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Items: 21

1.

Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.

Xu G, Gaul MD, Song F, Du F, Liang Y, DesJarlais RL, DiLoreto K, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126668. doi: 10.1016/j.bmcl.2019.126668. Epub 2019 Sep 4.

PMID:
31519374
2.

Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.

Song F, Xu G, Gaul MD, Zhao B, Lu T, Zhang R, DesJarlais RL, DiLoreto K, Huebert N, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1974-1980. doi: 10.1016/j.bmcl.2019.05.036. Epub 2019 May 18.

PMID:
31138472
3.

Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.

Xu G, Gaul MD, Kuo GH, Du F, Xu JZ, Wallace N, Hinke S, Kirchner T, Silva J, Huebert ND, Lee S, Murray W, Liang Y, Demarest K.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3446-3453. doi: 10.1016/j.bmcl.2018.09.025. Epub 2018 Sep 19.

PMID:
30268701
4.

Potent Sodium/Glucose Cotransporter SGLT1/2 Dual Inhibition Improves Glycemic Control Without Marked Gastrointestinal Adaptation or Colonic Microbiota Changes in Rodents.

Du F, Hinke SA, Cavanaugh C, Polidori D, Wallace N, Kirchner T, Jennis M, Lang W, Kuo GH, Gaul MD, Lenhard J, Demarest K, Ajami NJ, Liang Y, Hornby PJ.

J Pharmacol Exp Ther. 2018 Jun;365(3):676-687. doi: 10.1124/jpet.118.248575. Epub 2018 Apr 19.

PMID:
29674332
5.

Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.

Kuo GH, Gaul MD, Liang Y, Xu JZ, Du F, Hornby P, Xu G, Qi J, Wallace N, Lee S, Grant E, Murray WV, Demarest K.

Bioorg Med Chem Lett. 2018 Apr 15;28(7):1182-1187. doi: 10.1016/j.bmcl.2018.02.057. Epub 2018 Mar 1.

PMID:
29523385
6.

Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.

Patch RJ, Huang H, Patel S, Cheung W, Xu G, Zhao BP, Beauchamp DA, Rentzeperis D, Geisler JG, Askari HB, Liu J, Kasturi J, Towers M, Gaul MD, Player MR.

Eur J Med Chem. 2017 Sep 29;138:830-853. doi: 10.1016/j.ejmech.2017.07.015. Epub 2017 Jul 14.

PMID:
28735214
7.

Metabolic tracing of monoacylglycerol acyltransferase-2 activity in vitro and in vivo.

Qi J, Lang W, Connelly MA, Du F, Liang Y, Caldwell GW, Martin T, Hansen MK, Kuo GH, Gaul MD, Pocai A, Lee S.

Anal Biochem. 2017 May 1;524:68-75. doi: 10.1016/j.ab.2016.09.017. Epub 2016 Sep 22.

PMID:
27665677
8.

Synthesis of β-Substituted Cyclic Enones via Phosphonium Salt-Activated, Palladium-Catalyzed Cross-Coupling of Cyclic 1,3-Diones.

Yang SM, Kuo GH, Gaul MD, Murray WV.

J Org Chem. 2016 Apr 15;81(8):3464-9. doi: 10.1021/acs.joc.6b00317. Epub 2016 Apr 7.

PMID:
27052958
9.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs.

Yang SM, Tang Y, Rano T, Lu H, Kuo GH, Gaul MD, Li Y, Ho G, Lang W, Conway JG, Liang Y, Lenhard JM, Demarest KT, Murray WV.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1437-41. doi: 10.1016/j.bmcl.2013.12.075. Epub 2013 Dec 27.

PMID:
24405703
10.

4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.

Yang SM, Tang Y, Zhang R, Lu H, Kuo GH, Gaul MD, Li Y, Ho G, Conway JG, Liang Y, Lenhard JM, Demarest KT, Murray WV.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6773-6. doi: 10.1016/j.bmcl.2013.09.096. Epub 2013 Oct 9.

PMID:
24153205
11.

Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.

Subasinghe NL, Khalil E, Travins JM, Ali F, Ballentine SK, Hufnagel HR, Pan W, Leonard K, Bone RF, Soll RM, Crysler CS, Ninan N, Kirkpatrick J, Kolpak MX, Diloreto KA, Eisennagel SH, Huebert ND, Molloy CJ, Tomczuk BE, Gaul MD.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5303-7. doi: 10.1016/j.bmcl.2012.06.030. Epub 2012 Jun 16.

PMID:
22795627
12.

The use of stable isotope-labeled glycerol and oleic acid to differentiate the hepatic functions of DGAT1 and -2.

Qi J, Lang W, Geisler JG, Wang P, Petrounia I, Mai S, Smith C, Askari H, Struble GT, Williams R, Bhanot S, Monia BP, Bayoumy S, Grant E, Caldwell GW, Todd MJ, Liang Y, Gaul MD, Demarest KT, Connelly MA.

J Lipid Res. 2012 Jun;53(6):1106-16. doi: 10.1194/jlr.M020156. Epub 2012 Apr 3.

13.

Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.

Patch RJ, Searle LL, Kim AJ, De D, Zhu X, Askari HB, O'Neill JC, Abad MC, Rentzeperis D, Liu J, Kemmerer M, Lin L, Kasturi J, Geisler JG, Lenhard JM, Player MR, Gaul MD.

J Med Chem. 2011 Feb 10;54(3):788-808. doi: 10.1021/jm101063h. Epub 2011 Jan 10.

PMID:
21218783
14.

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.

Rheault TR, Caferro TR, Dickerson SH, Donaldson KH, Gaul MD, Goetz AS, Mullin RJ, McDonald OB, Petrov KG, Rusnak DW, Shewchuk LM, Spehar GM, Truesdale AT, Vanderwall DE, Wood ER, Uehling DE.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011. Epub 2008 Dec 7.

PMID:
19111461
15.

4-Amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes as potent FLT-3 inhibitors.

Gaul MD, Xu G, Kirkpatrick J, Ott H, Baumann CA.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4861-5. Epub 2007 Jun 14.

PMID:
17611106
16.

Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors.

Huang S, Li R, Connolly PJ, Xu G, Gaul MD, Emanuel SL, Lamontagne KR, Greenberger LM.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6063-6. Epub 2006 Sep 18.

PMID:
16979339
17.

Substrate specificity and novel selective inhibitors of TNF-alpha converting enzyme (TACE) from two-dimensional substrate mapping.

Lambert MH, Blackburn RK, Seaton TD, Kassel DB, Kinder DS, Leesnitzer MA, Bickett DM, Warner JR, Andersen MW, Badiang JG, Cowan DJ, Gaul MD, Petrov KG, Rabinowitz MH, Wiethe RW, Becherer JD, McDougald DL, Musso DL, Andrews RC, Moss ML.

Comb Chem High Throughput Screen. 2005 Jun;8(4):327-39.

PMID:
16101009
18.

CYP3A induction by N-hydroxyformamide tumor necrosis factor-alpha converting enzyme/matrix metalloproteinase inhibitors use of a pregname X receptor activation assay and primary hepatocyte culture for assessing induction potential in humans.

Tippin TK, Hamilton G, Moore L, Beaudet EJ, Jolley S, Brodie TA, Andrews RC, Becherer JD, McDougald DL, Gaul MD, Hoivik DJ, Mellon-Kusibab K, Lehmann J, Kliewer S, Novick S, Laethem R, Zhao Z, LeCluyse EL.

Drug Metab Dispos. 2003 Jul;31(7):870-7.

PMID:
12814963
19.

Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.

Gaul MD, Guo Y, Affleck K, Cockerill GS, Gilmer TM, Griffin RJ, Guntrip S, Keith BR, Knight WB, Mullin RJ, Murray DM, Rusnak DW, Smith K, Tadepalli S, Wood ER, Lackey K.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):637-40.

PMID:
12639547
20.

N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.

Musso DL, Andersen MW, Andrews RC, Austin R, Beaudet EJ, Becherer JD, Bubacz DG, Bickett DM, Chan JH, Conway JG, Cowan DJ, Gaul MD, Glennon KC, Hedeen KM, Lambert MH, Leesnitzer MA, McDougald DL, Mitchell JL, Moss ML, Rabinowitz MH, Rizzolio MC, Schaller LT, Stanford JB, Tippin T, Warner JR, Whitesell LG, Wiethe RW.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2147-51.

PMID:
11514157
21.

Aqueous ozonolysis products of methyl- and dimethylnaphthalenes.

Gaul MD, Junk GA, Svec HJ.

Environ Sci Technol. 1987 Aug;21(8):777-84. doi: 10.1021/es00162a008. No abstract available.

PMID:
19995061

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