Published in Drug Metab Dispos on November 20, 2012
A Novel Therapeutic Agent for Type 2 Diabetes Mellitus: SGLT2 Inhibitor. Diabetes Metab J (2014) 1.14
An evaluation of US patent 2015065565 (A1) for a new class of SGLT2 inhibitors for treatment 1 of type II diabetes mellitus. Expert Opin Ther Pat (2015) 0.75
SHR3824, a novel selective inhibitor of renal sodium glucose cotransporter 2, exhibits antidiabetic efficacy in rodent models. Acta Pharmacol Sin (2014) 0.75
Novel Treatments Target Type-2 Diabetes. P T (2016) 0.75
Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date. Drug Des Devel Ther (2017) 0.75
Determinants of Indian physicians' satisfaction & dissatisfaction from their job. Indian J Med Res (2014) 2.09
On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds. Nat Chem Biol (2011) 1.82
A novel mechanism of cyclooxygenase-2 inhibition involving interactions with Ser-530 and Tyr-385. J Biol Chem (2003) 1.69
Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States. Chem Res Toxicol (2011) 1.54
A comprehensive listing of bioactivation pathways of organic functional groups. Curr Drug Metab (2005) 1.47
Combined NIRS and IVUS imaging detects vulnerable plaque using a single catheter system: a head-to-head comparison with OCT. EuroIntervention (2014) 1.44
The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos (2004) 1.43
Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria. Proc Natl Acad Sci U S A (2012) 1.34
Biotransformation reactions of five-membered aromatic heterocyclic rings. Chem Res Toxicol (2002) 1.22
Design, methods, and evaluation directions of a multi-access service for the management of diabetes mellitus patients. Diabetes Technol Ther (2003) 1.18
ElectroShape: fast molecular similarity calculations incorporating shape, chirality and electrostatics. J Comput Aided Mol Des (2010) 1.14
Application of conformation design in acyclic stereoselection: total synthesis of borrelidin as the crystalline benzene solvate. J Am Chem Soc (2003) 1.08
Muscle glucose transport and phosphorylation in type 2 diabetic, obese nondiabetic, and genetically predisposed individuals. Am J Physiol Endocrinol Metab (2006) 1.05
Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance(). Medchemcomm (2012) 1.05
Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding. J Pharmacol Exp Ther (2005) 1.05
The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia. Sleep (2012) 1.04
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. J Med Chem (2012) 1.01
Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication. J Med Chem (2011) 1.01
Synthesis of sulfones from organozinc reagents, DABSO, and alkyl halides. Org Lett (2013) 1.01
Evaluation of cerebrospinal fluid concentration and plasma free concentration as a surrogate measurement for brain free concentration. Drug Metab Dispos (2006) 1.00
Inhibition of hepatobiliary transport as a predictive method for clinical hepatotoxicity of nefazodone. Toxicol Sci (2006) 0.99
Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity. J Med Chem (2010) 0.98
Validation of isolated metabolites from drug metabolism studies as analytical standards by quantitative NMR. Drug Metab Dispos (2010) 0.97
Immune-mediated agranulocytosis caused by the cocaine adulterant levamisole: a case for reactive metabolite(s) involvement. Drug Metab Dispos (2012) 0.96
Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist. J Psychopharmacol (2011) 0.95
Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose. Chem Res Toxicol (2008) 0.95
Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metab Dispos (2004) 0.94
2-[4-Chloro-3-(4-ethoxy-benz-yl)phen-yl]-1,3-dithiane. Acta Crystallogr Sect E Struct Rep Online (2010) 0.93
The use of plasma aldosterone and urinary sodium to potassium ratio as translatable quantitative biomarkers of mineralocorticoid receptor antagonism. J Transl Med (2011) 0.93
Multiple dose pharmacokinetics of paroxetine in children and adolescents with major depressive disorder or obsessive-compulsive disorder. Neuropsychopharmacology (2006) 0.92
Application of fundamental organometallic chemistry to the development of a gold-catalyzed synthesis of sulfinate derivatives. Angew Chem Int Ed Engl (2014) 0.92
Palladium-catalyzed sulfination of aryl and heteroaryl halides: direct access to sulfones and sulfonamides. Org Lett (2013) 0.91
Glycomimetic ligands for the human asialoglycoprotein receptor. J Am Chem Soc (2012) 0.91
The discovery of novel calcium sensing receptor negative allosteric modulators. Bioorg Med Chem Lett (2009) 0.90
In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam: insights into the hepatotoxicity of sudoxicam. Chem Res Toxicol (2008) 0.90
Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2). J Med Chem (2012) 0.90
Metabolic activation in drug-induced liver injury. Drug Metab Rev (2011) 0.90
Carbon monoxide poisoning is prevented by the energy costs of conformational changes in gas-binding haemproteins. Proc Natl Acad Sci U S A (2011) 0.90
Prevalence of extended spectrum beta lactamase and AmpC beta lactamase producers among Escherichia coli isolates in a tertiary care hospital in Jaipur. Indian J Pathol Microbiol (2008) 0.88
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg Med Chem Lett (2011) 0.87
Thiazolides as novel antiviral agents. 2. Inhibition of hepatitis C virus replication. J Med Chem (2011) 0.87
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem (2011) 0.87
Application of a linear ion trap/orbitrap mass spectrometer in metabolite characterization studies: examination of the human liver microsomal metabolism of the non-tricyclic anti-depressant nefazodone using data-dependent accurate mass measurements. J Am Soc Mass Spectrom (2006) 0.86
Within-subject comparison of striatal D2 receptor occupancy measurements using [123I]IBZM SPECT and [11C]Raclopride PET. Neuroimage (2009) 0.86
Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos (2011) 0.86
Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor. Drug Metab Dispos (2013) 0.86
Pharmacodynamic model of sodium-glucose transporter 2 (SGLT2) inhibition: implications for quantitative translational pharmacology. AAPS J (2011) 0.85
A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues. Chem Res Toxicol (2006) 0.84
Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide-1 Receptor (GLP-1R) Agonists. J Med Chem (2015) 0.84
Can in vitro metabolism-dependent covalent binding data distinguish hepatotoxic from nonhepatotoxic drugs? An analysis using human hepatocytes and liver S-9 fraction. Chem Res Toxicol (2009) 0.84
Characterization of a 7% carbon dioxide (CO2) inhalation paradigm to evoke anxiety symptoms in healthy subjects. J Psychopharmacol (2005) 0.84
Molecular similarity including chirality. J Mol Graph Model (2009) 0.84
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity. Bioorg Med Chem Lett (2010) 0.84
On-line monitoring of lung mechanics during spontaneous breathing: a physiological study. Respir Med (2010) 0.83
Synthesis of a potent antagonist of E-selectin. J Org Chem (2002) 0.83
Total synthesis of the cytotoxic cyclodepsipeptide (-)-doliculide: the "ester" effect in acyclic 1,3-induction of deoxypropionates. Proc Natl Acad Sci U S A (2004) 0.83
In vitro metabolism of the glucagon-like peptide-1 (GLP-1)-derived metabolites GLP-1(9-36)amide and GLP-1(28-36)amide in mouse and human hepatocytes. Drug Metab Dispos (2013) 0.83
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats. Bioorg Med Chem Lett (2010) 0.83
Inhibitors of PIM-1 kinase: a computational analysis of the binding free energies of a range of imidazo [1,2-b] pyridazines. J Chem Inf Model (2010) 0.83
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization. Bioorg Med Chem Lett (2010) 0.83
Enzyme-activated surfactants for dispersion of carbon nanotubes. Small (2009) 0.82
PF-03882845, a non-steroidal mineralocorticoid receptor antagonist, prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy. Front Pharmacol (2013) 0.82
Drug metabolites as cytochrome p450 inhibitors: a retrospective analysis and proposed algorithm for evaluation of the pharmacokinetic interaction potential of metabolites in drug discovery and development. Drug Metab Dispos (2013) 0.82
Analysis of Two Outbreaks of Scrub Typhus in Rajasthan: A Clinico-epidemiological Study. J Assoc Physicians India (2014) 0.81
Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma. Chem Res Toxicol (2011) 0.81
Pharmacokinetics, metabolism, and excretion of torcetrapib, a cholesteryl ester transfer protein inhibitor, in humans. Drug Metab Dispos (2008) 0.81
Comparison of the bioactivation potential of the antidepressant and hepatotoxin nefazodone with aripiprazole, a structural analog and marketed drug. Drug Metab Dispos (2008) 0.80
Characterization of T-5 N-oxide formation as the first highly selective measure of CYP3A5 activity. Drug Metab Dispos (2013) 0.80
Utility of MetaSite in improving metabolic stability of the neutral indomethacin amide derivative and selective cyclooxygenase-2 inhibitor 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)-N-phenethyl-acetamide. Drug Metab Dispos (2009) 0.80
Mechanism-based inactivation of human recombinant P450 2C9 by the nonsteroidal anti-inflammatory drug suprofen. Drug Metab Dispos (2003) 0.80
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists. Bioorg Med Chem Lett (2009) 0.80
Practical approaches to resolving reactive metabolite liabilities in early discovery. Drug Metab Rev (2014) 0.79
Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2). J Med Chem (2012) 0.79
The non-covalent functionalisation of carbon nanotubes studied by density functional and semi-empirical molecular orbital methods including dispersion corrections. Phys Chem Chem Phys (2007) 0.79
Pharmacokinetics and metabolism of the reactive oxygen scavenger alpha-phenyl-N-tert-butylnitrone in the male Sprague-Dawley rat. Drug Metab Dispos (2003) 0.79
Biaryl piperidines as potent and selective delta opioid receptor ligands. Bioorg Med Chem Lett (2009) 0.78
Antimalarial mannoxanes: hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action. ChemMedChem (2011) 0.78
Metabolism and transporter-mediated drug-drug interactions of the endothelin-A receptor antagonist CI-1034. Chem Biol Interact (2005) 0.78
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119. J Med Chem (2012) 0.78
Studies on the metabolism of the novel, selective cyclooxygenase-2 inhibitor indomethacin phenethylamide in rat, mouse, and human liver microsomes: identification of active metabolites. Drug Metab Dispos (2004) 0.78
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorg Med Chem Lett (2009) 0.78
Udp-glucuronosyltransferase 2b7 is the major enzyme responsible for gemcabene glucuronidation in human liver microsomes. Drug Metab Dispos (2005) 0.78
Pharmacodynamic model of parathyroid hormone modulation by a negative allosteric modulator of the calcium-sensing receptor. AAPS J (2011) 0.78
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor. Bioorg Med Chem Lett (2011) 0.78
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors. Bioorg Med Chem Lett (2012) 0.77
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation. Bioorg Med Chem Lett (2008) 0.77
Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro. Chem Res Toxicol (2011) 0.77
In vitro screening techniques for reactive metabolites for minimizing bioactivation potential in drug discovery. Curr Drug Metab (2008) 0.77