powles, George K. Abruzzo, Andrew Galgoci, Charles Gill, Andrew S. Misura, Shu Lee, Jasminka Dragovic, Hao Liu, Mark L. Greenlee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5813-5818
The clinical success of the echinocandins, which can only be administered parentally, has validated β-1,3-glucan synthase (GS) as an antifungal target. Semi-synthetic modification of enfumafungin, a triterpene glycoside natural product, was performe
Autor:
Michael Robert Peel, Andrew Scribner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters
Graphical abstract
Cyclophilins (Cyps) are ubiquitous proteins that effect the cis–trans isomerization of Pro amide bonds, and are thus crucial to protein folding. CypA is the most prevalent of the ∼19 human Cyps, and plays a crucial role in
Cyclophilins (Cyps) are ubiquitous proteins that effect the cis–trans isomerization of Pro amide bonds, and are thus crucial to protein folding. CypA is the most prevalent of the ∼19 human Cyps, and plays a crucial role in
Autor:
Dann L. Parker, James M. Apgar, Robert A. Giacobbe, Ming Jo Hsu, Kingsley H. Nelson, Gregory J. Pacofsky, Paul A. Liberator, Fred Racine, Dongfang Meng, Ghjuvanni Coti, James M. Balkovec, Ahmed Mamai, Brian H. Heasley, Mark L. Greenlee, Jennifer Nielsen Kahn, Michael Robert Peel, Robert R. Wilkening, Hao Liu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6811-6816
Orally bioavailable inhibitors of β-(1,3)- d -glucan synthase have been pursued as new, broad-spectrum fungicidal therapies suitable for treatment in immunocompromised patients. Toward this end, a collaborative medicinal chemistry program was establ
Synthesis and biological evaluation of [d-lysine]8cyclosporin A analogs as potential anti-HCV agents
Autor:
Andrew Scribner, David Renwick Houck, Sarah Mosier, Michael Robert Peel, Zhuhui Huang, Bernard Scorneaux
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6542-6546
An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)
Autor:
James Marvin Veal, Robert J. Griffin, Jennifer G. Badiang Alberti, Daniel J. Price, Michael J. Reno, Anne M. Hassell, Michael Robert Peel, Lisa M. Shewchuk, Victoria B. Knick, Stephen T. Davis, Laurie S. Kane-Carson, Kirk L. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5758-5762
A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions
Autor:
Andrew Scribner, Michael Robert Peel
Publikováno v:
ChemInform. 46
Background Since its isolation in 1970, and discovery of its potent inhibitory activity on T-cell proliferation, cyclosporin A (CsA) has been shown to play a significant role in diverse fields of biology. Furthermore, chemical modification of CsA has
Autor:
Michael Robert Peel, Andrew Scribner
Publikováno v:
Biochimica et biophysica acta. 1850(10)
Background Since its isolation in 1970, and discovery of its potent inhibitory activity on T-cell proliferation, cyclosporin A (CsA) has been shown to play a significant role in diverse fields of biology. Furthermore, chemical modification of CsA has
Autor:
Kristjan S. Gudmundsson, F. Leslie Boyd, Brian A. Johns, David Kendall Jung, Connie J. Sexton, Scott H. Allen, Michael Robert Peel, Elizabeth M. Turner
Publikováno v:
Tetrahedron. 59:9001-9011
Synthesis of a novel class of 7-amino-3-pyrimidinyl-pyrazolo[1,5-a]pyridine antiherpetic compounds is described. The synthetic methodology is designed to allow for rapid analog synthesis around the C-3 and C-7 positions of the pyrazolo[1,5-a]pyridine
Autor:
Stephen A. Stimpson, David Kendall Jung, Andrea H. Epperly, Michael Robert Peel, Mui Cheung, Michael J. Alberti, Stanley D. Chamberlain, Jennifer Gabriel Badiang, Philip A. Harris, Stephanie Harris, Neal H. Bramson, Peckham Gregory
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5428-5430
A series of pyrazolo[1,5-a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series are described.