63 articles for thisTarget
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Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
University of Washington
5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.
University of Washington
SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.
University of Washington
Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals.
University of Washington
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
University of Washington
HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2).
University of Washington
Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase.
University of Washington
Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization.
University of Washington
Development of Toxoplasma gondii calcium-dependent protein kinase 1 (TgCDPK1) inhibitors with potent anti-toxoplasma activity.
University of Washington
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.
University of Washington
Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.
University of Washington
Discovery of Potent and Selective Inhibitors of Calcium-Dependent Protein Kinase 1 (CDPK1) from C. parvum and T. gondii.
University of Washington
Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.
University of Washington
Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase.
University of Washington
Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.
University of Washington
Selective tight binding inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase via structure-based drug design.
University of Washington
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
University of Washington
Isothiocyanate-substituted benzyl ether opioid receptor ligands derived from 6 beta-naltrexol.
University of Washington
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
Selective inhibition of trypanosomal glyceraldehyde-3-phosphate dehydrogenase by protein structure-based design: toward new drugs for the treatment of sleeping sickness.
University of Washington
Isothiocyanate-substituted kappa-selective opioid receptor ligands derived from N-methyl-N-[(1S)-1-phenyl-2-(1-pyrrolidinyl)ethyl] phenylacetamide.
University of Washington
O3-(2-carbomethoxyallyl) ethers of opioid ligands derived from oxymorphone, naltrexone, etorphine, diprenorphine, norbinaltorphimine, and naltrindole. Unexpected O3-dealkylation in the opioid radioligand displacement assay.
University of Washington
Electrophilic opioid ligands. Oxygen tethered alpha-methylene-gamma-lactone, acrylate, isothiocyanate, and epoxide derivatives of 6 beta-naltrexol.
University of Washington
Electrophilic alpha-methylene-gamma-lactone and isothiocyanate opioid ligands related to etorphine.
University of Washington
Conjugate addition ligands of opioid antagonists. Methacrylate esters and ethers of 6 alpha- and 6 beta-naltrexol.
University of Washington
Interactions of thiol-containing androgens with human placental aromatase.
University of Washington
A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.
University of Washington
Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5' and 8.
University of Washington
Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL.
University of Washington
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
University of Washington
Rational modification of a candidate cancer drug for use against Chagas disease.
University of Washington
Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
University of Washington
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
University of Washington
Selective deuteration of bupropion slows epimerization and reduces metabolism.
University of Washington
The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.
University of Washington
Cyclic Peptide Screening Methods for Preclinical Drug Discovery.
University of Washington
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.
University of Washington
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against
University of Washington
Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy.
University of Washington
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
University of Washington
Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.
University of Washington
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
University of Washington
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
University of Washington
Structurally simple inhibitors of lanosterol 14alpha-demethylase are efficacious in a rodent model of acute Chagas disease.
University of Washington
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
University of Washington
Adenosine analogues as inhibitors of Trypanosoma brucei phosphoglycerate kinase: elucidation of a novel binding mode for a 2-amino-N(6)-substituted adenosine.
University of Washington
Phenotypic Optimization of Urea-Thiophene Carboxamides To Yield Potent, Well Tolerated, and Orally Active Protective Agents against Aminoglycoside-Induced Hearing Loss.
University of Washington
Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
University of Washington
1-sulfonamido-4-aryloxy compounds, and preparation method and medicinal application thereof
China Pharmaceutical University
Specific inhibitors of cytochrome P450 26 retinoic acid hydroxylase
University of Washington Through Its Center For Commercialization
Hydrazine compound as blood coagulation factor Xa inhibitor
North China Pharmaceutical
Design, synthesis and biological evaluation of pyridin-3-yl pyrimidines as potent Bcr-Abl inhibitors.
Xi'An Jiaotong University
Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles.
Adolor
Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
Amgen
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.
Wyeth Research