Výsledky vyhledávání - "Ronald L. Magolda"

Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities

Publikováno v: Proceedings of the National Academy of Sciences. 105:33-38

Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target of rapamycin (mTOR) binding region yields immunophilin ligands, WYE-592 and ILS-920, with p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c60bb03f86803494ea3efa91d69a376
https://doi.org/10.1073/pnas.0710424105

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Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists

Autor: Ronald C. Bernotas, David Zenan Li, Hassan Mahmoud Elokdah, Lee E. Schechter, Geraldine Ruth Mcfarlane, Guo Ming Zhang, Deborah L. Smith, Albert J. Robichaud, Ronald L. Magolda

Publikováno v: Bioorganic & Medicinal Chemistry. 15:6208-6226

1-Aminoethyl-3-arylsulfonyl-1H-indoles 1 are 5-HT(6) receptor ligands with modest activity in a 5-HT(6) cyclase assay. Introduction of an additional nitrogen in the indole ring provides 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 2 with bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::852b4ee5af4141d74fd3eec30baa58ef
https://doi.org/10.1016/j.bmc.2007.06.024

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Discovery of potent and selective PKC-θ inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:225-230

An uHTS campaign was performed to identify selective inhibitors of PKC-theta. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-theta i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a34c352960493e0ce0044cbad949680
https://doi.org/10.1016/j.bmcl.2006.09.056

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Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors

Autor: Joseph J. Petraitis, Margaret F. Favata, Joseph B. Santella, Robert A. Copeland, John Wityak, Ronald L. Magolda, James M. Trzaskos, Bruce D. Jaffe, George L. Trainor, Gardner Daniel S, Peggy A. Scherle, Kurumi Y. Horiuchi, Jung-Hui Sun, Frank W. Hobbs, Andrea J. Daulerio, John V. Duncia

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 14:1483-1486

Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC(50)=140 nM) were rapidly synthesized leading to single digit nM inhibitors, displaying submicromolar AP-1 transcription inhibition in COS-7 cel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47c68052de8368fc45bc4db9534d3974
https://doi.org/10.1016/j.bmcl.2004.01.012

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Rational design, synthesis and structure–activity relationships of a cyclic succinate series of TNF-α converting enzyme inhibitors. Part 2: lead optimization

Autor: Chu-Biao Xue, Xiaohua He, John Roderick, Ronald L Corbett, James J.-W Duan, Rui-Qin Liu, Maryanne B Covington, Mingxin Qian, Maria D Ribadeneira, Krishna Vaddi, David D Christ, Robert C Newton, James M Trzaskos, Ronald L Magolda, Ruth R Wexler, Carl P Decicco

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:4299-4304

Modifications of the lead TACE inhibitor 1 (N-hydroxy-trans-2-{[4-(4-quinolinyloxymethyl)anilinyl]carbonyl}-1-cyclohexanecarboxamide) at the cyclohexyl ring and the quinoline moiety led to the identification of a series of piperidine containing TACE

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e77c3dec33f6160bdbe29873bacd31d0
https://doi.org/10.1016/j.bmcl.2003.09.057

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Discovery of N-Hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Autor: James M. Trzaskos, Carl P. Decicco, Jingwu Duan, Chu-Biao Xue, Robert C. Newton, Rui-Qin Liu, Zelda R. Wasserman, Jennifer L. Seng, Zhonghui Lu, Ronald L. Magolda, Xiaohua He, John Roderick, Maryanne B. Covington

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:2035-2040

New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered using an N -hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series was found to be potent in a porcine TACE (pTACE) assay with IC 50 s typically below 5 nM. F

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eecef0fc1e086cce3db1b3112350ee7
https://doi.org/10.1016/s0960-894x(03)00313-5

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