Výsledky vyhledávání - "Susan E. Draheim"

Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 2. Indole-3-acetamides with Additional Functionality

Autor: Bach Nicholas J, Dennis R. Berry, Robert D. Dillard, Edward David Mihelich, Jean-Pierre Wery, Cynthia D. Sommers, Lea M. Johnson, David W. Snyder, Donald G. Carlson, David K. Clawson, Emma R. McKinney, Amy C. Smith, Richard Walter Schevitz, Susan E. Draheim, Lawrence W. Hartley, Jennifer L. Olkowski, Noel D. Jones, Nickolay Y. Chirgadze

Publikováno v: Journal of Medicinal Chemistry. 39:5137-5158

As reported in our previous paper, a series of indole-3-acetamides which possessed potency and selectivity as inhibitors of human nonpancreatic secretory phospholipase A2(hnps-PLA2) was developed. The design of these compounds was based on informatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdb0858e7cadcd119a6d3f11a160b093
https://doi.org/10.1021/jm960486n

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Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 3. Indole-3-glyoxamides

Autor: Robert D. Dillard, Susan E. Draheim, Bach Nicholas J, Cynthia D. Sommers, Amy C. Smith, Emma R. McKinney, Noel D. Jones, Jennifer L. Olkowski, Edward David Mihelich, Jean-Pierre Wery, David W. Snyder, Lawrence W. Hartley, Donald G. Carlson, Richard Walter Schevitz, Nickolay Y. Chirgadze, Dennis R. Berry, David K. Clawson, Lea M. Johnson

Publikováno v: Journal of Medicinal Chemistry. 39:5159-5175

Phospholipases (PLAs) produce rate-limiting precursors in the biosynthesis of various types of biologically active lipids involved in inflammatory processes. Increased levels of human nonpancreatic secretory phospholipase A2 (hnps-PLA2) have been det

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96a4d3e2c3e6fd72e60021a3469bd5da
https://doi.org/10.1021/jm960487f

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Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2

Autor: Lawrence W. Hartley, Bach Nicholas J, David W. Snyder, Edward David Mihelich, Robert D. Dillard, Susan E. Draheim, Jean-Pierre Wery, David K. Clawson, C. Sommers, Donald G. Carlson, Richard Walter Schevitz, Jennifer L. Olkowski, Noel D. Jones, Nickolay Y. Chirgadze

Publikováno v: Nature Structural Biology

A lead compound obtained from a high volume human non-pancreatic secretory phospholipase A2 (hnps-PLA2) screen has been developed into a potent inhibitor using detailed structural knowledge of inhibitor binding to the enzyme active site. Four crystal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a39496bafe98a1eb877d330d4835647
http://europepmc.org/articles/PMC7097651

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Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 2. Effect of side-chain modification on in vitro activity and pharmacokinetic parameters

Autor: Jeffrey S. Kasher, Andrew Pike, Susan E. Draheim, Judy A. Eudaly, F. T. Counter, Robert J. Ternansky

Publikováno v: Journal of Medicinal Chemistry. 36:3224-3229

The structure-activity relationship among a series of novel pyrazolidinone antibacterial agents is described. Specifically, the effect of modification of the side chain attached to the nitrogen at C-7 was explored in an attempt to improve the potency

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0da672439f54dc301b7891be0a81f80a
https://doi.org/10.1021/jm00074a002

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Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 1. Effect of nuclear modification on in vitro activity

Autor: Robert J. Ternansky, Susan E. Draheim

Publikováno v: Journal of Medicinal Chemistry. 36:3219-3223

The synthesis and biological evaluation of a series of pyrazolidinone-containing mono- and bicyclic compounds are described. The results of this investigation indicate that the [3.3.0] ring system bearing strongly electron-withdrawing groups in the 3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ad77e0a647103f7b9911699b8732985
https://doi.org/10.1021/jm00074a001

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[3.3.0] Pyrazolodinones: An efficient synthesis of a new class of synthetic antibacterial agents

Autor: Susan E. Draheim, Robert J. Ternansky

Publikováno v: Tetrahedron Letters. 31:2805-2808

A novel synthesis of [3.3.0] fused pyrazolidinones is described. The methodology relies on selective stepwise functionalization of the ring nitrogens of a known pyrazolidinone monocycle. Intramolecular Wadsworth-Horner-Emmons condensation gives rise

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d8d3fbea51c94a4d3e991a77a2a67258
https://doi.org/10.1016/0040-4039(90)80153-d

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Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides

Autor: Robert D. Dillard, Nicholas J. Bach, Susan E. Draheim, Dennis R. Berry, Donald G. Carlson, Nickolay Y. Chirgadze, David K. Clawson, Lawrence W. Hartley, Lea M. Johnson, Noel D. Jones, Emma R. McKinney, Edward D. Mihelich, Jennifer L. Olkowski, Richard W. Schevitz, Amy C. Smith, David W. Snyder, Cynthia D. Sommers, Jean-Pierre Wery

Publikováno v: Journal of medicinal chemistry. 39(26)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::258b47ef40521e42d74456539df7f156
https://pubmed.ncbi.nlm.nih.gov/9005255

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Transgenic model for the discovery of novel human secretory non-pancreatic phospholipase A2 inhibitors

Autor: John D. Sharp, Lawrence W. Hartley, James Schrementi, Bach Nicholas J, Min Song, Susan E. Draheim, David W. Snyder, Donald G. Carlson, Jesse L. Bobbitt, Donald L. White, Lawrence Fisher, Niles Fox, Robert D. Dillard, Edward David Mihelich

Publikováno v: European journal of pharmacology. 308(2)

Transgenic mice were created which overexpress human secretory non-pancreatic phospholipase A2 (sPLA2) pansomatically as a potential disease and drug-testing model. The mice were produced using a DNA construct in which the inducible mouse metallothio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f6960cd88c36019cfd5826d9ed593ca
https://pubmed.ncbi.nlm.nih.gov/8840132

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