Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Tamara A. Miskowski"'
Autor:
Chaozhong Cai, Alexey B. Dyatkin, Paul R. Wade, Kavash Robert W, Sui-Po Zhang, Henry J. Breslin, Craig J. Diamond, Wei He, Tamara A. Miskowski, Pamela J. Hornby
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4869-4872
A small set of acyclic analogs 5 were prepared to explore their structure-activity relationships (SARs) relative to heterocyclic core, opioid receptor (OR) agonists 4. Compound 5l was found to have very favorable OR binding affinities at the δ and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2c81ce41ee0795527efdfdb550ea3b0
https://doi.org/10.1016/j.bmcl.2012.05.042
https://doi.org/10.1016/j.bmcl.2012.05.042
Autor:
Pamela J. Hornby, Bruce P. Damiano, Alexey B. Dyatkin, N. H. Wallace, M. Carolyn Fisher, Stephen M. Prouty, Bruce E. Maryanoff, Edward S. Kimball, Wei He, Rosemary J. Santulli, Craig R. Schneider, Yong Gong, William A. Kinney, Craig J. Diamond, Tamara A. Miskowski
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:6693-6702
A series of N-carboxy, N-alkyl, and N-carboxamido azabicyclo[2.2.2]octane carboxamides were prepared and assayed for inhibition of α4β1-VCAM-1 and α4β7-MAdCAM-1 interactions. Potency and α4β1/α4β7 selectivity were sensitive to the substituent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::04fac0ca403e4acd6788a9ee123e776a
https://doi.org/10.1016/j.bmc.2005.07.022
https://doi.org/10.1016/j.bmc.2005.07.022
Publikováno v:
Journal of Molecular Graphics and Modelling. 23:409-418
A homology model of the active site region of tripeptidyl peptidase II (TPP II) was constructed based on the crystal structures of four subtilisin-like templates. The resulting model was subsequently validated by judging expectations of the model ver
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::413674b9f723324c105f450da608f8c2
https://doi.org/10.1016/j.jmgm.2004.11.009
https://doi.org/10.1016/j.jmgm.2004.11.009
Autor:
Jeffrey M. Palmer, Mark Schulz, Alexey B. Dyatkin, Joseph G. Lisko, Pamela J. Hornby, Janet L. Ralbovsky, Kristen M. Chevalier, Wei He, John R. Mabus, Tamara A. Miskowski, Steven J. Coats
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(10)
A series of guanidine triazinediones were identified as potent PK1 receptor antagonists. A compound in this series inhibited the PK1 invoked prosecretory response in rat ileum tissue.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63cd1ef3583ea052045fd6ecd6feb9e0
https://pubmed.ncbi.nlm.nih.gov/19375913
https://pubmed.ncbi.nlm.nih.gov/19375913
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists
Autor:
Yong Gong, Barbay Jk, Dennis J. Hlasta, Stephen M. Prouty, Scott A. Ballentine, Patricia Andrade-Gordon, Alexey B. Dyatkin, William Hageman, John A. Masucci, Rosemary J. Santulli, M. C. Fisher, Pamela J. Hornby, Wei He, N. H. Wallace, Bruce P. Damiano, Craig R. Schneider, Tamara A. Miskowski, Edward S. Kimball, Bruce E. Maryanoff
Publikováno v:
Journal of medicinal chemistry. 49(11)
A novel series of pyridazinone-functionalized phenylalanine analogues was prepared and evaluated for inhibition of cellular adhesion mediated by alpha4beta1/VCAM-1 and alpha4beta7/MAdCAM-1 interactions. Concise syntheses were developed and applied fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ab6d43b8982876cebeb4e969ff606aa
https://pubmed.ncbi.nlm.nih.gov/16722660
https://pubmed.ncbi.nlm.nih.gov/16722660
Autor:
Tamara A. Miskowski, Raymond W. Colburn, Jian Li, Jeffrey M. Palmer, Wei He, Dennis J. Stone, N. H. Wallace, Rebecca P. Martinez, Craig R. Schneider, Sui-Po Zhang, Henry J. Breslin, Bryan M. Rafferty, Edward S. Kimball, Santosh V. Coutinho
Publikováno v:
Journal of medicinal chemistry. 47(21)
A small series of novel, imidazoles 4 have been prepared that exhibit very good binding affinities for the delta and mu opioid receptors (ORs), as well as demonstrate potent agonist functional activity at the delta OR. Representative imidazole 4a (K(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b1144fc2fb49ba472b339ed0f8f78fb
https://pubmed.ncbi.nlm.nih.gov/15456245
https://pubmed.ncbi.nlm.nih.gov/15456245
Autor:
Peter Walter Maria Roevens, Hans De Winter, Kavash Robert W, Michael Joseph Kukla, Maria V. F. Somers, Henry J. Breslin, Tamara A. Miskowski
Publikováno v:
ChemInform. 35
We have systematically explored the structure–activity relationship (SAR) for a series of compounds 2 as inhibitors of tripeptidyl-peptidase II (TPP II), a serine protease responsible for the degradation of cholecystokinin-8 (CCK-8). This SAR evalu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::01d68875052e7e78e263510fd9ce94e6
https://doi.org/10.1002/chin.200412135
https://doi.org/10.1002/chin.200412135
Autor:
Maria V. F. Somers, Tamara A. Miskowski, Michael Joseph Kukla, Peter Walter Maria Roevens, Hans De Winter, Kavash Robert W, Henry J. Breslin
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(24)
We have systematically explored the structure–activity relationship (SAR) for a series of compounds 2 as inhibitors of tripeptidyl-peptidase II (TPP II), a serine protease responsible for the degradation of cholecystokinin-8 (CCK-8). This SAR evalu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b79c48ff52a08881f068c8b3e2557ea
https://pubmed.ncbi.nlm.nih.gov/14643348
https://pubmed.ncbi.nlm.nih.gov/14643348
Autor:
Hans De Winter, Tamara A. Miskowski, Daniëlle C G Peeters, Diane A. Gauthier, Henry J. Breslin, Michael Joseph Kukla, William H Leister, Maria V. F. Somers, Peter Walter Maria Roevens
Publikováno v:
Journal of medicinal chemistry. 45(24)
Butabindide, 1, was previously reported as a potent inhibitor (IC50 = 7 nM) of the serine protease enzyme tripeptidyl peptidase II (TPPII), an endogenous protease that degrades cholecystokinin-8 (CCK-8). We found that 1 has some inherent chemical ins
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83f845ae4fa75673139357af37d064da
https://pubmed.ncbi.nlm.nih.gov/12431057
https://pubmed.ncbi.nlm.nih.gov/12431057