Výsledky vyhledávání - "Harry B. Marr"

FXR agonist activity of conformationally constrained analogs of GW 4064

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

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Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064

Autor: Justin A. Caravella, David N. Deaton, Katrina L. Creech, G. Bruce Wisely, Jonathan Y. Bass, Lihong Chen, Harry B. Marr, Robert B. McFadyen, Shawn P. Williams, Richard Dana Caldwell, Kevin P. Madauss, Aaron B. Miller, Derek J. Parks, Dan Todd

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2969-2973

Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-posit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecaaf14e70189436e51664e2f641b1ca
https://doi.org/10.1016/j.bmcl.2009.04.047

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Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064

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

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Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene

Autor: Aaron B. Miller, Harry B. Marr, Katrina L. Creech, G. Bruce Wisely, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Lihong Chen, David N. Deaton, Justin A. Caravella, Paul Kenneth Spearing, Kevin P. Madauss, Derek J. Parks, Frank Navas, Dan Todd

Publikováno v: Bioorganicmedicinal chemistry letters. 21(20)

To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f939259f5c374490a071b94fee47ab3
https://pubmed.ncbi.nlm.nih.gov/21890356

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Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene

Autor: Justin A. Caravella, Terrence L. Smalley, Jonathan Y. Bass, Kevin P. Madauss, Aaron B. Miller, Robert B. McFadyen, Katrina L. Creech, G. Bruce Wisely, Harry B. Marr, Lihong Chen, Dan Todd, Shawn P. Williams, David N. Deaton, Paul Kenneth Spearing, Derek J. Parks, Frank Navas, Wendy Y. Mills

Publikováno v: Bioorganicmedicinal chemistry letters. 21(4)

To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74fde8626b56404560d9578dd0bfc42d
https://pubmed.ncbi.nlm.nih.gov/21256005

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Application of phosphoramidate ProTide technology significantly improves antiviral potency of carbocyclic adenosine derivatives

Autor: Alshaimaa Hassan-Abdallah, Jennifer Poole Peckham, Yikang Wang, Harry B. Marr, Richard J. Hazen, Jan Balzarini, S Srinivasan, Huiqiang Zhou, Christopher McGuigan, Adam Siddiqui, Ed W. McLean, Kristjan Gudmundsson, Lynn D. Condreay, Lance C. Johnson, Susan Daluge, Thimysta C. Burnette

Publikováno v: Journal of medicinal chemistry. 49(24)

We report the application of phosphoramidate pronucleotide (ProTide) technology to the antiviral agent carbocyclic L-d4A (L-Cd4A). The phenyl methyl alaninyl parent ProTide of L-Cd4A was prepared by Grignard-mediated phosphorochloridate reaction and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7824881a4d809b81a6bb35631e73c45
https://pubmed.ncbi.nlm.nih.gov/17125274

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Application of phosphoramidate pronucleotide technology to abacavir leads to a significant enhancement of antiviral potency

Autor: Erik De Clercq, Richard J. Hazen, Jan Balzarini, Kristjan S. Gudmundsson, Sarah Ann Harris, Harry B. Marr, Ed W. McLean, Thimysta C. Burnette, Christopher McGuigan, Lance C. Johnson, Lynn D. Condreay, Susan Mary Daluge

Publikováno v: Journal of medicinal chemistry. 48(10)

We report the first application of pronucleotide (ProTide) technology to the antiviral agent abacavir (Ziagen), used for the treatment of HIV infection. The phenylmethoxyalaninyl phosphoramidate of abacavir was prepared in good yield in one step. Als

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf9178a1a2d682447c328ddadc7c8205
https://pubmed.ncbi.nlm.nih.gov/15887959

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A new assay and solubilization procedure for steroid 17,20-lyase from rat testes

Autor: Harry B Marr, Fred I. Chasalow, George T. Taylor

Publikováno v: Steroids. 39(6)

We report an assay for testicular 17,20-lyase which depends on the use of [21-14C]progesterone as a substrate. The method is made possible by a simplified procedure for the synthesis of [21-14C]progesterone. A chromatographic separation of the unreac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7449bbfca5aa3f3ebdfb3d5a28839257
https://pubmed.ncbi.nlm.nih.gov/7157434

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