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Items: 48

1.

Design, synthesis, structure-function relationship, bioconversion, and pharmacokinetic evaluation of ertapenem prodrugs.

Singh SB, Rindgen D, Bradley P, Suzuki T, Wang N, Wu H, Zhang B, Wang L, Ji C, Yu H, Soll RM, Olsen DB, Meinke PT, Nicoll-Griffith DA.

J Med Chem. 2014 Oct 23;57(20):8421-44. doi: 10.1021/jm500879a. Epub 2014 Oct 14.

PMID:
25265501
2.

Design, synthesis, and evaluation of prodrugs of ertapenem.

Singh SB, Rindgen D, Bradley P, Cama L, Sun W, Hafey MJ, Suzuki T, Wang N, Wu H, Zhang B, Wang L, Ji C, Yu H, Soll R, Olsen DB, Meinke PT, Nicoll-Griffith DA.

ACS Med Chem Lett. 2013 Jul 3;4(8):715-9. doi: 10.1021/ml400092n. eCollection 2013 Aug 8.

3.

Reversible cysteine protease inhibitors show promise for a Chagas disease cure.

Ndao M, Beaulieu C, Black WC, Isabel E, Vasquez-Camargo F, Nath-Chowdhury M, Massé F, Mellon C, Methot N, Nicoll-Griffith DA.

Antimicrob Agents Chemother. 2014;58(2):1167-78. doi: 10.1128/AAC.01855-13. Epub 2013 Dec 9.

4.

Using human recombinant UDP-glucuronosyltransferase isoforms and a relative activity factor approach to model total body clearance of laropiprant (MK-0524) in humans.

Gibson CR, Lu P, Maciolek C, Wudarski C, Barter Z, Rowland-Yeo K, Stroh M, Lai E, Nicoll-Griffith DA.

Xenobiotica. 2013 Dec;43(12):1027-36. doi: 10.3109/00498254.2013.791761. Epub 2013 May 3.

PMID:
23641955
5.

Use of cysteine-reactive small molecules in drug discovery for trypanosomal disease.

Nicoll-Griffith DA.

Expert Opin Drug Discov. 2012 Apr;7(4):353-66. doi: 10.1517/17460441.2012.668520. Epub 2012 Mar 6. Review.

PMID:
22458506
6.

Managing the challenge of chemically reactive metabolites in drug development.

Park BK, Boobis A, Clarke S, Goldring CE, Jones D, Kenna JG, Lambert C, Laverty HG, Naisbitt DJ, Nelson S, Nicoll-Griffith DA, Obach RS, Routledge P, Smith DA, Tweedie DJ, Vermeulen N, Williams DP, Wilson ID, Baillie TA.

Nat Rev Drug Discov. 2011 Apr;10(4):292-306. doi: 10.1038/nrd3408. Review.

PMID:
21455238
7.

The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.

Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):887-92. doi: 10.1016/j.bmcl.2009.12.083. Epub 2009 Dec 28.

PMID:
20061146
8.

Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.

Lacombe P, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Gallant M, Girard Y, Huang Z, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini JA, Masson P, Nicholson DW, Nicoll-Griffith DA, Salem M, Styhler A, Young RN.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5266-9. doi: 10.1016/j.bmcl.2009.03.105. Epub 2009 Mar 26.

PMID:
19640717
9.

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15.

PMID:
18226527
10.

Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.

Gallant M, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Huang Z, Lacombe P, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini J, Masson P, Mastracchio A, Nicholson D, Nicoll-Griffith DA, Perrier H, Salem M, Styhler A, Young RN, Girard Y.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1407-12. doi: 10.1016/j.bmcl.2008.01.004. Epub 2008 Jan 8.

PMID:
18207397
11.

High-throughput cytochrome P450 inhibition assays using laser diode thermal desorption-atmospheric pressure chemical ionization-tandem mass spectrometry.

Wu J, Hughes CS, Picard P, Letarte S, Gaudreault M, Lévesque JF, Nicoll-Griffith DA, Bateman KP.

Anal Chem. 2007 Jun 15;79(12):4657-65. Epub 2007 May 12.

PMID:
17497828
12.

Metabolic activation of indole-containing prostaglandin D2 receptor 1 antagonists: impacts of glutathione trapping and glucuronide conjugation on covalent binding.

Lévesque JF, Day SH, Chauret N, Seto C, Trimble L, Bateman KP, Silva JM, Berthelette C, Lachance N, Boyd M, Li L, Sturino CF, Wang Z, Zamboni R, Young RN, Nicoll-Griffith DA.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3038-43. Epub 2007 Mar 23.

PMID:
17418572
13.

MSE with mass defect filtering for in vitro and in vivo metabolite identification.

Bateman KP, Castro-Perez J, Wrona M, Shockcor JP, Yu K, Oballa R, Nicoll-Griffith DA.

Rapid Commun Mass Spectrom. 2007;21(9):1485-96.

PMID:
17394128
14.

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM.

J Med Chem. 2007 Feb 22;50(4):794-806.

PMID:
17300164
15.

In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites.

Nicoll-Griffith DA, Seto C, Aubin Y, Lévesque JF, Chauret N, Day S, Silva JM, Trimble LA, Truchon JF, Berthelette C, Lachance N, Wang Z, Sturino C, Braun M, Zamboni R, Young RN.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):301-4. Epub 2006 Oct 25.

PMID:
17095220
16.

Use of a fluorescent substrate for the selective quantification of rat CYP3A in the liver and the intestine.

Michaud J, Leblond FA, Naud J, Boisvert C, Desbiens K, Nicoll-Griffith DA, Pichette V.

J Pharmacol Toxicol Methods. 2007 Mar-Apr;55(2):209-13. Epub 2006 Aug 4.

PMID:
16979351
17.

Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.

Macdonald D, Mastracchio A, Perrier H, Dubé D, Gallant M, Lacombe P, Deschênes D, Roy B, Scheigetz J, Bateman K, Li C, Trimble LA, Day S, Chauret N, Nicoll-Griffith DA, Silva JM, Huang Z, Laliberté F, Liu S, Ethier D, Pon D, Muise E, Boulet L, Chan CC, Styhler A, Charleson S, Mancini J, Masson P, Claveau D, Nicholson D, Turner M, Young RN, Girard Y.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. Epub 2005 Sep 15.

PMID:
16168647
18.

A strategy for identification of drug metabolites from dried blood spots using triple-quadrupole/linear ion trap hybrid mass spectrometry.

Mauriala T, Chauret N, Oballa R, Nicoll-Griffith DA, Bateman KP.

Rapid Commun Mass Spectrom. 2005;19(14):1984-92.

PMID:
15954171
19.

Use of a benzyloxy-substituted lactone cyclooxygenase-2 inhibitor as a selective fluorescent probe for CYP3A activity in primary cultured rat and human hepatocytes.

Nicoll-Griffith DA, Chauret N, Houle R, Day SH, D'Antoni M, Silva JM.

Drug Metab Dispos. 2004 Dec;32(12):1509-15.

PMID:
15550722
20.

Detection of covalent adducts to cytochrome P450 3A4 using liquid chromatography mass spectrometry.

Bateman KP, Baker J, Wilke M, Lee J, Leriche T, Seto C, Day S, Chauret N, Ouellet M, Nicoll-Griffith DA.

Chem Res Toxicol. 2004 Oct;17(10):1356-61.

PMID:
15487896
21.

Drug-protein adducts: an industry perspective on minimizing the potential for drug bioactivation in drug discovery and development.

Evans DC, Watt AP, Nicoll-Griffith DA, Baillie TA.

Chem Res Toxicol. 2004 Jan;17(1):3-16. Review. Erratum in: Chem Res Toxicol. 2005 Nov;18(11):1777.

PMID:
14727914
22.

Retention of transporter activities in cryopreserved, isolated rat hepatocytes.

Houle R, Raoul J, Lévesque JF, Pang KS, Nicoll-Griffith DA, Silva JM.

Drug Metab Dispos. 2003 Apr;31(4):447-51.

PMID:
12642471
23.

Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.

Leblanc Y, Roy P, Wang Z, Li CS, Chauret N, Nicoll-Griffith DA, Silva JM, Aubin Y, Yergey JA, Chan CC, Riendeau D, Brideau C, Gordon R, Xu L, Webb J, Visco DM, Prasit P.

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3317-20.

PMID:
12392741
24.

Diversity in the oxidation of substrates by cytochrome P450 2D6: lack of an obligatory role of aspartate 301-substrate electrostatic bonding.

Guengerich FP, Miller GP, Hanna IH, Martin MV, Léger S, Black C, Chauret N, Silva JM, Trimble LA, Yergey JA, Nicoll-Griffith DA.

Biochemistry. 2002 Sep 10;41(36):11025-34.

PMID:
12206675
25.

Improving metabolic stability of phosphodiesterase-4 inhibitors containing a substituted catechol: prevention of reactive intermediate formation and covalent binding.

Chauret N, Guay D, Li C, Day S, Silva J, Blouin M, Ducharme Y, Yergey JA, Nicoll-Griffith DA.

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2149-52.

PMID:
12127525
26.

The use of 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin (AMMC) as a specific CYP2D6 probe in human liver microsomes.

Chauret N, Dobbs B, Lackman RL, Bateman K, Nicoll-Griffith DA, Stresser DM, Ackermann JM, Turner SD, Miller VP, Crespi CL.

Drug Metab Dispos. 2001 Sep;29(9):1196-200.

PMID:
11502727
27.

In vitro metabolism considerations, including activity testing of metabolites, in the discovery and selection of the COX-2 inhibitor etoricoxib (MK-0663).

Chauret N, Yergey JA, Brideau C, Friesen RW, Mancini J, Riendeau D, Silva J, Styhler A, Trimble LA, Nicoll-Griffith DA.

Bioorg Med Chem Lett. 2001 Apr 23;11(8):1059-62.

PMID:
11327589
28.

Reduction of animal usage by serial bleeding of mice for pharmacokinetic studies: application of robotic sample preparation and fast liquid chromatography-mass spectrometry.

Bateman KP, Castonguay G, Xu L, Rowland S, Nicoll-Griffith DA, Kelly N, Chan CC.

J Chromatogr B Biomed Sci Appl. 2001 Apr 15;754(1):245-51.

PMID:
11318421
29.

Novel enzymological profiles of human 11beta-hydroxysteroid dehydrogenase type 1.

Hult M, Nobel CS, Abrahmsen L, Nicoll-Griffith DA, Jörnvall H, Oppermann UC.

Chem Biol Interact. 2001 Jan 30;130-132(1-3):805-14.

PMID:
11306096
30.

In vitro metabolism of the COX-2 inhibitor DFU, including a novel glutathione adduct rearomatization.

Yergey JA, Trimble LA, Silva J, Chauret N, Li C, Therien M, Grimm E, Nicoll-Griffith DA.

Drug Metab Dispos. 2001 May;29(5):638-44.

PMID:
11302928
31.

Investigation of the in vitro metabolism profile of a phosphodiesterase-IV inhibitor, CDP-840: leading to structural optimization.

Li C, Chauret N, Trimble LA, Nicoll-Griffith DA, Silva JM, MacDonald D, Perrier H, Yergey JA, Parton T, Alexander RP, Warrellow GJ.

Drug Metab Dispos. 2001 Mar;29(3):232-41.

PMID:
11181489
32.

Application of rat hepatocyte culture to predict in vivo metabolic auto-induction: studies with DFP, a cyclooxygenase-2 inhibitor.

Nicoll-Griffith DA, Silva JM, Chauret N, Day S, Leblanc Y, Roy P, Yergey JA, Dixit R, Patrick D.

Drug Metab Dispos. 2001 Feb;29(2):159-65.

PMID:
11159806
33.

Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).

Nicoll-Griffith DA, Yergey JA, Trimble LA, Silva JM, Li C, Chauret N, Gauthier JY, Grimm E, Léger S, Roy P, Thérien M, Wang Z, Prasit P, Zamboni R, Young RN, Brideau C, Chan CC, Mancini J, Riendeau D.

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2683-6.

PMID:
11128651
34.

Description of a 96-well plate assay to measure cytochrome P4503A inhibition in human liver microsomes using a selective fluorescent probe.

Chauret N, Tremblay N, Lackman RL, Gauthier JY, Silva JM, Marois J, Yergey JA, Nicoll-Griffith DA.

Anal Biochem. 1999 Dec 15;276(2):215-26.

PMID:
10603245
35.

Induction of cytochrome-P450 in cryopreserved rat and human hepatocytes.

Silva JM, Day SH, Nicoll-Griffith DA.

Chem Biol Interact. 1999 Jun 1;121(1):49-63.

PMID:
10418970
36.

Cryopreservation of rat and human liver slices by rapid freezing.

Day SH, Nicoll-Griffith DA, Silva JM.

Cryobiology. 1999 Mar;38(2):154-9.

PMID:
10191038
37.

Oxidative bioactivation of the lactol prodrug of a lactone cyclooxygenase-2 inhibitor.

Nicoll-Griffith DA, Falgueyret JP, Silva JM, Morin PE, Trimble L, Chan CC, Clas S, Leger S, Wang Z, Yergey JA, Riendeau D.

Drug Metab Dispos. 1999 Mar;27(3):403-9.

PMID:
10064573
38.

Refinement of an in vitro cell model for cytochrome P450 induction.

Silva JM, Morin PE, Day SH, Kennedy BP, Payette P, Rushmore T, Yergey JA, Nicoll-Griffith DA.

Drug Metab Dispos. 1998 May;26(5):490-6.

PMID:
9571231
39.

Effect of common organic solvents on in vitro cytochrome P450-mediated metabolic activities in human liver microsomes.

Chauret N, Gauthier A, Nicoll-Griffith DA.

Drug Metab Dispos. 1998 Jan;26(1):1-4.

PMID:
9443844
40.

In vitro comparison of cytochrome P450-mediated metabolic activities in human, dog, cat, and horse.

Chauret N, Gauthier A, Martin J, Nicoll-Griffith DA.

Drug Metab Dispos. 1997 Oct;25(10):1130-6.

PMID:
9321515
41.

Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.

Delorme D, Ducharme Y, Brideau C, Chan CC, Chauret N, Desmarais S, Dubé D, Falgueyret JP, Fortin R, Guay J, Hamel P, Jones TR, Lépine C, Li C, McAuliffe M, McFarlane CS, Nicoll-Griffith DA, Riendeau D, Yergey JA, Girard Y.

J Med Chem. 1996 Sep 27;39(20):3951-70.

PMID:
8831761
42.

Verlukast (MK-0679) conjugation with glutathione by rat liver and kidney cytosols and excretion in the bile.

Nicoll-Griffith DA, Gupta N, Twa SP, Williams H, Trimble LA, Yergey JA.

Drug Metab Dispos. 1995 Oct;23(10):1085-93.

PMID:
8654196
43.

Integrated application of capillary HPLC/continuous-flow liquid secondary ion mass spectrometry to discovery stage metabolism studies.

Li C, Chauret N, Ducharme Y, Trimble LA, Nicoll-Griffith DA, Yergey JA.

Anal Chem. 1995 Sep 1;67(17):2931-6.

PMID:
8779418
44.

In vitro and in vivo biotransformations of the naphthalenic lignan lactone 5-lipoxygenase inhibitor, L-702,539.

Chauret N, Li C, Ducharme Y, Trimble LA, Yergey JA, Ramachandran C, Nicoll-Griffith DA.

Drug Metab Dispos. 1995 Jan;23(1):65-71.

PMID:
7720527
45.

Increased cosedimentation of cytosolic glutathione S-transferases with microsomal fractions prepared from frozen rat liver.

Cribb AE, Griffin GP, Spielberg SP, Rushmore TH, Chauret N, Nicoll-Griffith DA.

Drug Metab Dispos. 1994 Nov-Dec;22(6):969-72. No abstract available.

PMID:
7895617
46.

Characterization of verlukast metabolites arising from an epoxide intermediate produced with hepatic microsomes from beta-naphthoflavone-treated rodents (P-4501A1).

Nicoll-Griffith DA, Chauret N, Yergey JA, Trimble LA, Favreau L, Zamboni R, Grossman SJ, Drey J, Herold E.

Drug Metab Dispos. 1993 Sep-Oct;21(5):861-7.

PMID:
7902249
47.

Method to determine the enantiomers of ibuprofen from human urine by high-performance liquid chromatography.

Nicoll-Griffith DA, Inaba T, Tang BK, Kalow W.

J Chromatogr. 1988 Jun 24;428(1):103-12.

PMID:
3170663
48.

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