Amit S. Kalgutkar: search on Z-Library

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1

Metabolism and Excretion of (S)-6-(3-Cyclopentyl-2-(4-trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid (PF-04991532), a Hepatoselective Glucokinase Activator, in Humans: Confirmation of the MIST Potential Noted in First-in-Human Metabolite Scouting Studies

Sharma, Raman, Bergman, Arthur, Litchfield, John, Atkinson, Karen, Kazierad, David J., Kalgutkar, Amit S.

Journal:

Year:

2019

Language:

english

File:

PDF, 1.11 MB

english, 2019

2

Toxicophores, reactive metabolites and drug safety: when is it a cause for concern?

Kalgutkar, Amit S, Fate, Gwendolyn, Didiuk, Mary T, Bauman, Jonathan

Journal:

Expert Review of Clinical Pharmacology

Year:

2008

Language:

english

File:

PDF, 777 KB

english, 2008

3

Liabilities Associated with the Formation of “Hard” Electrophiles in Reactive Metabolite Trapping Screens

Kalgutkar, Amit S.

Journal:

Chemical Research in Toxicology

Year:

2016

Language:

english

File:

PDF, 736 KB

english, 2016

4

Predicting Toxicities of Reactive Metabolite–Positive Drug Candidates

Kalgutkar, Amit S., Dalvie, Deepak

Journal:

Annual Review of Pharmacology

Year:

2015

Language:

english

File:

PDF, 1.01 MB

english, 2015

5

Interactions of Nitrogen-Containing Xenobiotics with Monoamine Oxidase (MAO) Isozymes A and B: SAR Studies on MAO Substrates and Inhibitors

Kalgutkar, Amit S., Dalvie, Deepak K., Castagnoli,, Neal, Taylor, Timothy J.

Journal:

Chemical Research in Toxicology

Year:

2001

Language:

english

File:

PDF, 292 KB

english, 2001

6

Establishing Transcriptional Signatures to Differentiate PXR-, CAR- and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes

Moscovitz, Jamie E, Kalgutkar, Amit S., Nulick, Kelly, Johnson, Nathaniel, Lin, Zhiwu, Goosen, Theunis C, Weng, Yan

Journal:

Journal of Pharmacology and Experimental Therapeutics

Year:

2018

Language:

english

File:

PDF, 1.11 MB

english, 2018

7

NADPH-Dependent Covalent Binding of [ 3 H]Paroxetine to Human Liver Microsomes and S-9 Fractions: Identification of an Electrophilic Quinone Metabolite of Paroxetine

Zhao, Sabrina X., Dalvie, Deepak K., Kelly, Joan M., Soglia, John R., Frederick, Kosea S., Smith, Evan B., Obach, R. Scott, Kalgutkar, Amit S.

Journal:

Chemical Research in Toxicology

Year:

2007

Language:

english

File:

PDF, 225 KB

english, 2007

8

On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds

White, Tina R, Renzelman, Chad M, Rand, Arthur C, Rezai, Taha, McEwen, Cayla M, Gelev, Vladimir M, Turner, Rushia A, Linington, Roger G, Leung, Siegfried S F, Kalgutkar, Amit S

Journal:

Nature Chemical Biology

Year:

2011

Language:

english

File:

PDF, 622 KB

english, 2011

9

Minimising the potential for metabolic activation in drug discovery

Kalgutkar, Amit S, Soglia, John R

Journal:

Expert Opinion on Drug Metabolism & Toxicology

Year:

2005

Language:

english

File:

PDF, 738 KB

english, 2005

10

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

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

Year:

2012

Language:

english

File:

PDF, 166 KB

english, 2012

11

Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB. O-BK) || Pathways of Reactive Metabolite Formation with Toxicophores/-Structural Alerts

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

Year:

2012

Language:

english

File:

PDF, 373 KB

english, 2012

12

A sensitive method for the quantitation of the peptide-based glucagon-like peptide-1 receptor agonist liraglutide in plasma using microfluidics chromatography tandem MS

King-Ahmad, Amanda J, Kalgutkar, Amit S, Niosi, Mark, Eng, Heather, Holliman, Christopher

Journal:

Year:

2018

Language:

english

File:

PDF, 546 KB

english, 2018

13

THE EFFECTIVE APPLICATION OF METABOLITE PROFILING IN DRUG DESIGN AND DISCOVERY

Cerny, Matthew, Kalgutkar, Amit S., Obach, R. Scott, Sharma, Raman, Spracklin, Douglas K., Walker, Gregory S

Journal:

Journal of Medicinal Chemistry

Year:

2020

Language:

english

File:

PDF, 939 KB

english, 2020

14

ChemInform Abstract: Covalent Modification of Cyclooxygenase-2 (COX-2) by 2-Acetoxyphenyl Alkyl Sulfides, a New Class of Selective COX-2 Inactivators.

Amit S. Kalgutkar, Kevin R. Kozak, Brenda C. Crews, G. Phillip Jr. Hochgesang, Lawrence J. Marnett

Journal:

Year:

1999

File:

PDF, 32 KB

1999

15

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

John Litchfield, Raman Sharma, Karen Atkinson, Kevin J. Filipski, Stephen W. Wright, Jeffrey A. Pfefferkorn, Beijing Tan, Rachel E. Kosa, Benjamin Stevens, Meihua Tu, Amit S. Kalgutkar

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 689 KB

english, 2010

16

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

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

Year:

2012

Language:

english

File:

PDF, 222 KB

english, 2012

17

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

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

Year:

2012

Language:

english

File:

PDF, 406 KB

english, 2012

18

CCR2 receptor blockade alters blood monocyte subpopulations but does not affect atherosclerotic lesions in apoE−/− mice

Robert J. Aiello, Bret D. Perry, Patricia-Ann Bourassa, Andrew Robertson, Weifan Weng, Delvin R. Knight, Andrew H. Smith, Kosea S. Frederick, Amit Kalgutkar, Ronald P. Gladue

Journal:

Atherosclerosis

Year:

2010

Language:

english

File:

PDF, 1.18 MB

english, 2010

19

Design, Synthesis, and Biochemical Evaluation of N -Substituted Maleimides as Inhibitors of Prostaglandin Endoperoxide Synthases †

Kalgutkar, Amit S., Crews, Brenda C., Marnett, Lawrence J.

Journal:

Journal of Medicinal Chemistry

Year:

1996

Language:

english

File:

PDF, 613 KB

english, 1996

20

Optimization of amide-based EP3 receptor antagonists

Lee, Esther C.Y., Futatsugi, Kentaro, Arcari, Joel T., Bahnck, Kevin, Coffey, Steven B., Derksen, David R., Kalgutkar, Amit S., Loria, Paula M., Sharma, Raman

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2016

Language:

english

File:

PDF, 1.95 MB

english, 2016

21

Selective Activation of AMPK β 1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy

Salatto, Christopher T., Miller, Russell A., Cameron, Kimberly O., Cokorinos, Emily, Reyes, Allan, Ward, Jessica, Calabrese, Matthew F., Kurumbail, Ravi G., Rajamohan, Francis, Kalgutkar, Amit S., Tes

Journal:

Journal of Pharmacology and Experimental Therapeutics

Year:

2017

Language:

english

File:

PDF, 1.33 MB

english, 2017

22

Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: Retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct detection using linear ion trap/orbitrap mass spectrometry

Hao Sun, Raman Sharma, Jonathan Bauman, Daniel P. Walker, Gary E. Aspnes, Michael P. Zawistoski, Amit S. Kalgutkar

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 426 KB

english, 2009

23

Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB. O-BK) || Retrospective Analysis of Structure-Toxicity Relationships of Drugs

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

Year:

2012

Language:

english

File:

PDF, 184 KB

english, 2012

24

Metabolism-guided drug design

Stepan, Antonia F., Mascitti, Vincent, Beaumont, Kevin, Kalgutkar, Amit S.

Journal:

Year:

2013

Language:

english

File:

PDF, 1.06 MB

english, 2013

25

Selective cyclooxygenase-2 inhibitors as non-ulcerogenic anti-inflammatory agents

Kalgutkar, Amit S

Journal:

Expert Opinion on Therapeutic Patents

Year:

1999

Language:

english

File:

PDF, 217 KB

english, 1999

26

Rapid Inactivation of Prostaglandin Endoperoxide Synthases by N-(Carboxyalkyl)maleimides

Kalgutkar, Amit S., Marnett, Lawrence J.

Journal:

Year:

1994

Language:

english

File:

PDF, 437 KB

english, 1994

27

N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a “chemical knock-out equivalent” to assess the impact of efflux transporters on oral drug absorption in the rat

Amit S. Kalgutkar, Kosea S. Frederick, Jonathan Chupka, Bo Feng, Sarah Kempshall, Rochelle J. Mireles, Katherine S. Fenner, Matthew D. Troutman

Journal:

Journal of Pharmaceutical Sciences

Year:

2009

Language:

english

File:

PDF, 193 KB

english, 2009

28

The discovery of novel calcium sensing receptor negative allosteric modulators

Gayatri Balan, Jonathan Bauman, Samit Bhattacharya, Mayda Castrodad, David R. Healy, Michael Herr, Paul Humphries, Sandra Jennings, Amit S. Kalgutkar, Brendon Kapinos, Vishal Khot, Kimberly Lazarra, M

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 769 KB

english, 2009

29

A Rational Chemical Intervention Strategy To Circumvent Bioactivation Liabilities Associated with a Nonpeptidyl Thrombopoietin Receptor Agonist Containing a 2-Amino-4-arylthiazole Motif

Kalgutkar, Amit S., Driscoll, James, Zhao, Sabrina X., Walker, Gregory S., Shepard, Richard M., Soglia, John R., Atherton, James, Yu, Linning, Mutlib, Abdul E., Munchhof, Michael J.

Journal:

Chemical Research in Toxicology

Year:

2007

Language:

english

File:

PDF, 426 KB

english, 2007

30

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products

Bockus, Andrew T., Lexa, Katrina W., Pye, Cameron R., Kalgutkar, Amit S., Gardner, Jarret W., Hund, Kathryn C. R., Hewitt, William M., Schwochert, Joshua A., Glassey, Emerson, Price, David A., Mathiow

Journal:

Journal of Medicinal Chemistry

Year:

2015

Language:

english

File:

PDF, 1.31 MB

english, 2015

31

Tracking Where the O’s Go

Kalgutkar, Amit S.

Journal:

ACS Central Science

Year:

2015

Language:

english

File:

PDF, 710 KB

english, 2015

32

ChemInform Abstract: 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:

Year:

2010

File:

PDF, 15 KB

2010

33

On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin

Mascitti, Vincent, Thuma, Benjamin A., Smith, Aaron C., Robinson, Ralph P., Brandt, Thomas, Kalgutkar, Amit S., Maurer, Tristan S., Samas, Brian, Sharma, Raman

Journal:

Year:

2013

Language:

english

File:

PDF, 967 KB

english, 2013

34

Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4

Amit S. Kalgutkar, Kirk R. Henne, Mary E. Lame, Alfin D.N. Vaz, Claire Collin, John R. Soglia, Sabrina X. Zhao, Cornelis E.C.A. Hop

Journal:

Chemico-Biological Interactions

Year:

2005

Language:

english

File:

PDF, 461 KB

english, 2005

35

Examination of the Human Cytochrome P4503A4 Induction Potential of PF-06282999, an Irreversible Myeloperoxidase Inactivator: Integration of Preclinical, In Silico, and Biomarker Methodologies in the Prediction of the Clinical Outcome

Dong, Jennifer Q., Gosset, James R., Fahmi, Odette A., Lin, Zhiwu, Chabot, Jeffrey R., Terra, Steven G., Le, Vu, Chidsey, Kristin, Nouri, Parya, Kim, Albert, Buckbinder, Leonard, Kalgutkar, Amit S.

Journal:

Drug Metabolism and Disposition

Year:

2017

Language:

english

File:

PDF, 1.62 MB

english, 2017

36

Discovery of a Novel Small Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis

Menhaji-Klotz, Elnaz, Hesp, Kevin D., Londregan, Allyn Timothy, Kalgutkar, Amit S., Piotrowski, David W., Boehm, Markus, Song, Kun, Ryder, Tim, Beaumont, Kevin, Jones, Rhys M, Atkinson, Karen, Brown,

Journal:

Journal of Medicinal Chemistry

Year:

2018

Language:

english

File:

PDF, 487 KB

english, 2018

37

6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577) is a Highly Selective Substrate for Glucuronidation by Uridine Diphosphoglucuronosyl Transferase (UGT) 1A1, Relative to b-Estradiol

Lapham, Kimberly, Lin, Jian, Novak, Jonathan, Orozco, Christine, Niosi, Mark, Di, Li, Goosen, Theunis C, Ryu, Sangwoo, Riccardi, Keith, Eng, Heather, Cameron, Kimberly O., Kalgutkar, Amit S.

Journal:

Drug Metabolism and Disposition

Year:

2018

Language:

english

File:

PDF, 1.18 MB

english, 2018

38

A Comprehensive Listing of Bioactivation Pathways of Organic Functional Groups

Kalgutkar, Amit, Gardner, Iain, Obach, R., Shaffer, Christopher, Callegari, Ernesto, Henne, Kirk, Mutlib, Abdul, Dalvie, Deepak, Lee, Jae, Nakai, Yasuhiro, O'Donnell, John, Boer, Jason, Harriman, Shaw

Journal:

Current Drug Metabolism

Year:

2005

Language:

english

File:

PDF, 483 KB

english, 2005

39

Discovery of potent and orally bioavailable macrocyclic peptide-peptoid hybrid CXCR7 modulators.

Boehm, Markus, Beaumont, Kevin, Jones, Rhys M, Kalgutkar, Amit S., Zhang, Liying, Atkinson, Karen, Bai, Guoyun, Brown, Janice A., Eng, Heather, Goetz, Gilles H., Holder, Brian R, Khunte, Bhagyashree,

Journal:

Journal of Medicinal Chemistry

Year:

2017

Language:

english

File:

PDF, 899 KB

english, 2017

40

Pharmacokinetics and Metabolism in Drug Design Volume 5931 (SMITH:PHARMACOKINETICS 3E O-BK) || Predicting Human Pharmacokinetics

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

Year:

2012

Language:

english

File:

PDF, 160 KB

english, 2012

41

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

Obach, R. Scott, Kalgutkar, Amit S., Soglia, John R., Zhao, Sabrina X.

Journal:

Chemical Research in Toxicology

Year:

2008

Language:

english

File:

PDF, 403 KB

english, 2008

42

Mechanistic Studies on the Monoamine Oxidase B Catalyzed Oxidation of 1,4-Disubstituted Tetrahydropyridines

Kuttab, Simon, Kalgutkar, Amit, Castagnoli, Neal

Journal:

Chemical Research in Toxicology

Year:

1994

Language:

english

File:

PDF, 667 KB

english, 1994

43

Simulation of human plasma concentration–time profiles of the partial glucokinase activator PF-04937319 and its disproportionate N-demethylated metabolite using humanized chimeric mice and semi-physiological pharmacokinetic modeling

Kamimura, Hidetaka, Ito, Satoshi, Chijiwa, Hiroyuki, Okuzono, Takeshi, Ishiguro, Tomohiro, Yamamoto, Yosuke, Nishinoaki, Sho, Ninomiya, Shin-Ichi, Mitsui, Marina, Kalgutkar, Amit S., Yamazaki, Hiroshi

Journal:

Year:

2016

Language:

english

File:

PDF, 832 KB

english, 2016

44

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Origin and Historical Perspective on Reactive Metabolites

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

Year:

2012

Language:

english

File:

PDF, 113 KB

english, 2012

45

Indolyl esters and amides related to indomethacin are selective COX-2 inhibitors

Amit S. Kalgutkar, Brenda C. Crews, Sam Saleh, Daniel Prudhomme, Lawrence J. Marnett

Journal:

Bioorganic & Medicinal Chemistry

Year:

2005

Language:

english

File:

PDF, 321 KB

english, 2005

46

Revisiting N-to-O Acyl Shift for Synthesis of Natural Product-like Cyclic Depsipeptides

Schwochert, Joshua, Pye, Cameron, Ahlbach, Christopher, Abdollahian, Yashar, Farley, Kathleen, Khunte, Bhagyashree, Limberakis, Chris, Kalgutkar, Amit S., Eng, Heather, Shapiro, Michael J., Mathiowetz

Journal:

Organic Letters

Year:

2014

Language:

english

File:

PDF, 1013 KB

english, 2014

47

Predicting toxicities of reactive metabolite-positive drug candidates

Kalgutkar, Amit S.

Journal:

Drug Metabolism and Pharmacokinetics

Year:

2017

Language:

english

File:

PDF, 43 KB

english, 2017

48

[Methods and Principles in Medicinal Chemistry] Reactive Drug Metabolites (KALGUTKAR:REACTIVE METAB.) || Experimental Approaches to Reactive Metabolite Detection

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

Year:

2012

Language:

english

File:

PDF, 189 KB

english, 2012

49

Is there enough evidence to classify cycloalkyl amine substituents as structural alerts?

Kalgutkar, Amit S., Driscoll, James P.

Journal:

Biochemical Pharmacology

Year:

2020

Language:

english

File:

PDF, 1.30 MB

english, 2020

50

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

Stepan, Antonia F., Walker, Daniel P., Bauman, Jonathan, Price, David A., Baillie, Thomas A., Kalgutkar, Amit S., Aleo, Michael D.

Journal:

Chemical Research in Toxicology

Year:

2011

Language:

english

File:

PDF, 3.56 MB

english, 2011

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