Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Aaron B. Miller"'
Autor:
Harry B. Marr, Kevin P. Madauss, Jonathan Y. Bass, Shawn P. Williams, Dan Todd, Paul Kenneth Spearing, Adwoa Akwabi-Ameyaw, Lihong Chen, Robert B. McFadyen, Justin A. Caravella, Derek J. Parks, Frank Navas, David N. Deaton, Katrina L. Creech, G. Bruce Wisely, Richard Dana Caldwell, Aaron B. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4733-4739
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::537fc0c9b0822e4038f1ffd07428e5e6
https://doi.org/10.1016/j.bmcl.2009.06.062
https://doi.org/10.1016/j.bmcl.2009.06.062
Autor:
Mary H. Hanlon, Aaron B. Miller, David J.T. Porter, Kevin P. Madauss, J. David Becherer, Robert A. Reid, Caroline J. Diaz, Luke H. Carter, A.M. Hassell, Curt D. Haffner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4360-4363
We report the synthesis and in vitro activity of a series of novel pyrrolidinyl pyridones and pyrazinones as potent inhibitors of prolyl oligopeptidase (POP). Within this series, compound 39 was co-crystallized within the catalytic site of a human ch
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d2d58be90cd92e414d6f27d3989a221
https://doi.org/10.1016/j.bmcl.2008.06.067
https://doi.org/10.1016/j.bmcl.2008.06.067
Autor:
Lihong Chen, Jonathan Y. Bass, David N. Deaton, Aaron B. Miller, Justin A. Caravella, Istvan Kaldor, Robert B. McFadyen, Stacey A. Jones, Dan Todd, Paul Kenneth Spearing, Kevin P. Madauss, Adwoa Akwabi-Ameyaw, Derek J. Parks, Richard Dana Caldwell, Frank Navas, Yaping Liu, Katrina L. Creech, G. Bruce Wisely, Harry B. Marr, Shawn P. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4339-4343
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::519480e527d445babf5d509d5d05a857
https://doi.org/10.1016/j.bmcl.2008.06.073
https://doi.org/10.1016/j.bmcl.2008.06.073
Autor:
David Barrett, Stacey T. Long, Francis X. Tavares, David N. Deaton, Lois L. Wright, Hui-Qiang Q. Zhou, Vicente Samano, John G. Catalano, Kevin J. Wells-Knecht, Aaron B. Miller, Robert B. McFadyen, Larry R. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:22-27
Starting from a potent ketone-based inhibitor with poor drug properties, incorporation of P2–P3 elements from a ketoamide-based inhibitor led to the identification of a hybrid series of ketone-based cathepsin K inhibitors with better oral bioavaila
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::777f108ae24de7e7a380b16adbe58df6
https://doi.org/10.1016/j.bmcl.2006.10.102
https://doi.org/10.1016/j.bmcl.2006.10.102
Autor:
Timothy M. Willson, William J. Zuercher, Robert T. Nolte, Lisa A. Orband-Miller, Jon L. Collins, Aaron B. Miller, Donald P. McDonnell, Esther Y. Chao, Liping Wang, Stephanie Gaillard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:821-824
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1f894c8bd07d4f3f45e6d37f5158b50
https://doi.org/10.1016/j.bmcl.2005.11.030
https://doi.org/10.1016/j.bmcl.2005.11.030
Autor:
Lisa M. Shewchuk, Anne M. Hassell, Derril H. Willard, J. Alan Payne, David Barrett, Lois L. Wright, Robert B. McFadyen, Larry R. Miller, Aaron B. Miller, David N. Deaton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3039-3043
Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bee27c96bb071b57f116d0d8db816d21
https://doi.org/10.1016/j.bmcl.2005.04.032
https://doi.org/10.1016/j.bmcl.2005.04.032
Autor:
Robert B. McFadyen, Aaron B. Miller, Stacey T. Long, Kevin J. Wells-Knecht, Larry R. Miller, David N. Deaton, David Barrett, John G. Catalano, Lois L. Wright
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2209-2213
Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P2 elements led to 100-fold enhancements in inhibitory activity. Modifications to one of these leads resu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88a64514a36399c164dd9f5b63bc8a1a
https://doi.org/10.1016/j.bmcl.2005.03.023
https://doi.org/10.1016/j.bmcl.2005.03.023
Autor:
Eric E. Boros, David N. Deaton, Anne M. Hassell, Robert B. McFadyen, Aaron B. Miller, Larry R. Miller, Margot G. Paulick, Lisa M. Shewchuk, James B. Thompson, Derril H. Willard, Lois L. Wright
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3425-3429
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 pos
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2d893fe77b49a68c37528fd61c26e5d
https://doi.org/10.1016/j.bmcl.2004.04.084
https://doi.org/10.1016/j.bmcl.2004.04.084
Autor:
Aaron B. Miller, Steve Blanchard, Kate A. Dwornik, Dallas K. Croom, Robert T. Gampe, Tom G. Consler, James M. Lenhard, Olivia Ittoop, Valerie G. Montana, Randy K. Bledsoe, and Andrea Ayscue, Darryl Lynn Mcdougald, Curt D. Haffner, H. Eric Xu
Publikováno v:
Journal of Medicinal Chemistry. 47:2010-2029
A series of tetrahydrobenzofuranyl and tetrahydrobenzothienyl propenoic acids that showed potent agonist activity against RXRalpha were synthesized via a structure-based design approach. Among the compounds studied, 46a,b showed not only very good po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37272a91a5f51d032982fc530dd7de0b
https://doi.org/10.1021/jm030565g
https://doi.org/10.1021/jm030565g
Autor:
Kevin J. Wells-Knecht, Stacey T. Long, Anne M. Hassell, Larry R. Miller, David N. Deaton, Huiqiang Zhou, Lisa M. Shewchuk, Francis X. Tavares, Lois L. Wright, Alan A Payne, Virginia M. Boncek, Aaron B. Miller, Derril H. Willard
Publikováno v:
Journal of Medicinal Chemistry. 47:588-599
Osteoclast-mediated bone matrix resorption has been attributed to cathepsin K, a cysteine protease of the papain family that is abundantly and selectively expressed in osteoclast. Inhibition of cathepsin K could potentially be an effective method to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::751a111c6a75eea2babc9f09bee524a3
https://doi.org/10.1021/jm030373l
https://doi.org/10.1021/jm030373l