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Items: 1 to 50 of 68

1.

Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.

Hong Q, Bakshi RK, Palucki BL, Park MK, Ye Z, He S, Pollard PG, Sebhat IK, Liu J, Guo L, Cashen DE, Martin WJ, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, MacIntyre DE, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4. doi: 10.1016/j.bmcl.2011.02.090. Epub 2011 Mar 1.

PMID:
21439820
2.

Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.

He S, Ye Z, Dobbelaar PH, Bakshi RK, Hong Q, Dellureficio JP, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Reibarkh M, Holmes MA, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Wyvratt MJ Jr, Nargund RP.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6524-32. doi: 10.1016/j.bmcl.2010.09.049. Epub 2010 Sep 19.

PMID:
20933410
3.

In vitro and in vivo metabolism of a novel cannabinoid-1 receptor inverse agonist, taranabant, in rats and monkeys.

Reddy VB, Doss GA, Karanam BV, Samuel K, Lanza TJ Jr, Lin LS, Yu NX, Zhang AS, Raab CE, Stearns RA, Kumar S.

Xenobiotica. 2010 Sep;40(9):650-62. doi: 10.3109/00498254.2010.501117.

PMID:
20608842
4.

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.

He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Weinberg DH, Macneil T, Tang R, Strack AM, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Fong TM, Wyvratt MJ Jr, Nargund RP.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4399-405. doi: 10.1016/j.bmcl.2010.06.062. Epub 2010 Jun 15.

PMID:
20598882
5.

Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.

Hong Q, Bakshi RK, Dellureficio J, He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Tang R, Kalyani RN, Macneil T, Vongs A, Rosenblum CI, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen D, Martin WJ, Chen AS, Metzger JM, Chen HY, Strack AM, Fong TM, Maclntyre E, Van der Ploeg LH, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10.

PMID:
20598533
6.

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Tsou NN, Ball RG, Cashen DE, Martin WJ, Weinberg DH, Macneil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Macintyre DE, Wyvratt MJ Jr, Nargund RP.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19.

PMID:
20207541
7.

Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: a case study with melanocortin-4 receptor agonists.

Tang W, Stearns RA, Wang RW, Miller RR, Chen Q, Ngui J, Bakshi RK, Nargund RP, Dean DC, Baillie TA.

Xenobiotica. 2008 Nov;38(11):1437-51. doi: 10.1080/00498250802464685.

PMID:
18841517
8.

Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.

Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, Hafey M, Evers R, Dean DC, Magriotis PA, Lanza TJ, Lin LS, Hagmann WK, Baillie TA.

Xenobiotica. 2008 Feb;38(2):223-37. doi: 10.1080/00498250701744682 .

PMID:
18197560
9.

In vitro metabolic activation of lumiracoxib in rat and human liver preparations.

Li Y, Slatter JG, Zhang Z, Li Y, Doss GA, Braun MP, Stearns RA, Dean DC, Baillie TA, Tang W.

Drug Metab Dispos. 2008 Feb;36(2):469-73. Epub 2007 Nov 12.

PMID:
17998295
10.

Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.

Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH.

Drug Metab Dispos. 2007 Apr;35(4):525-32. Epub 2007 Jan 12.

PMID:
17220241
11.

Characterization of two cyclic metabolites of sitagliptin.

Liu DQ, Arison BH, Stearns RA, Kim D, Vincent SH.

Drug Metab Dispos. 2007 Apr;35(4):521-4. Epub 2007 Jan 12.

PMID:
17220240
12.

Metabolic activation of a pentafluorophenylethylamine derivative: formation of glutathione conjugates in vitro in the rat.

Shang J, Xu S, Teffera Y, Doss GA, Stearns RA, Edmonson S, Beconi MG.

Xenobiotica. 2005 Jul;35(7):697-713.

PMID:
16316929
13.

Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.

Chen Q, Doss GA, Tung EC, Liu W, Tang YS, Braun MP, Didolkar V, Strauss JR, Wang RW, Stearns RA, Evans DC, Baillie TA, Tang W.

Drug Metab Dispos. 2006 Jan;34(1):145-51. Epub 2005 Oct 26.

PMID:
16251255
14.

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.

Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.

PMID:
15982875
15.

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.

Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3.

PMID:
15951175
16.

In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: formation of reactive iminium and quinone type metabolites.

Zhang Z, Chen Q, Li Y, Doss GA, Dean BJ, Ngui JS, Silva Elipe M, Kim S, Wu JY, Dininno F, Hammond ML, Stearns RA, Evans DC, Baillie TA, Tang W.

Chem Res Toxicol. 2005 Apr;18(4):675-85.

PMID:
15833027
17.

2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.

Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6.

PMID:
15808454
18.

Metabolic activation of a 1,3-disubstituted piperazine derivative: evidence for a novel ring contraction to an imidazoline.

Doss GA, Miller RR, Zhang Z, Teffera Y, Nargund RP, Palucki B, Park MK, Tang YS, Evans DC, Baillie TA, Stearns RA.

Chem Res Toxicol. 2005 Feb;18(2):271-6.

PMID:
15720132
19.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.

Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5.

PMID:
15582434
20.

Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes.

Xu S, Zhu B, Teffera Y, Pan DE, Caldwell CG, Doss G, Stearns RA, Evans DC, Beconi MG.

Drug Metab Dispos. 2005 Jan;33(1):121-30. Epub 2004 Oct 14.

PMID:
15486074
21.

Influence of different recombinant systems on the cooperativity exhibited by cytochrome P4503A4.

Zhang Z, Li Y, Shou M, Zhang Y, Ngui JS, Stearns RA, Evans DC, Baillie TA, Tang W.

Xenobiotica. 2004 May;34(5):473-86.

PMID:
15370963
22.

Effect of quinidine on the 10-hydroxylation of R-warfarin: species differences and clearance projection.

Chen Q, Tan E, Strauss JR, Zhang Z, Fenyk-Melody JE, Booth-Genthe C, Rushmore TH, Stearns RA, Evans DC, Baillie TA, Tang W.

J Pharmacol Exp Ther. 2004 Oct;311(1):307-14. Epub 2004 May 26.

PMID:
15163679
23.
24.

Identification of a hydroxylamine glucuronide metabolite of an oral hypoglycemic agent.

Miller RR, Doss GA, Stearns RA.

Drug Metab Dispos. 2004 Feb;32(2):178-85.

PMID:
14744939
26.

Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques.

Samuel K, Yin W, Stearns RA, Tang YS, Chaudhary AG, Jewell JP, Lanza T Jr, Lin LS, Hagmann WK, Evans DC, Kumar S.

J Mass Spectrom. 2003 Feb;38(2):211-21.

PMID:
12577288
28.

Extrapolation of diclofenac clearance from in vitro microsomal metabolism data: role of acyl glucuronidation and sequential oxidative metabolism of the acyl glucuronide.

Kumar S, Samuel K, Subramanian R, Braun MP, Stearns RA, Chiu SH, Evans DC, Baillie TA.

J Pharmacol Exp Ther. 2002 Dec;303(3):969-78.

PMID:
12438516
29.

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.

Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

J Med Chem. 2002 Oct 10;45(21):4589-93.

PMID:
12361385
30.

Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation.

Chen Q, Ngui JS, Doss GA, Wang RW, Cai X, DiNinno FP, Blizzard TA, Hammond ML, Stearns RA, Evans DC, Baillie TA, Tang W.

Chem Res Toxicol. 2002 Jul;15(7):907-14.

PMID:
12119000
31.

Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate.

Tang W, Stearns RA, Miller RR, Ngui JS, Mathvink RJ, Weber AE, Kwei GY, Strauss JR, Keohane CA, Doss GA, Chiu SH, Baillie TA.

Drug Metab Dispos. 2002 Jul;30(7):778-87.

PMID:
12065436
32.

The pharmacokinetics of a thiazole benzenesulfonamide beta 3-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability.

Stearns RA, Miller RR, Tang W, Kwei GY, Tang FS, Mathvink RJ, Naylor EM, Chitty D, Colandrea VJ, Weber AE, Colletti AE, Strauss JR, Keohane CA, Feeney WP, Iliff SA, Chiu SH.

Drug Metab Dispos. 2002 Jul;30(7):771-7.

PMID:
12065435
33.

Cytochrome P450 3A4-mediated oxidative conversion of a cyano to an amide group in the metabolism of pinacidil.

Zhang Z, Li Y, Stearns RA, Ortiz De Montellano PR, Baillie TA, Tang W.

Biochemistry. 2002 Feb 26;41(8):2712-8.

PMID:
11851418
34.

Bioactivation of diclofenac via benzoquinone imine intermediates-identification of urinary mercapturic acid derivatives in rats and humans.

Poon GK, Chen Q, Teffera Y, Ngui JS, Griffin PR, Braun MP, Doss GA, Freeden C, Stearns RA, Evans DC, Baillie TA, Tang W.

Drug Metab Dispos. 2001 Dec;29(12):1608-13.

PMID:
11717180
35.

Heterotropic cooperativity of cytochrome P450 3A4 and potential drug-drug interactions.

Tang W, Stearns RA.

Curr Drug Metab. 2001 Jun;2(2):185-98. Review.

PMID:
11469725
36.

In vitro stimulation of warfarin metabolism by quinidine: increases in the formation of 4'- and 10-hydroxywarfarin.

Ngui JS, Chen Q, Shou M, Wang RW, Stearns RA, Baillie TA, Tang W.

Drug Metab Dispos. 2001 Jun;29(6):877-86.

PMID:
11353757
37.

Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.

Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE.

J Med Chem. 2000 Oct 19;43(21):3832-6.

PMID:
11052788
38.

Determination of brain and plasma drug concentrations by liquid chromatography/tandem mass spectrometry.

Tamvakopoulos CS, Colwell LF, Barakat K, Fenyk-Melody J, Griffin PR, Nargund R, Palucki B, Sebhat I, Shen X, Stearns RA.

Rapid Commun Mass Spectrom. 2000;14(19):1729-35.

PMID:
11006579
39.

Cytochrome P450 3A4-mediated interaction of diclofenac and quinidine.

Ngui JS, Tang W, Stearns RA, Shou M, Miller RR, Zhang Y, Lin JH, Baillie TA.

Drug Metab Dispos. 2000 Sep;28(9):1043-50.

PMID:
10950847
40.

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
41.

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
42.

Interaction of diclofenac and quinidine in monkeys: stimulation of diclofenac metabolism.

Tang W, Stearns RA, Kwei GY, Iliff SA, Miller RR, Egan MA, Yu NX, Dean DC, Kumar S, Shou M, Lin JH, Baillie TA.

J Pharmacol Exp Ther. 1999 Dec;291(3):1068-74.

PMID:
10565826
43.

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

Shih TL, Candelore MR, Cascieri MA, Chiu SH, 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. 1999 May 3;9(9):1251-4.

PMID:
10340609
44.

Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, 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. 1999 Mar 8;9(5):749-54.

PMID:
10201841
45.

Studies on cytochrome P-450-mediated bioactivation of diclofenac in rats and in human hepatocytes: identification of glutathione conjugated metabolites.

Tang W, Stearns RA, Bandiera SM, Zhang Y, Raab C, Braun MP, Dean DC, Pang J, Leung KH, Doss GA, Strauss JR, Kwei GY, Rushmore TH, Chiu SH, Baillie TA.

Drug Metab Dispos. 1999 Mar;27(3):365-72.

PMID:
10064567
46.

Roles of human hepatic cytochrome P450s 2C9 and 3A4 in the metabolic activation of diclofenac.

Tang W, Stearns RA, Wang RW, Chiu SH, Baillie TA.

Chem Res Toxicol. 1999 Feb;12(2):192-9.

PMID:
10027798
47.

3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.

Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6.

PMID:
9873496
48.

Disposition of L-732,531, a potent immunosuppressant, in rats and baboons.

Karanam BV, Miller RR, Colletti A, Montgomery T, Carey KD, Hawkins T, Tang YS, Lavin M, Stearns RA, Chiu SH, Vincent SH.

Drug Metab Dispos. 1998 Oct;26(10):949-57.

PMID:
9763399
49.

A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.

Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al.

J Clin Invest. 1998 Jun 1;101(11):2387-93.

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