Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Nalin L. Subasinghe"'
Autor:
Ning Qin, Michael F.A. Finley, Christopher M. Flores, Michael P. Neeper, Michael P. Winters, Michael R. Brandt, Wall Mark, Nalin L. Subasinghe, Raymond W. Colburn, Zhihua Sui, Craig R. Schneider, Mary Lou Lubin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3780-3783
A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay.
Autor:
Mark J, Wall, Nalin L, Subasinghe, Michael P, Winters, Mary Lou, Lubin, Michael F A, Finley, Ning, Qin, Michael R, Brandt, Michael P, Neeper, Craig R, Schneider, Raymond W, Colburn, Christopher M, Flores, Zhihua, Sui
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(23-24)
A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay.
Autor:
Jeremy M. Travins, Carl Crysler, Hufnagel Heather Rae, Karen DiLoreto, Norman Huebert, Michael X. Kolpak, Nalin L. Subasinghe, Jennifer Kirkpatrick, Stephen H. Eisennagel, Bruce E. Tomczuk, Wenxi Pan, Christopher J. Molloy, Ehab Khalil, Nisha S. Ninan, Shelley K. Ballentine, Kristi A. Leonard, Roger F. Bone, Richard Soll, Farah Ali, Michael D. Gaul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5303-5307
Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as humorally mediated graft rejection, ischemia-reperfusion injury (IRI), vascular leak syndrom
Autor:
Michael R. Brandt, Michael F.A. Finley, Ning Qin, Michael P. Winters, Craig R. Schneider, Mary Lou Lubin, Michael P. Neeper, Nalin L. Subasinghe, Zhihua Sui, Raymond W. Colburn, Christopher M. Flores, Wall Mark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4080-4083
Selective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered synthetic ω-conotoxin MVIIA from Conus magnus (ziconotide [Prialt®]) has been approved for t
Autor:
Cuifen Hou, Evan Opas, Dana L. Johnson, Monica Singer, Carl Crysler, James C. Lanter, Zhihua Sui, Fu-An Kang, Sandra McKenney, Xuqing Zhang, Nalin L. Subasinghe, Thomas P. Markotan, Christopher J. Molloy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7496-7501
As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of Q
Autor:
Renee L. DesJarlais, Hui Huang, Jennifer Kirkpatrick, Nalin L. Subasinghe, Norman Huebert, Gaul Michael David, Nisha S. Ninan, Joan Gushue, Jeremy M. Travins, Bruce E. Tomczuk, Roger F. Bone, Shelley K. Ballentine, Christopher J. Molloy, Kristi A. Leonard, Ehab Khalil, Hufnagel Heather Rae, Farah Ali, Maxwell D. Cummings, Richard M. Soll, Wenxi Pan, Carl Crysler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1603-1606
Complement activation has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury, acute respiratory distress syndrome, and acute transplant rejection. Even though the complement cascade provides several protein t
Autor:
Scott I. Klein, M. Jonathan Rudolph, Carl R. Illig, Ehab Khalil, Farah Ali, John C. Spurlino, Renee L. DesJarlais, Carl Crysler, Philip E. Morris, J. M. Kilpatrick, Richard Soll, Y. Sudhakara Babu, Nalin L. Subasinghe, Roger F. Bone, Maxwell D. Cummings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3043-3047
Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and acute transplant rejection. The trypsin-like serine protease C1s represents a pivotal upstream poin
Autor:
Carl R. Illig, Ingrid Deckman, Troy Randle, Kenneth J. Wilson, Frank A. Lewandowski, Bruce L. Grasberger, Renee L. DesJarlais, M. Jonathan Rudolph, James B. Hoffman, Marie Zhang, Carl L. Manthey, David Green, Zhao Zhou, Diane M. Maguire, Nalin L. Subasinghe, Christopher J. Molloy, Celia Sharp, Roger F. Bone, John C. Spurlino, Richard Soll
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:491-495
A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of a variety of substituents at the thiophene 5-position. The 5-alkyl substituted and unsubsti
Autor:
Ning Qin, Mary Lou Lubin, Michael R. Brandt, Edward J. Beck, Zhihua Sui, Christopher M. Flores, Michael P. Winters, Yi Liu, Michael P. Neeper, Michael F.A. Finley, Wall Mark, Nalin L. Subasinghe
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(9)
A novel series of substituted tetrahydropyrrolo[3,4-c]pyrazoles were investigated as blockers of the N-type calcium channel (Cav2.2 channels), a chronic pain target.
Autor:
Yi Liu, Mary Lou Lubin, Christopher M. Flores, Michael P. Winters, Michael F.A. Finley, Wall Mark, Ning Qin, Nalin L. Subasinghe, Michael R. Brandt, Michael P. Neeper, Zhihua Sui, Edward J. Beck
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(9)
A novel series of substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles were investigated as N-type calcium channel blockers (Cav2.2 channels), a chronic pain target. One compound was active in vivo in the rat CFA pain model.