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1Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists

Robert J Ardecky,Dawn A Brooks,A G Godfrey, Sarah Beth Jones,Nathan Bryan Mantlo,James R Mccarthy,P Y Michellys,Christopher J Rito,John S Tyhonas,Leonard L Winneroski,Yanping Xu

2007引用：23

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2Design, Synthesis and Structure - Activity Relationship of Novel Rxr-Selective Modulators

Py Michellys,J D'Arrigo,Ta Grese,Ds Karanewsky,Md Leibowitz,Da Mais,Cm Mapes, A Reifel-Miller,D Rungta,Mf Boehm

The synthesis and in vitro characterization of novel RXR-selective ligands possessing various substituted 1-benzofuran or 1-benzothiophene moieties are described.

2004ChemInform（2004）引用：30

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3Design and Synthesis of Benzofused Heterocyclic Rxr Modulators

DL Gernert,DA Neel,MF Boehm,MD Leibowitz,DA Mais,PY Michellys,D Rungta, A Reifel-Miller,TA Grese

Benzofused heterocyclic analogs of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the choice of heterocycle as well as the sidechain employed.

2004BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2004）引用：19

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4Rxr Modulators. Design And Synthesis Of New Rxr-Selective Phenyl- And Pyridine-Locked Dienoic Acids For The Treatment Of Type 2 Diabetes.

Jh Chen,Py Michellys,Rj Ardecky,Cm Mapes,Js Tyhonas,Md Leibowitz,Aw Thompson,Mf Boehm,A Miller,Ta Grese,G Etgen,N Yumibe,

2003ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2003）

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5Design and Synthesis of Fluorinated RXR Modulators

DL Gernert,R Ajamie,RA Ardecky,MG Bell,MD Leibowitz,DA Mais,CM Mapes,PY Michellys,D Rungta,A Reifel-Miller,JS Tyhonas,N Yumibe,

Fluorinated trienoic acid analogues of the RXR selective modulator 1 (LG101506) were synthesized, and tested for their ability to bind RXRalpha and activate RXR homo and heterodimers. Potency and efficacy were observed to be dependent upon the position of fluorination, and improvement in pharmacological profile was demonstrated in some cases.

2003Bioorganic & Medicinal Chemistry Letters（2003）引用：27

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6Design and Synthesis of Novel RXR-selective Modulators with Improved Pharmacological Profile.

PY Michellys, MF Boehms, JH Chen,TA Grese, DS Karanewsky,MD Leibowitz, S Liu,DA Mais,CM Mapes, A Reifel-Miller,KM Ogilvie,D Rungta,

New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their metabolic properties (exposure in IRC male mice) and show a dramatic increase of exposure compared to our reference compound, 3 (LG101506).

2003Bioorganic & Medicinal Chemistry Letters（2003）引用：28

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7Novel (2E,4e,6z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic Acid Retinoid X Receptor Modulators Are Active in Models of Type 2 Diabetes

Py Michellys,Rj Ardecky,Jh Chen,Dl Crombie,Gj Etgen,Mm Faul,Al Faulkner,Ta Grese,Ra Heyman,Ds Karanewsky,K Klausing,Md Leibowitz,

Previous data have shown that RXR-selective agonists (e.g., 3 and 4) are insulin sensitizers in rodent models of non-insulin-dependent diabetes mellitus (NIDDM). Unfortunately, they also produce dramatic increases in triglycerides and profound suppression of the thyroid hormone axis. Here we describe the design and synthesis of new RXR modulators that retain the insulin-sensitizing activity of RXR agonists but produce substantially reduced side effects. These molecules bind selectively and with high affinity to RXR and, unlike RXR agonists, do not activate RXR homodimers. To further evaluate the antidiabetic activity of these RXR modulators, we have designed a concise and systematic structure-activity relationship around the 2E,4E,6Z-7-aryl-3-methylocta-2,4,6-trienoic acid scaffold. Selected compounds have been evaluated using insulin-resistant rodents (db/db mice) to characterize effects on glucose homeostasis. Our studies demonstrate the effectiveness of RXR modulators in lowering plasma glucose in the db/db mouse model.

2003Journal of Medicinal Chemistry（2003）引用：58

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8Rxr Modulators. Design, Synthesis And Hypoglycemic Activity Of New Rxr-Selective Locked-Dienoic Acids.