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Publikationer i urvalet

12 träffar

Bibliografisk träff 2020-06-10

Identification of Highly Selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors by a Covalent Fragment-Based Approach.

Huang F, Hu H, Wang K, Peng C, Xu W, Zhang Y, Gao J, Liu Y, Zhou H, Huang R, Li M, Shen J, Xu Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c00372

Bibliografisk träff 2017-12-24

Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis.

Guibbal F, Bénard S, Patché J, Meneyrol V, Couprie J, Yong-Sang J, Meilhac O, Jestin E.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.12.052

Bibliografisk träff 2017-12-15

Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2.

Liu Q, Huang F, Yuan X, Wang K, Zou Y, Shen J, Xu Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.7b01530

Bibliografisk träff 2016-11-18

Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA<sub>2</sub>).

Woolford AJ, Day PJ, Bénéton V, Berdini V, Coyle JE, Dudit Y, Grondin P, Huet P, Lee LY, Manas ES, McMenamin RL, Murray CW, Page LW, Patel VK, Potvain F, Rich SJ, Sang Y, Somers DO, Trottet L, Wan Z, Zhang X.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.6b01427

Bibliografisk träff 2016-11-15

Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLA<sub>2</sub> Inhibitor.

Measom ND, Down KD, Hirst DJ, Jamieson C, Manas ES, Patel VK, Somers DO.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.6b00281

Bibliografisk träff 2016-05-20

Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening.

Woolford AJ, Pero JE, Aravapalli S, Berdini V, Coyle JE, Day PJ, Dodson AM, Grondin P, Holding FP, Lee LY, Li P, Manas ES, Marino J, Martin AC, McCleland BW, McMenamin RL, Murray CW, Neipp CE, Page LW, Patel VK, Potvain F, Rich S, Rivero RA, Smith K, Somers DO, Trottet L, Velagaleti R, Williams G, Xie R.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.6b00212

Bibliografisk träff 2016-04-26

Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors.

Liu Q, Chen X, Chen W, Yuan X, Su H, Shen J, Xu Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.6b00282

Bibliografisk träff 2016-03-08

Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular Edema.

Chen X, Wang K, Xu W, Ma Q, Chen M, Du L, Mo M, Wang Y, Shen J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01930

Bibliografisk träff 2015-10-28

Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors.

Chen X, Xu W, Wang K, Mo M, Zhang W, Du L, Yuan X, Xu Y, Wang Y, Shen J.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01024

Bibliografisk träff 2013-03-26

Triazole derivatives: a series of Darapladib analogues as orally active Lp-PLA2 inhibitors.

Wang K, Xu W, Zhang W, Mo M, Wang Y, Shen J.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2013.03.062

Bibliografisk träff 2013-01-16

Design and synthesis of imidazole and triazole derivatives as Lp-PLA₂ inhibitors and the unexpected discovery of highly potent quaternary ammonium salts.

Wang K, Xu W, Liu Y, Zhang W, Wang W, Shen J, Wang Y.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2013.01.029

Bibliografisk träff 2003-03-01

The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.

Blackie JA, Bloomer JC, Brown MJ, Cheng HY, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Smith SA, Stansfield IG, Stanway SJ, Taylor MA, Theobald CJ.

Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(03)00058-1