P. E. Bender | AMiner学者主页

Evaluation of a variety of PDE4 inhibitors in a series of cellular and in vivo assays suggested a strategy to improve the therapeutic index of PDE4 inhibitors by increasing their selectivity for the ability to inhibit PDE4 catalytic activity versus the ability to compete for high affinity [3H]rolipram-binding sites in the central nervous system. Use of this strategy led ultimately to the identification of cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxyl ic acid (1, SB 207499, Ariflo), a potent second-generation inhibitor of PDE4 with a decreased potential for side effects versus the archetypic first generation inhibitor, (R)-rolipram.

1998Journal of Medicinal Chemistry（1998）引用：164

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7Regulation of Stress-Induced Cytokine Production by Pyridinylimidazoles; Inhibition of CSBP Kinase

TF Gallagher,GL Seibel,S Kassis,JT Laydon,MJ Blumenthal,JC Lee,D Lee,JC Boehm, SM FierThompson,JW Abt, ME Soreson,JM Smietana,

Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway. Based upon SAR and protein homology modeling, the pharmacophore and three potential modes of binding to the enzyme are presented. For a subset of pyridinylimidazoles, binding is shown to correlate with inhibition of CSBP kinase activity, whereas no significant inhibition of PKA, PKC alpha and ERK kinase activity is observed.

1997BIOORGANIC & MEDICINAL CHEMISTRY（1997）引用：267

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8Monomeres de 4,4-cyclohexan(disubstitue)-1-ols et composes s'y rapportant

Paul E Bender,Siegfried B Christensen,Joseph M Karpinski,M Dominic Ryan

1996引用：23

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94.4-(DISUBSTITUTED)CYCLOHEXAN-1-OLS-MONOMERS AND RELATED COMPOUNDS

Siegfried B Christensen,Joseph M Karpinski,Dominic M Ryan,Paul E Bender

1995引用：33

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10Monomeres de 1,3,3-(trisubstitue)cyclohexane et composes apparentes

Siegfried B Christensen,Joseph M Karpinski,M Dominic Ryan,Paul E Bender

1995引用：23

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11Monomeres 3,3-(disubstitues) cyclohexan-1-carboxylate et composes correspondants

Paul E Bender,Siegfried B Christensen,Joseph M Karpinski,M Dominic Ryan

1995引用：23

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122,4,5-Triarylimidazole Inhibitors of Il-1 Biosynthesis

TF GALLAGHER, SM FIERTHOMPSON,RS GARIGIPATI, ME SORENSON,JM SMIETANA,D LEE,PE BENDER,JC LEE,JT LAYDON,DE GRISWOLD,MC CHABOTFLETCHER,JJ BRETON,

As part of an effort to define the pharmacophore and discover the mechanism by which the anti-inflammatory dual cyclooxygenase / 5-lipoxygenase inhibitors SK & F 86002 and SK & F 105809 inhibit IL-1 biosynthesis, a series of substituted 2,4,5-triarylimidazole derivatives were prepared and evaluated as inhibitors of IL-1 and 5-lipoxygenase biosynthesis.

1995BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1995）引用：176

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134-phenyl-1,2-cyclohexyl derivatives and anti-inflammatory compositions and methods thereof

Siegfried B Christensen,Paul E Bender,Cornelia J Forster,John G Gleason

1995引用：32

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14TRI-SUBSTITUTED IMIDAZOLES HAVING MULTIPLE THERAPEUTIC PROPERTIES

Jerry L Adams,Paul E Bender,Jeffrey C Boehm,Timothy F Gallagher,Ravi Shanker Garigipati,Peter William Sheldrake

1994引用：72

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15Inhibition of interleukin-1 and tumor necrosis factor production by monocytes and/or macrophages

Paul E Bender,Don E Griswold,Nabil Hanna,John C Lee,Bartholomew J Votta,P L Simon,Alison M Badger,K M Esser

1994引用：73

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16Process for the preparation of trisubstituted imidazole compounds with multiple therapeutic properties

Jerry L Adams,Paul E Bender,Jeffrey C Boehm,Timothy F Gallagher,Ravi Shanker Garigipati,Peter William Sheldrake

1994引用：23

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17Formamide intermediates for the preparation of tri-substituted imidazole compounds with multiple therapeutic properties

Jerry L Adams,Paul E Bender,Jeffrey C Boehm,Timothy F Gallagher,Ravi Shanker Garigipati,Peter William Sheldrake

1994引用：23

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18Bicyclic Imidazoles As a Novel Class of Cytokine Biosynthesis Inhibitors

JC LEE,AM BADGER,DE GRISWOLD,D DUNNINGTON,A TRUNEH,B VOTTA,JR WHITE,PR YOUNG,PE BENDER

Annals of the New York Academy of SciencesVolume 696, Issue 1 p. 149-170 Bicyclic Imidazoles as a Novel Class of Cytokine Biosynthesis Inhibitors J. C. LEE, J. C. LEE Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorA. M. BADGER, A. M. BADGER Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorD. E. GRISWOLD, D. E. GRISWOLD Department of Respiratory and Inflammation Pharmacology, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorD. DUNNINGTON, D. DUNNINGTON Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorA. TRUNEH, A. TRUNEH Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorB. VOTTA, B. VOTTA Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorJ. R. WHITE, J. R. WHITE Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorP. R. YOUNG, P. R. YOUNG Department of Molecular Genetics, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorP. E. BENDER, P. E. BENDER Department of Medicinal Chemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this author J. C. LEE, J. C. LEE Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorA. M. BADGER, A. M. BADGER Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorD. E. GRISWOLD, D. E. GRISWOLD Department of Respiratory and Inflammation Pharmacology, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorD. DUNNINGTON, D. DUNNINGTON Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorA. TRUNEH, A. TRUNEH Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorB. VOTTA, B. VOTTA Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorJ. R. WHITE, J. R. WHITE Department of Cellular Biochemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorP. R. YOUNG, P. R. YOUNG Department of Molecular Genetics, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this authorP. E. BENDER, P. E. BENDER Department of Medicinal Chemistry, SmithKline Beecham Pharmaceutical 709 Swedeland Road Post Office Box 1539 King of Prussia, Pennsylvania 19406Search for more papers by this author First published: November 1993 https://doi.org/10.1111/j.1749-6632.1993.tb17149.xCitations: 73AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinked InRedditWechat Citing Literature Volume696, Issue1Immunosuppressive and Anti‐Inflammatory DrugsNovember 1993Pages 149-170 RelatedInformation

1993IMMUNOSUPPRESSIVE AND ANTIINFLAMMATORY DRUGS（1993）引用：181

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19ChemInform Abstract: Synthesis, X‐Ray Crystal Structure Determination and Antiinflammatory Activity of the Regioisomers: 5‐Phenyl‐6‐(4‐pyridyl)‐2,3‐dihydroimidazo(2,1‐b)thiazole and 6‐Phenyl‐5‐(4‐pyridyl)‐2,3‐dihydroimidazo(2,1‐b)thiazole. A Structural Reassignment.