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Items: 38

1.

Catalytic Ring Expansions of Cyclic Alcohols Enabled by Proton-Coupled Electron Transfer.

Zhao K, Yamashita K, Carpenter JE, Sherwood TC, Ewing WR, Cheng PTW, Knowles RR.

J Am Chem Soc. 2019 Jun 5;141(22):8752-8757. doi: 10.1021/jacs.9b03973. Epub 2019 May 23.

PMID:
31117664
2.

Overcoming the Limitations of γ- and δ-C-H Arylation of Amines through Ligand Development.

Chen YQ, Wang Z, Wu Y, Wisniewski SR, Qiao JX, Ewing WR, Eastgate MD, Yu JQ.

J Am Chem Soc. 2018 Dec 26;140(51):17884-17894. doi: 10.1021/jacs.8b07109. Epub 2018 Dec 14.

PMID:
30500192
3.

Factor XIa Inhibitors as New Anticoagulants.

Quan ML, Pinto DJP, Smallheer JM, Ewing WR, Rossi KA, Luettgen JM, Seiffert DA, Wexler RR.

J Med Chem. 2018 Sep 13;61(17):7425-7447. doi: 10.1021/acs.jmedchem.8b00173. Epub 2018 May 18.

PMID:
29775297
4.

Decarboxylative alkylation for site-selective bioconjugation of native proteins via oxidation potentials.

Bloom S, Liu C, Kölmel DK, Qiao JX, Zhang Y, Poss MA, Ewing WR, MacMillan DWC.

Nat Chem. 2018 Feb;10(2):205-211. doi: 10.1038/nchem.2888. Epub 2017 Dec 4.

5.

Ni-Catalyzed Carbon-Carbon Bond-Forming Reductive Amination.

Heinz C, Lutz JP, Simmons EM, Miller MM, Ewing WR, Doyle AG.

J Am Chem Soc. 2018 Feb 14;140(6):2292-2300. doi: 10.1021/jacs.7b12212. Epub 2018 Feb 1.

PMID:
29341599
6.

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.

Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27.

PMID:
29316397
7.

Selective C-H Halogenation with a Highly Fluorinated Manganese Porphyrin.

Li G, Dilger AK, Cheng PT, Ewing WR, Groves JT.

Angew Chem Int Ed Engl. 2018 Jan 26;57(5):1251-1255. doi: 10.1002/anie.201710676. Epub 2017 Dec 28.

PMID:
29235203
8.

Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).

Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR.

J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17.

PMID:
29077405
9.

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.

Corte JR, Yang W, Fang T, Wang Y, Osuna H, Lai A, Ewing WR, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Quan ML, Wexler RR, Lam PYS.

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3833-3839. doi: 10.1016/j.bmcl.2017.06.058. Epub 2017 Jun 23.

PMID:
28687203
10.

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9.

PMID:
28112924
11.

Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.

Ellsworth BA, Sher PM, Wu X, Wu G, Sulsky RB, Gu Z, Murugesan N, Zhu Y, Yu G, Sitkoff DF, Carlson KE, Kang L, Yang Y, Lee N, Baska RA, Keim WJ, Cullen MJ, Azzara AV, Zuvich E, Thomas MA, Rohrbach KW, Devenny JJ, Godonis HE, Harvey SJ, Murphy BJ, Everlof GG, Stetsko PI, Gudmundsson O, Johnghar S, Ranasinghe A, Behnia K, Pelleymounter MA, Ewing WR.

J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20.

PMID:
24182233
12.

Solid phase synthesis of 1,5-diarylpyrazole-4-carboxamides: discovery of antagonists of the CB-1 receptor.

Pendri A, Dodd DS, Chen J, Cvijic ME, Kang L, Baska RA, Carlson KE, Burford NT, Sun C, Ewing WR, Gerritz SW.

ACS Comb Sci. 2012 Mar 12;14(3):197-204. doi: 10.1021/co200147y. Epub 2012 Feb 16.

PMID:
22340081
13.

Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.

Yang Y, Miller KJ, Zhu Y, Hong Y, Tian Y, Murugesan N, Gu Z, O'Tanyi E, Keim WJ, Rohrbach KW, Johnghar S, Behnia K, Pelleymounter MA, Carlson KE, Ewing WR.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6856-60. doi: 10.1016/j.bmcl.2011.09.016. Epub 2011 Sep 13.

PMID:
21962575
14.

Cannabinoid CB(1) receptor ligand binding and function examined through mutagenesis studies of F200 and S383.

Sitkoff DF, Lee N, Ellsworth BA, Huang Q, Kang L, Baska R, Huang Y, Sun C, Pendri A, Malley MF, Scaringe RP, Gougoutas JZ, Reggio PH, Ewing WR, Pelleymounter MA, Carlson KE.

Eur J Pharmacol. 2011 Jan 25;651(1-3):9-17. doi: 10.1016/j.ejphar.2010.10.056. Epub 2010 Oct 31.

PMID:
21044623
15.

Exploration of structure-activity relationships at the two C-terminal residues of potent 11mer Glucagon-Like Peptide-1 receptor agonist peptides via parallel synthesis.

Haque TS, Martinez RL, Lee VG, Riexinger DG, Lei M, Feng M, Koplowitz B, Mapelli C, Cooper CB, Zhang G, Huang C, Ewing WR, Krupinski J.

Peptides. 2010 Jul;31(7):1353-60. doi: 10.1016/j.peptides.2010.04.013. Epub 2010 Apr 24.

PMID:
20420872
16.

Identification of potent 11mer glucagon-like peptide-1 receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs.

Haque TS, Lee VG, Riexinger D, Lei M, Malmstrom S, Xin L, Han S, Mapelli C, Cooper CB, Zhang G, Ewing WR, Krupinski J.

Peptides. 2010 May;31(5):950-5. doi: 10.1016/j.peptides.2010.01.008. Epub 2010 Feb 4.

PMID:
20138099
17.

Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase.

Haque TS, Liang N, Golla R, Seethala R, Ma Z, Ewing WR, Cooper CB, Pelleymounter MA, Poss MA, Cheng D.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5872-6. doi: 10.1016/j.bmcl.2009.08.077. Epub 2009 Aug 26.

PMID:
19740659
18.

Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.

Mapelli C, Natarajan SI, Meyer JP, Bastos MM, Bernatowicz MS, Lee VG, Pluscec J, Riexinger DJ, Sieber-McMaster ES, Constantine KL, Smith-Monroy CA, Golla R, Ma Z, Longhi DA, Shi D, Xin L, Taylor JR, Koplowitz B, Chi CL, Khanna A, Robinson GW, Seethala R, Antal-Zimanyi IA, Stoffel RH, Han S, Whaley JM, Huang CS, Krupinski J, Ewing WR.

J Med Chem. 2009 Dec 10;52(23):7788-99. doi: 10.1021/jm900752a.

PMID:
19702274
19.

(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.

Li J, Chen SY, Murphy BJ, Flynn N, Seethala R, Slusarchyk D, Yan M, Sleph P, Zhang H, Humphreys WG, Ewing WR, Robl JA, Gordon D, Tino JA.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4072-4. doi: 10.1016/j.bmcl.2008.05.100. Epub 2008 Jun 12.

PMID:
18554903
20.

Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.

Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P, Slusarchyk D, Yan M, Humphreys WG, Zhang H, Ewing WR, Robl JA, Gordon D, Tino JA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1825-9. doi: 10.1016/j.bmcl.2008.02.021. Epub 2008 Feb 13.

PMID:
18295486
21.

Design and SAR of selective T-type calcium channel antagonists containing a biaryl sulfonamide core.

Hangeland JJ, Cheney DL, Friends TJ, Swartz S, Levesque PC, Rich AJ, Sun L, Bridal TR, Adam LP, Normandin DE, Murugesan N, Ewing WR.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):474-8. Epub 2007 Dec 3.

PMID:
18160281
22.

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA.

J Med Chem. 2007 Nov 29;50(24):5890-3. Epub 2007 Oct 31.

PMID:
17973363
23.

Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.

Ellsworth BA, Wang Y, Zhu Y, Pendri A, Gerritz SW, Sun C, Carlson KE, Kang L, Baska RA, Yang Y, Huang Q, Burford NT, Cullen MJ, Johnghar S, Behnia K, Pelleymounter MA, Washburn WN, Ewing WR.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. Epub 2007 Apr 29.

PMID:
17513109
24.

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R, Harrity T, Stoffel R, Taylor DS, Lavoie TB, Kish K, Jacobson BL, Sheriff S, Adam LP, Ewing WR, Robl JA.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. Epub 2006 Dec 21.

PMID:
17502136
25.

Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys.

Zhang H, Zhang D, Li W, Yao M, D'Arienzo C, Li YX, Ewing WR, Gu Z, Zhu Y, Murugesan N, Shyu WC, Humphreys WG.

Drug Metab Dispos. 2007 May;35(5):795-805. Epub 2007 Feb 15.

PMID:
17303626
26.

Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.

Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE.

J Med Chem. 2005 Jan 13;48(1):171-9.

PMID:
15634011
27.

Discovery of a potent and novel motilin agonist.

Li JJ, Chao HG, Wang H, Tino JA, Lawrence RM, Ewing WR, Ma Z, Yan M, Slusarchyk D, Seethala R, Sun H, Li D, Burford NT, Stoffel RH, Salyan ME, Li CY, Witkus M, Zhao N, Rich A, Gordon DA.

J Med Chem. 2004 Mar 25;47(7):1704-8.

PMID:
15027861
28.

Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket.

Maignan S, Guilloteau JP, Choi-Sledeski YM, Becker MR, Ewing WR, Pauls HW, Spada AP, Mikol V.

J Med Chem. 2003 Feb 27;46(5):685-90.

PMID:
12593649
29.

The design of competitive, small-molecule inhibitors of coagulation factor Xa.

Pauls HW, Ewing WR.

Curr Top Med Chem. 2001 Jun;1(2):83-100. Review.

PMID:
11899252
30.

Crystal structures of human factor Xa complexed with potent inhibitors.

Maignan S, Guilloteau JP, Pouzieux S, Choi-Sledeski YM, Becker MR, Klein SI, Ewing WR, Pauls HW, Spada AP, Mikol V.

J Med Chem. 2000 Aug 24;43(17):3226-32.

PMID:
10966741
31.

Pharmacodynamic activity and antithrombotic efficacy of RPR120844, a novel inhibitor of coagulation factor Xa.

Leadley RJ Jr, Morgan SR, Bentley R, Bostwick JS, Kasiewski CJ, Heran C, Chu V, Brown K, Moxey P, Ewing WR, Pauls H, Spada AP, Perrone MH, Dunwiddie CT.

J Cardiovasc Pharmacol. 1999 Dec;34(6):791-9.

PMID:
10598121
32.

Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

Becker MR, Ewing WR, Davis RS, Pauls HW, Ly C, Li A, Mason HJ, Choi-Sledeski YM, Spada AP, Chu V, Brown KD, Colussi DJ, Leadley RJ, Bentley R, Bostwick J, Kasiewski C, Morgan S.

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2753-8.

PMID:
10509929
33.

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.

Choi-Sledeski YM, Becker MR, Green DM, Davis R, Ewing WR, Mason HJ, Ly C, Spada A, Liang G, Cheney D, Barton J, Chu V, Brown K, Colussi D, Bentley R, Leadley R, Dunwiddie C, Pauls HW.

Bioorg Med Chem Lett. 1999 Sep 6;9(17):2539-44.

PMID:
10498204
34.

Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.

Choi-Sledeski YM, McGarry DG, Green DM, Mason HJ, Becker MR, Davis RS, Ewing WR, Dankulich WP, Manetta VE, Morris RL, Spada AP, Cheney DL, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Leadley RJ, Maignan S, Guilloteau JP, Dunwiddie CT, Pauls HW.

J Med Chem. 1999 Sep 9;42(18):3572-87.

PMID:
10479289
35.

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.

Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V.

J Med Chem. 1999 Sep 9;42(18):3557-71.

PMID:
10479288
36.

RPR120844, a novel, specific inhibitor of coagulation factor Xa inhibits venous thrombosis in the rabbit.

Bostwick JS, Bentley R, Morgan S, Brown K, Chu V, Ewing WR, Spada AP, Pauls H, Perrone MH, Dunwiddie CT, Leadley RJ Jr.

Thromb Haemost. 1999 Jan;81(1):157-60.

PMID:
10348709
37.

Affinity of fibroblast growth factors for beta-cyclodextrin tetradecasulfate.

Yuen SN, Folkman J, Weisz PB, Joullie MM, Ewing WR.

Anal Biochem. 1990 Feb 15;185(1):108-11.

PMID:
2344037
38.

Control of angiogenesis with synthetic heparin substitutes.

Folkman J, Weisz PB, Joullié MM, Li WW, Ewing WR.

Science. 1989 Mar 17;243(4897):1490-3.

PMID:
2467380

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