Zobrazeno 1 - 10
of 143
pro vyhledávání: '"and Roger M. Freidinger"'
Publikováno v:
International Journal of Peptide and Protein Research. 16:464-470
gamma, delta- and epsilon-lactam containing cyclic hexapeptide analogs of cyclo-(Ala-Sar)3 have been prepared by cyclotrimerization. The analogs are covalently bridged between the methyl groups of the alanine and sarcosine residues. Only the delta-la
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60115a1d6c7861061e9375901a4a38a5
https://doi.org/10.1111/j.1399-3011.1980.tb02970.x
https://doi.org/10.1111/j.1399-3011.1980.tb02970.x
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f489daa5ddd1907e6d600a79ad35db5d
https://doi.org/10.1016/j.bmcl.2007.11.050
https://doi.org/10.1016/j.bmcl.2007.11.050
Autor:
Douglas J. Pettibone, Thomayant Prueksaritanont, Christina Ng, Ronald K. Chang, Cuyue Tang, Roger M. Freidinger, Richard W. Ransom, Mark G. Bock, Kathy L. Murphy, Scott D. Kuduk
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3925-3929
SAR study of the biphenyl region of 2,3-diaminopyridine bradykinin B 1 antagonists was investigated with non-aromatic carbo- and heterocyclic rings. A piperidine ring was found to be a good replacement for the proximal phenyl ring while replacement o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::896941299378e294f50e0645c266a9a0
https://doi.org/10.1016/j.bmcl.2005.05.133
https://doi.org/10.1016/j.bmcl.2005.05.133
Autor:
J. Fred Hess, Michael A. Wallace, Rick W. Ransom, Douglas J. Pettibone, C. Meacham Harrell, Kathy L. Murphy, Matthew M. Zrada, Roger M. Freidinger, M. Kristine Markowitz, Bang-Lin Wan, Dai-Shi Su, Mark G. Bock, Dennis C. Dean, R. S. L. Chang, S. S. O'malley, Conrad E. Raab
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:6045-6048
We have developed an efficient and selective radioligand, the [35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in transgenic rats over-expressing the human bradykinin B1 receptor.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd26b8e760658cf74db72a04fe61f73b
https://doi.org/10.1016/j.bmcl.2004.09.074
https://doi.org/10.1016/j.bmcl.2004.09.074
Autor:
Roger M. Freidinger
Publikováno v:
Journal of Medicinal Chemistry. 46:5553-5566
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79ef6f7e3142e73a9142c322f8b7a203
https://doi.org/10.1021/jm030484k
https://doi.org/10.1021/jm030484k
Autor:
Duan Chen, Chun-Mei Zhao, Martin Beinborn, Alan S. Kopin, Ci Chen, Roger M. Freidinger, Edward W. McBride
Publikováno v:
Proceedings of the National Academy of Sciences. 100:5525-5530
The search for small-molecule drugs that act at peptide hormone receptors has resulted in the identification of a wide variety of antagonists. In contrast, the discovery of nonpeptide agonists has been far more elusive. We have used a constitutively
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f82f3abeed4ac9decaad5d44d475660
https://doi.org/10.1073/pnas.0831223100
https://doi.org/10.1073/pnas.0831223100
Autor:
Punam Sandhu, Stacey O'Malley, Michael R. Wood, Tsing-Bau Chen, June J. Kim, Douglas J. Pettibone, Joseph J. Lynch, Wei Han, Gary L. Stump, Roger M. Freidinger, Tanya MacNeil, Bruce D. Dorsey, Richard W. Ransom, E V Lis, Raymond S.L. Chang, Charles M. Harrell, Peter J. Bondiskey, Robert M. DiPardo, Joan D. Ellis, Carl F. Homnick, Kathy L. Murphy, Mark G. Bock, Scott D. Kuduk, Patricia Miller
Publikováno v:
Journal of Medicinal Chemistry. 46:1803-1806
Antagonism of the bradykinin B(1) receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B(1) receptor (K(i) = 0.59 nM) and hi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4339898a624691ea9cc43463fa84f9b0
https://doi.org/10.1021/jm034020y
https://doi.org/10.1021/jm034020y
Autor:
Georgia B. McGaughey, Joseph G. Joyce, Xiaoping Liang, Renee Danzeisen, Michael W. Miller, Roger M. Freidinger, Victor M. Garsky, John W. Shiver, Michael P. Citron, Michael J. Bogusky, W M Hurni
Publikováno v:
Biochemistry. 42:3214-3223
The human immunodeficiency virus type I (HIV-1) transmembrane glycoprotein gp41 mediates viral entry through fusion of the target cellular and viral membranes. A segment of gp41 containing the sequence Glu-Leu-Asp-Lys-Trp-Ala has previously been iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::636529910cd91841429d5eb67a2ead10
https://doi.org/10.1021/bi026952u
https://doi.org/10.1021/bi026952u
Autor:
Rodney A. Bednar, Roger M. Freidinger, John A. McCauley, Keith A. Wafford, David A. Claremon, Christopher F. Claiborne, Brian E. Libby, Stuart R. Michelson, Alison J. Macaulay, Nigel J. Liverton, Thomas M. Connolly, Bohumil Bednar, Kenneth S. Koblan, Stanley L. Gaul, Scott D. Mosser, Joseph J. Lynch, Cindra L. Condra, Gary L. Stump, Helen J. Diggle, Janusz Jozef Kulagowski, Kenneth D. Anderson, Neil Roy Curtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:697-700
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dd299167537625261e03641a62d5a8a0
https://doi.org/10.1016/s0960-894x(02)01061-2
https://doi.org/10.1016/s0960-894x(02)01061-2
Autor:
Wei Lemaire, Julie A. O'Brien, Roger M. Freidinger, Maryann Burno, Dennis C. Dean, Peter D. Williams, Douglas J. Pettibone, Ashok Chaudhary, David L. Williams
Publikováno v:
European Journal of Pharmacology. 450:19-28
A novel, potent nonpeptide oxytocin receptor antagonist (1-(1-(2-(2,2,2-trifluoroethoxy)-4-(1-methylsulfonyl-4-piperidinyloxy) phenylacetyl)-4-piperidinyl)-3,4-dihydro-2(1H)-quinolinone) has been identified that can be labeled to high specific activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7835a909017623c8488ae58826bfba0a
https://doi.org/10.1016/s0014-2999(02)02048-4
https://doi.org/10.1016/s0014-2999(02)02048-4