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Items: 38

1.

Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver.

Muise ES, Guan HP, Liu J, Nawrocki AR, Yang X, Wang C, Rodríguez CG, Zhou D, Gorski JN, Kurtz MM, Feng D, Leavitt KJ, Wei L, Wilkening RR, Apgar JM, Xu S, Lu K, Feng W, Li Y, He H, Previs SF, Shen X, van Heek M, Souza SC, Rosenbach MJ, Biftu T, Erion MD, Kelley DE, Kemp DM, Myers RW, Sebhat IK.

PLoS One. 2019 Feb 27;14(2):e0211568. doi: 10.1371/journal.pone.0211568. eCollection 2019.

2.

Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

Feng D, Biftu T, Romero FA, Kekec A, Dropinski J, Kassick A, Xu S, Kurtz MM, Gollapudi A, Shao Q, Yang X, Lu K, Zhou G, Kemp D, Myers RW, Guan HP, Trujillo ME, Li C, Weber A, Sebhat IK.

ACS Med Chem Lett. 2017 Dec 1;9(1):39-44. doi: 10.1021/acsmedchemlett.7b00417. eCollection 2018 Jan 11.

3.

Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.

Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE, Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M, Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM, Sebhat IK.

Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13.

PMID:
28705990
4.

The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.

Cox JM, Chu HD, Kuethe JT, Gao YD, Scapin G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Sinha-Roy R, Weber AE, Biftu T.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2622-6. doi: 10.1016/j.bmcl.2016.04.020. Epub 2016 Apr 9.

PMID:
27106708
5.

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5767-71. doi: 10.1016/j.bmcl.2015.10.070. Epub 2015 Oct 30.

PMID:
26546218
6.

Improved Stability of Proline-Derived Direct Thrombin Inhibitors through Hydroxyl to Heterocycle Replacement.

Chobanian HR, Pio B, Guo Y, Shen H, Huffman MA, Madeira M, Salituro G, Terebetski JL, Ormes J, Jochnowitz N, Hoos L, Zhou Y, Lewis D, Hawes B, Mitnaul L, O'Neill K, Ellsworth K, Wang L, Biftu T, Duffy JL.

ACS Med Chem Lett. 2015 Mar 13;6(5):553-7. doi: 10.1021/acsmedchemlett.5b00047. eCollection 2015 May 14.

7.

Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE.

J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2.

PMID:
24660890
8.

Heterocyclic core analogs of a direct thrombin inhibitor.

Blizzard TA, Singh S, Patil B, Chidurala N, Komanduri V, Debnath S, Belyakov S, Crespo A, Struck A, Kurtz M, Wiltsie J, Shen X, Sonatore L, Arocho M, Lewis D, Ogletree M, Biftu T.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1111-5. doi: 10.1016/j.bmcl.2014.01.002. Epub 2014 Jan 10.

PMID:
24461292
9.

Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected].

Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Erratum in: Bioorg Med Chem Lett. 2014 Jun 1;24(11):2590.

PMID:
23972441
10.

Synthesis and biological activity of anticoccidial agents: 2,3-diarylindoles.

Scribner A, Moore JA 3rd, Ouvry G, Fisher M, Wyvratt M, Leavitt P, Liberator P, Gurnett A, Brown C, Mathew J, Thompson D, Schmatz D, Biftu T.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1517-21. doi: 10.1016/j.bmcl.2009.01.001. Epub 2009 Jan 9.

PMID:
19195883
11.

Synthesis and biological activity of anticoccidial agents: 5,6-diarylimidazo[2,1-b][1,3]thiazoles.

Scribner A, Meitz S, Fisher M, Wyvratt M, Leavitt P, Liberator P, Gurnett A, Brown C, Mathew J, Thompson D, Schmatz D, Biftu T.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5263-7. doi: 10.1016/j.bmcl.2008.08.063. Epub 2008 Aug 22.

PMID:
18789686
12.

Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.

Liang GB, Qian X, Biftu T, Singh S, Gao YD, Scapin G, Patel S, Leiting B, Patel R, Wu J, Zhang X, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3706-10. doi: 10.1016/j.bmcl.2008.05.061. Epub 2008 May 20.

PMID:
18524582
13.

N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents.

Liang GB, Qian X, Feng D, Fisher M, Crumley T, Darkin-Rattray SJ, Dulski PM, Gurnett A, Leavitt PS, Liberator PA, Misura AS, Samaras S, Tamas T, Schmatz DM, Wyvratt M, Biftu T.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2019-22. doi: 10.1016/j.bmcl.2008.01.104. Epub 2008 Feb 2.

PMID:
18276140
14.

Synthesis and biological activity of imidazopyridine anticoccidial agents: Part II.

Scribner A, Dennis R, Lee S, Ouvry G, Perrey D, Fisher M, Wyvratt M, Leavitt P, Liberator P, Gurnett A, Brown C, Mathew J, Thompson D, Schmatz D, Biftu T.

Eur J Med Chem. 2008 Jun;43(6):1123-51. Epub 2007 Sep 26.

PMID:
17981367
15.

Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.

Gao YD, Feng D, Sheridan RP, Scapin G, Patel SB, Wu JK, Zhang X, Sinha-Roy R, Thornberry NA, Weber AE, Biftu T.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3877-9. Epub 2007 May 3.

PMID:
17502141
16.

Synthesis and SAR studies of potent imidazopyridine anticoccidial agents.

Liang GB, Qian X, Feng D, Fisher M, Brown CM, Gurnett A, Leavitt PS, Liberator PA, Misura AS, Tamas T, Schmatz DM, Wyvratt M, Biftu T.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3558-61. Epub 2007 Apr 24.

PMID:
17475489
17.

Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.

Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. Epub 2007 Apr 2.

PMID:
17433672
18.

Synthesis and biological activity of imidazopyridine anticoccidial agents: part I.

Scribner A, Dennis R, Hong J, Lee S, McIntyre D, Perrey D, Feng D, Fisher M, Wyvratt M, Leavitt P, Liberator P, Gurnett A, Brown C, Mathew J, Thompson D, Schmatz D, Biftu T.

Eur J Med Chem. 2007 Nov-Dec;42(11-12):1334-57. Epub 2007 Feb 25.

PMID:
17433505
19.

Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

Liang GB, Qian X, Feng D, Biftu T, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1903-7. Epub 2007 Jan 24.

PMID:
17291750
20.

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. Epub 2006 Oct 5.

PMID:
17055272
21.

Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents.

Feng D, Fisher M, Liang GB, Qian X, Brown C, Gurnett A, Leavitt PS, Liberator PA, Mathew J, Misura A, Samaras S, Tamas T, Schmatz DM, Wyvratt M, Biftu T.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):5978-81. Epub 2006 Sep 26.

PMID:
17000105
22.

Synthesis and SAR studies of diarylpyrrole anticoccidial agents.

Qian X, Liang GB, Feng D, Fisher M, Crumley T, Rattray S, Dulski PM, Gurnett A, Leavitt PS, Liberator PA, Misura AS, Samaras S, Tamas T, Schmatz DM, Wyvratt M, Biftu T.

Bioorg Med Chem Lett. 2006 May 15;16(10):2817-21. Epub 2006 Mar 6.

PMID:
16517161
23.

Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents.

Biftu T, Feng D, Fisher M, Liang GB, Qian X, Scribner A, Dennis R, Lee S, Liberator PA, Brown C, Gurnett A, Leavitt PS, Thompson D, Mathew J, Misura A, Samaras S, Tamas T, Sina JF, McNulty KA, McKnight CG, Schmatz DM, Wyvratt M.

Bioorg Med Chem Lett. 2006 May 1;16(9):2479-83. Epub 2006 Feb 7.

PMID:
16464591
24.

Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.

Lankas GR, Leiting B, Roy RS, Eiermann GJ, Beconi MG, Biftu T, Chan CC, Edmondson S, Feeney WP, He H, Ippolito DE, Kim D, Lyons KA, Ok HO, Patel RA, Petrov AN, Pryor KA, Qian X, Reigle L, Woods A, Wu JK, Zaller D, Zhang X, Zhu L, Weber AE, Thornberry NA.

Diabetes. 2005 Oct;54(10):2988-94.

25.

Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.

Liang GB, Qian X, Biftu T, Feng D, Fisher M, Crumley T, Darkin-Rattray SJ, Dulski PM, Gurnett A, Leavitt PS, Liberator PA, Misura AS, Samaras S, Tamas T, Schmatz DM, Wyvratt M.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4570-3.

PMID:
16087336
26.

Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents.

Biftu T, Feng D, Ponpipom M, Girotra N, Liang GB, Qian X, Bugianesi R, Simeone J, Chang L, Gurnett A, Liberator P, Dulski P, Leavitt PS, Crumley T, Misura A, Murphy T, Rattray S, Samaras S, Tamas T, Mathew J, Brown C, Thompson D, Schmatz D, Fisher M, Wyvratt M.

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3296-301.

PMID:
15922595
27.

Purification and molecular characterization of cGMP-dependent protein kinase from Apicomplexan parasites. A novel chemotherapeutic target.

Gurnett AM, Liberator PA, Dulski PM, Salowe SP, Donald RG, Anderson JW, Wiltsie J, Diaz CA, Harris G, Chang B, Darkin-Rattray SJ, Nare B, Crumley T, Blum PS, Misura AS, Tamas T, Sardana MK, Yuan J, Biftu T, Schmatz DM.

J Biol Chem. 2002 May 3;277(18):15913-22. Epub 2002 Feb 7.

28.

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.

Biftu T, Feng DD, Liang GB, Kuo H, Qian X, Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Forrest MJ, Hom GJ, MacIntyre DE, Stearns RA, Strader CD, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1431-4.

PMID:
10888325
29.

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9.

PMID:
10888324
30.

Selective protection and relative importance of the carboxylic acid groups of zaragozic acid A for squalene synthase inhibition.

Biftu T, Acton JJ, Berger GD, Bergstrom JD, Dufresne C, Kurtz MM, Marquis RW, Parsons WH, Rew DR, Wilson KE.

J Med Chem. 1994 Feb 4;37(3):421-4.

PMID:
8308869
31.

Epibatidine is a nicotinic analgesic.

Qian C, Li T, Shen TY, Libertine-Garahan L, Eckman J, Biftu T, Ip S.

Eur J Pharmacol. 1993 Dec 21;250(3):R13-4.

PMID:
8112391
33.

(+/-)-trans-2-(3-Methoxy-5-methylsulfonyl-4-propoxyphenyl)-5-(3,4,5- trimethoxyphenyl)tetrahydrofuran (L-659,989), a novel, potent PAF receptor antagonist.

Ponpipom MM, Hwang SB, Doebber TW, Acton JJ, Alberts AW, Biftu T, Brooker DR, Bugianesi RL, Chabala JC, Gamble NL, et al.

Biochem Biophys Res Commun. 1988 Feb 15;150(3):1213-20. Erratum in: Biochem Biophys Res Commun 1988 Apr 29;152(2):949.

PMID:
2829894
35.

Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonists.

Biftu T, Gamble NF, Doebber T, Hwang SB, Shen TY, Snyder J, Springer JP, Stevenson R.

J Med Chem. 1986 Oct;29(10):1917-21.

PMID:
3020247
37.
38.

TLC screening techniques for the qualitative determination of natural and synthetic capsaicinoids.

Todd P Jr, Bensinger M, Biftu T.

J Chromatogr Sci. 1975 Dec;13(12):577-9.

PMID:
1194398

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