Timothy L Macdonald

Author PubWeight™ 69.42‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Immunosuppressive and anti-angiogenic sphingosine 1-phosphate receptor-1 agonists induce ubiquitinylation and proteasomal degradation of the receptor. J Biol Chem 2007 3.07
2 Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem 2004 2.63
3 Selective sphingosine 1-phosphate 1 receptor activation reduces ischemia-reperfusion injury in mouse kidney. Am J Physiol Renal Physiol 2006 2.39
4 Sphingosine kinase 2 is required for modulation of lymphocyte traffic by FTY720. J Biol Chem 2005 1.84
5 Sphingosine-1 phosphate prevents monocyte/endothelial interactions in type 1 diabetic NOD mice through activation of the S1P1 receptor. Circ Res 2006 1.81
6 Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists. Bioorg Med Chem 2006 1.70
7 Sphingosine-1-phosphate receptor subtypes differentially regulate smooth muscle cell phenotype. Arterioscler Thromb Vasc Biol 2008 1.37
8 Synthesis and antimicrobial evaluation of nitazoxanide-based analogues: identification of selective and broad spectrum activity. ChemMedChem 2010 1.33
9 Activation of sphingosine-1-phosphate 1 receptor in the proximal tubule protects against ischemia-reperfusion injury. J Am Soc Nephrol 2010 1.31
10 Discovery, biological evaluation, and structure-activity relationship of amidine based sphingosine kinase inhibitors. J Med Chem 2010 1.28
11 Sphingosine-1-phosphate prevents tumor necrosis factor-{alpha}-mediated monocyte adhesion to aortic endothelium in mice. Arterioscler Thromb Vasc Biol 2005 1.26
12 Asymmetric synthesis of conformationally constrained fingolimod analogues--discovery of an orally active sphingosine 1-phosphate receptor type-1 agonist and receptor type-3 antagonist. J Med Chem 2007 1.22
13 Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells. J Med Chem 2011 1.21
14 Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist. Bioorg Med Chem Lett 2004 1.11
15 S-nitrosothiol depletion in amyotrophic lateral sclerosis. Proc Natl Acad Sci U S A 2006 1.11
16 Nutrient isothiocyanates covalently modify and inhibit the inflammatory cytokine macrophage migration inhibitory factor (MIF). Biochem J 2009 1.09
17 Reduction of infarct size and postischemic inflammation from ATL-146e, a highly selective adenosine A2A receptor agonist, in reperfused canine myocardium. Am J Physiol Heart Circ Physiol 2004 1.08
18 Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists. Bioorg Med Chem Lett 2003 1.06
19 FTY720 promotes local microvascular network formation and regeneration of cranial bone defects. Tissue Eng Part A 2010 1.04
20 Amixicile, a novel inhibitor of pyruvate: ferredoxin oxidoreductase, shows efficacy against Clostridium difficile in a mouse infection model. Antimicrob Agents Chemother 2012 1.03
21 Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists. Bioorg Med Chem Lett 2005 1.02
22 In vitro metabolism of a model cyclopropylamine to reactive intermediate: insights into trovafloxacin-induced hepatotoxicity. Chem Res Toxicol 2008 1.02
23 Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists. Bioorg Med Chem Lett 2004 1.02
24 A novel series of 2-pyridyl-containing compounds as lysophosphatidic acid receptor antagonists: development of a nonhydrolyzable LPA3 receptor-selective antagonist. Bioorg Med Chem Lett 2004 1.01
25 Inhibition of autotaxin production or activity blocks lysophosphatidylcholine-induced migration of human breast cancer and melanoma cells. Mol Carcinog 2009 1.00
26 Sphingosine kinase type 1 inhibition reveals rapid turnover of circulating sphingosine 1-phosphate. Biochem J 2011 0.99
27 Biological activity of the tryprostatins and their diastereomers on human carcinoma cell lines. J Med Chem 2002 0.98
28 A rapid assay for assessment of sphingosine kinase inhibitors and substrates. Anal Biochem 2011 0.97
29 The isothiocyanate class of bioactive nutrients covalently inhibit the MEKK1 protein kinase. BMC Cancer 2007 0.96
30 Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Bioorg Med Chem Lett 2007 0.95
31 Sphingosine-1-phosphate receptors mediate neuromodulatory functions in the CNS. J Neurochem 2009 0.94
32 Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium channel agonists/antagonists. Bioorg Med Chem 2005 0.94
33 Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorg Med Chem Lett 2004 0.93
34 Sphingosine 1-phosphate chemical biology. Biochim Biophys Acta 2008 0.93
35 alpha- and beta-substituted phosphonate analogs of LPA as autotaxin inhibitors. Bioorg Med Chem 2007 0.93
36 The pharmacology and regulation of T type calcium channels: new opportunities for unique therapeutics for cancer. Cell Calcium 2006 0.92
37 Synthesis, stability, and implications of phosphothioate agonists of sphingosine-1-phosphate receptors. Bioorg Med Chem Lett 2005 0.92
38 Nitazoxanide inhibits biofilm formation by Staphylococcus epidermidis by blocking accumulation on surfaces. Antimicrob Agents Chemother 2010 0.90
39 Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide. Bioorg Med Chem Lett 2010 0.87
40 In vitro metabolism of tolcapone to reactive intermediates: relevance to tolcapone liver toxicity. Chem Res Toxicol 2003 0.86
41 Structure-activity relationships of lysophosphatidic acid analogs. Biochim Biophys Acta 2002 0.86
42 Comparative molecular field analysis and QSAR on substrates binding to cytochrome p450 2D6. Bioorg Med Chem 2003 0.86
43 2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors. Bioorg Med Chem Lett 2002 0.86
44 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. J Med Chem 2005 0.86
45 Synthesis and biological evaluation of sphingosine kinase substrates as sphingosine-1-phosphate receptor prodrugs. Bioorg Med Chem 2009 0.85
46 Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J Pharmacol Exp Ther 2011 0.85
47 The role of voltage gated T-type Ca2+ channel isoforms in mediating "capacitative" Ca2+ entry in cancer cells. Cell Calcium 2004 0.85
48 Mechanisms of idiosyncratic drug reactions: the case of felbamate. Chem Biol Interact 2002 0.84
49 Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes. Bioorg Med Chem Lett 2006 0.84
50 Cardioprotection by adenosine A2A agonists in a canine model of myocardial stunning produced by multiple episodes of transient ischemia. Am J Physiol Heart Circ Physiol 2007 0.83
51 Synthesis and structure-activity relationships of tyrosine-based inhibitors of autotaxin (ATX). Bioorg Med Chem Lett 2010 0.83
52 Reactivity of atropaldehyde, a felbamate metabolite in human liver tissue in vitro. Chem Biol Interact 2002 0.80
53 Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein. Bioorg Med Chem 2008 0.79
54 In vitro metabolism of 2-acetylbenzothiophene: relevance to zileuton hepatotoxicity. Chem Res Toxicol 2004 0.79
55 Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs. Bioorg Med Chem Lett 2010 0.78
56 Irreversible alkylation of human serum albumin by zileuton metabolite 2-acetylbenzothiophene-S-oxide: a potential model for hepatotoxicity. Chem Res Toxicol 2007 0.78
57 Influence of propranolol, enalaprilat, verapamil, and caffeine on adenosine A(2A)-receptor-mediated coronary vasodilation. J Am Coll Cardiol 2002 0.77
58 Accelerated CuZn-SOD-mediated oxidation and reduction in the presence of hydrogen peroxide. Biochem Biophys Res Commun 2004 0.77
59 N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists. Bioorg Med Chem Lett 2006 0.77
60 Neutrophil- and myeloperoxidase-mediated metabolism of reduced nimesulide: evidence for bioactivation. Chem Res Toxicol 2010 0.77
61 Interaction between human serum albumin and the felbamate metabolites 4-Hydroxy-5-phenyl-[1,3]oxazinan-2-one and 2-phenylpropenal. Chem Res Toxicol 2002 0.77
62 Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm 2011 0.77
63 A model for the regulation of T-type Ca(2+) channels in proliferation: roles in stem cells and cancer. Expert Rev Anticancer Ther 2013 0.77
64 Mechanisms of trovafloxacin hepatotoxicity: studies of a model cyclopropylamine-containing system. Bioorg Med Chem Lett 2007 0.76
65 In vitro nimesulide studies toward understanding idiosyncratic hepatotoxicity: diiminoquinone formation and conjugation. Chem Res Toxicol 2009 0.76
66 Synthesis of diketopiperazine-based carboline homodimers and in vitro growth inhibition of human carcinomas. Bioorg Med Chem Lett 2008 0.76
67 Cost-effective and Large-scale synthesis of 16:0 Lysophosphatidic Acid. Synth Commun 2012 0.75
68 Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists. Bioorg Med Chem Lett 2004 0.75
69 Regioselective oxidation of 2-amino-3-aroyl-4,5-dialkylthiophenes by DMSO. Bioorg Med Chem Lett 2004 0.75