Amit S. Kalgutkar: search on Z-Library

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51

Elucidation of the biochemical basis for a clinical drug–drug interaction between atorvastatin and 5-( N -(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid (CP-778 875), a subtype selective agonist of the peroxisome proliferator-activated receptor alpha

Kalgutkar, Amit S., Chen, Danny, Varma, Manthena V., Feng, Bo, Terra, Steven G., Scialis, Renato J., Rotter, Charles J., Frederick, Kosea S., West, Mark A., Goosen, Theunis C., Gosset, James R., Walsk

Journal:

Year:

2013

Language:

english

File:

PDF, 349 KB

english, 2013

52

Novel 4-(Aryloxy)tetrahydropyridine Analogs of MPTP as Monoamine Oxidase A and B Substrates

Kalgutkar, Amit S., Castagnoli, Kay, Hall, Andrea, Castagnoli, Neal

Journal:

Journal of Medicinal Chemistry

Year:

1994

Language:

english

File:

PDF, 810 KB

english, 1994

53

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Case Studies on Eliminating/Reducing Reactive Metabolite Formation in Drug Discovery

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 570 KB

english, 2012

54

Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): Structure–activity relationships and strategies for the elimination of reactive metabolite formation

Daniel P. Walker, F. Christopher Bi, Amit S. Kalgutkar, Jonathan N. Bauman, Sabrina X. Zhao, John R. Soglia, Gary E. Aspnes, Daniel W. Kung, Jacquelyn Klug-McLeod, Michael P. Zawistoski, Molly A. McGl

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 345 KB

english, 2008

55

Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors

Amit S Kalgutkar, Scott W Rowlinson, Brenda C Crews, Lawrence J Marnett

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2002

Language:

english

File:

PDF, 107 KB

english, 2002

56

Drug discovery for a new generation of covalent drugs

Kalgutkar, Amit S, Dalvie, Deepak K

Journal:

Expert Opinion on Drug Discovery

Year:

2012

Language:

english

File:

PDF, 707 KB

english, 2012

57

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Mitigating Toxicity Risks with Affinity Labeling Drug Candidates

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 253 KB

english, 2012

58

Cyclooxygenase 2 inhibitors: discovery, selectivity and the future

Lawrence J. Marnett, Amit S. Kalgutkar

Journal:

Trends in Pharmacological Sciences

Year:

1999

Language:

english

File:

PDF, 364 KB

english, 1999

59

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Dealing with Reactive Metabolite-Positive Compounds in Drug Discovery

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 291 KB

english, 2012

60

Structural Alerts, Reactive Metabolites, and Protein Covalent Binding: How Reliable Are These Attributes as Predictors of Drug Toxicity?

Amit S. Kalgutkar, Mary T. Didiuk

Journal:

Chemistry & Biodiversity

Year:

2009

Language:

english

File:

PDF, 308 KB

english, 2009

61

Metabolic activation in drug-induced liver injury

Leung, Louis, Kalgutkar, Amit S., Obach, R. Scott

Journal:

Drug Metabolism Reviews

Year:

2012

Language:

english

File:

PDF, 1.18 MB

english, 2012

62

Discovery of a Clinical Candidate from the Structurally Unique Dioxa-bicyclo[3.2.1]octane Class of Sodium-Dependent Glucose Cotransporter 2 Inhibitors

Mascitti, Vincent, Maurer, Tristan S., Robinson, Ralph P., Bian, Jianwei, Boustany-Kari, Carine M., Brandt, Thomas, Collman, Benjamin M., Kalgutkar, Amit S., Klenotic, Michelle K., Leininger, Michael

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 1.66 MB

english, 2011

63

Pharmacokinetics and Metabolism in Drug Design (SMITH:PHARMACOKINETICS 3E O-BK) || Metabolic (Hepatic) Clearance

Smith, Dennis A., Allerton, Charlotte, Kalgutkar, Amit S., van de Waterbeemd, Han, Walker, Don K.

Year:

2012

Language:

english

File:

PDF, 386 KB

english, 2012

64

Ester and Amide Derivatives of the Nonsteroidal Antiinflammatory Drug, Indomethacin, as Selective Cyclooxygenase-2 Inhibitors

Kalgutkar, Amit S., Marnett, Alan B., Crews, Brenda C., Remmel, Rory P., Marnett, Lawrence J.

Journal:

Journal of Medicinal Chemistry

Year:

2000

Language:

english

File:

PDF, 587 KB

english, 2000

65

Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility

Kalgutkar, Amit S., Frederick, Kosea S., Hatch, Heather L., Ambler, Catherine M., Perry, David A., Garigipati, Ravi S., Chang, George C., Lefker, Bruce A., Clark, Ronald W., Morehouse, Lee A., Francon

Journal:

Year:

2014

Language:

english

File:

PDF, 1.08 MB

english, 2014

66

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Managing IADRs - a Risk-Benefit Analysis

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 163 KB

english, 2012

67

Nicotinic acid transport into human liver involves organic anion transporter 2 (SLC22A7)

Mathialagan, Sumathy, Bi, Yi-an, Costales, Chester, Kalgutkar, Amit S., David Rodrigues, A., Varma, Manthena V.S.

Journal:

Biochemical Pharmacology

Year:

2020

Language:

english

File:

PDF, 1.06 MB

english, 2020

68

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Intrinsically Electrophilic Compounds as a Liability in Drug Discovery

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 242 KB

english, 2012

69

Structural attributes influencing unbound tissue distribution

Orozco, Christine C., Atkinson, Karen, Ryu, Sangwoo, Chang, George, Keefer, Christopher, Lin, Jian, Riccardi, Keith, Mongillo, Robert K., Tess, David, Filipski, Kevin J., Kalgutkar, Amit S., Litchfiel

Journal:

European Journal of Medicinal Chemistry

Year:

2019

Language:

english

File:

PDF, 4.66 MB

english, 2019

70

Bioactivation of Phencyclidine in Rat and Human Liver Microsomes and Recombinant P450 2B Enzymes: Evidence for the Formation of a Novel Quinone Methide Intermediate

Driscoll, James P., Kornecki, Katherine, Wolkowski, Joanna P., Chupak, Lou, Kalgutkar, Amit S., O’Donnell, John P.

Journal:

Chemical Research in Toxicology

Year:

2007

Language:

english

File:

PDF, 225 KB

english, 2007

71

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Role of Reactive Metabolites in Pharmacological Action

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 621 KB

english, 2012

72

Intrinsic Electrophilicity of a 4-Substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine Derivative: Structural Characterization of Glutathione Conjugates in Vitro

Kalgutkar, Amit S., Mascitti, Vincent, Sharma, Raman, Walker, Gregory W., Ryder, Tim, McDonald, Thomas S., Chen, Yue, Preville, Cathy, Basak, Arindrajit, McClure, Kim F., Kohrt, Jeffrey T., Robinson,

Journal:

Chemical Research in Toxicology

Year:

2011

Language:

english

File:

PDF, 1.05 MB

english, 2011

73

Identification of a novel conformationally constrained glucagon receptor antagonist

Lee, Esther C.Y., Tu, Meihua, Stevens, Benjamin D., Bian, Jianwei, Aspnes, Gary, Perreault, Christian, Sammons, Matthew F., Wright, Stephen W., Litchfield, John, Kalgutkar, Amit S., Sharma, Raman, Did

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 1.35 MB

english, 2014

74

Pharmacokinetics and metabolism studies on the glucagon-like peptide-1 (GLP-1)-derived metabolite GLP-1(9-36)amide in male Beagle dogs

Eng, Heather, Sharma, Raman, McDonald, Thomas S., Landis, Margaret S., Stevens, Benjamin D., Kalgutkar, Amit S.

Journal:

Year:

2014

Language:

english

File:

PDF, 246 KB

english, 2014

75

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Bioactivation and Natural Products

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 335 KB

english, 2012

76

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

Scott M. Peterman, Nicholas Duczak Jr, Amit S. Kalgutkar, Mary E. Lame, John R. Soglia

Journal:

Journal of the American Society for Mass Spectrometry

Year:

2006

Language:

english

File:

PDF, 451 KB

english, 2006

77

Pharmacokinetics and Metabolism in Drug Design (SMITH:PHARMACOKINETICS 3E O-BK) || ADME Screening

Smith, Dennis A., Allerton, Charlotte, Kalgutkar, Amit S., van de Waterbeemd, Han, Walker, Don K.

Year:

2012

Language:

english

File:

PDF, 169 KB

english, 2012

78

Discovery Tactics To Mitigate Toxicity Risks Due to Reactive Metabolite Formation with 2-(2-Hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3- d ]pyrimidin-4(3 H )-one Derivatives, Potent Calcium-Sensing Receptor Antagonists and Clinical Candidate(s) for the Treatment of Osteoporosis

Kalgutkar, Amit S., Griffith, David A., Ryder, Tim, Sun, Hao, Miao, Zhuang, Bauman, Jonathan N., Didiuk, Mary T., Frederick, Kosea S., Zhao, Sabrina X., Prakash, Chandra, Soglia, John R., Bagley, Scot

Journal:

Chemical Research in Toxicology

Year:

2010

Language:

english

File:

PDF, 427 KB

english, 2010

79

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

Soglia, John R., Contillo, Leonard G., Kalgutkar, Amit S., Zhao, Sabrina, Hop, Cornelis E. C. A., Boyd, James G., Cole, Mark J.

Journal:

Chemical Research in Toxicology

Year:

2006

Language:

english

File:

PDF, 301 KB

english, 2006

80

Synthesis of novel MPTP analogs as potential monoamine oxidase B (MAO-B) inhibitors

Kalgutkar, Amit S., Castagnoli, Neal

Journal:

Journal of Medicinal Chemistry

Year:

1992

Language:

english

File:

PDF, 1.32 MB

english, 1992

81

Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism

Ahn, Kay, Brown, Matthew F., Boehm, Markus, Calloway, Jessica, Che, Ye, Chen, Jinshan M., Fennell, Kimberly, Geoghegan, Kieran F, Gilbert, Adam M., Gutierrez, Jemy A., Kalgutkar, Amit S., Lanba, Adhir

Journal:

ACS Chemical Biology

Year:

2016

Language:

english

File:

PDF, 1.68 MB

english, 2016

82

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Cameron, Kimberly O., Kung, Daniel W., Kalgutkar, Amit S., Kurumbail, Ravi G., Miller, Russell, Salatto, Christopher T., Ward, Jessica, Withka, Jane M., Bhattacharya, Samit K., Boehm, Markus, Borzille

Journal:

Journal of Medicinal Chemistry

Year:

2016

Language:

english

File:

PDF, 1.18 MB

english, 2016

83

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue

Price, David A., Eng, Heather, Farley, Kathleen A., Goetz, Gilles H., Huang, Yong, Jiao, Zhaodong, Kalgutkar, Amit S., Kablaoui, Natasha M., Khunte, Bhagyashree, Liras, Spiros, Limberakis, Chris, Math

Journal:

Organic & Biomolecular Chemistry

Year:

2017

Language:

english

File:

PDF, 844 KB

english, 2017

84

In Vitro Metabolism and Covalent Binding of Enol-Carboxamide Derivatives and Anti-Inflammatory Agents Sudoxicam and Meloxicam: Insights into the Hepatotoxicity of Sudoxicam

Obach, R. Scott, Kalgutkar, Amit S., Ryder, Tim F., Walker, Gregory S.

Journal:

Chemical Research in Toxicology

Year:

2008

Language:

english

File:

PDF, 613 KB

english, 2008

85

Predicting metabolism-mediated toxicities of drug candidates

Kalgutkar, Amit S.S.

Journal:

Drug Metabolism and Pharmacokinetics

Year:

2018

Language:

english

File:

PDF, 44 KB

english, 2018

86

COX-2 Inhibitors Modulate IL-12 Signaling Through JAK-STAT Pathway Leading to Th1 Response in Experimental Allergic Encephalomyelitis

Gladson Muthian, Himanshu P. Raikwar, Caroline Johnson, Johnson Rajasingh, Amit Kalgutkar, Lawrence J. Marnett, John J. Bright

Journal:

Journal of Clinical Immunology

Year:

2006

Language:

english

File:

PDF, 730 KB

english, 2006

87

Mechanism-Based Inactivation of Cytochrome P450 Enzymes: Chemical Mechanisms, Structure-Activity Relationships and Relationship to Clinical Drug-Drug Interactions and Idiosyncratic Adverse Drug Reactions

Amit S. Kalgutkar, Bentham Science Publisher, R. Scott Obach, Bentham Science Publisher, Tristan S. Maurer, Bentham Science Publisher

Journal:

Current Drug Metabolism

Year:

2007

Language:

english

File:

PDF, 1.02 MB

english, 2007

88

Elucidation of parmacokinetics of PF-04937319, a partial glucokinase activator, and its disproportionate n-demethylated metabolite in chimeric mice with humanized livers

Ito, Satoshi, Chijiwa, Hiroyuki, Okuzono, Takeshi, Ishiguro, Tomohiro, Yamamoto, Yosuke, Nishinoaki, Sho, Kuronuma, Miyuki, Suemizu, Hiroshi, Kalgutkar, Amit S., Kamimura, Hidetaka, Ninomiya, Shin-ich

Journal:

Drug Metabolism and Pharmacokinetics

Year:

2017

Language:

english

File:

PDF, 69 KB

english, 2017

89

Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase (ACC) Inhibitors Through Liver Targeting

Huard, Kim, Smith, Aaron C., Cappon, Gregg D, Dow, Robert L., Edmonds, David J., El-Kattan, Ayman, Esler, William P, Fernando, Dilinie P., Griffith, David A., Kalgutkar, Amit S., Ross, Trenton, Bagley

Journal:

Journal of Medicinal Chemistry

Year:

2020

File:

PDF, 427 KB

2020

90

Selective inhibitors of monoamine oxidase (MAO-A and MAO-B) as probes of its catalytic site and mechanism

Amit S. Kalgutkar, Neal Castagnoli Jr., Bernard Testa

Journal:

Medicinal Research Reviews

Year:

1995

Language:

english

File:

PDF, 3.38 MB

english, 1995

91

Structure–activity relationships of triazolopyridine oxazole p38 inhibitors: Identification of candidates for clinical development

Kim F. McClure, Michael A. Letavic, Amit S. Kalgutkar, Christopher A. Gabel, Laurent Audoly, John T. Barberia, John F. Braganza, Demetrius Carter, Thomas J. Carty, Santo R. Cortina, Mark A. Dombroski,

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 141 KB

english, 2006

92

Handling reactive metabolite positives in drug discovery: What has retrospective structure–toxicity analyses taught us?

Amit S. Kalgutkar

Journal:

Chemico-Biological Interactions

Year:

2011

Language:

english

File:

PDF, 367 KB

english, 2011

93

Pharmacokinetics and Metabolism in Drug Design (SMITH:PHARMACOKINETICS 3E O-BK) || Pharmacokinetics

Smith, Dennis A., Allerton, Charlotte, Kalgutkar, Amit S., van de Waterbeemd, Han, Walker, Don K.

Year:

2012

Language:

english

File:

PDF, 187 KB

english, 2012

94

Biotransformation Reactions of Five-Membered Aromatic Heterocyclic Rings

Dalvie, Deepak K., Kalgutkar, Amit S., Khojasteh-Bakht, S. Cyrus, Obach, R. Scott, O'Donnell, John P.

Journal:

Chemical Research in Toxicology

Year:

2002

Language:

english

File:

PDF, 447 KB

english, 2002

95

Induction of Human Cytochrome P450 3A4 by the Irreversible Myeloperoxidase Inactivator PF-06282999 is Mediated by the Pregnane X Receptor

Moscovitz, Jamie E., Lin, Zhiwu, Johnson, Nathaniel, Tu, Meihua, Goosen, Theunis, Weng, Yan, Kalgutkar, Amit S.

Journal:

Year:

2017

Language:

english

File:

PDF, 765 KB

english, 2017

96

Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38α inhibitor: identification of an active metabolite in preclinical species and human liver microsomes

Amit S. Kalgutkar, Heather L. Hatch, Frederick Kosea, Hang T. Nguyen, Edna F. Choo, Kim F. McClure, Timothy J. Taylor, Kirk R. Henne, Alexander V. Kuperman, Mark A. Dombroski, Michael A. Letavic

Journal:

Biopharmaceutics & Drug Disposition

Year:

2006

Language:

english

File:

PDF, 406 KB

english, 2006

97

Pharmacodynamic Model of Parathyroid Hormone Modulation by a Negative Allosteric Modulator of the Calcium-Sensing Receptor

Anson K. Abraham, Tristan S. Maurer, Amit S. Kalgutkar, Xiang Gao, Mei Li, David R. Healy, Donna N. Petersen, David A. Griffith, Donald E. Mager

Journal:

The AAPS Journal

Year:

2011

Language:

english

File:

PDF, 231 KB

english, 2011

98

Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB. O-BK) || Role of Reactive Metabolites in Genotoxicity

Kalgutkar, Amit S., Dalvie, Deepak, Obach, R. Scott, Smith, Dennis A.

Year:

2012

Language:

english

File:

PDF, 532 KB

english, 2012

99

Practical approaches to resolving reactive metabolite liabilities in early discovery

Dalvie, Deepak, Kalgutkar, Amit S., Chen, Weichao

Journal:

Drug Metabolism Reviews

Year:

2015

Language:

english

File:

PDF, 716 KB

english, 2015

100

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-activated Protein Kinase (AMPK)

Edmonds, David J., Kung, Daniel W., Kalgutkar, Amit S., Filipski, Kevin J., Ebner, David C, Cabral, Shawn, Smith, Aaron C., Aspnes, Gary E, Bhattacharya, Samit K., Borzilleri, Kris A, Brown, Janice A.

Journal:

Journal of Medicinal Chemistry

Year:

2018

Language:

english

File:

PDF, 787 KB

english, 2018

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