Additional Publications

2008

Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Pontillo J, Wu D, Ching B, Hudson S, Genicot MJ, Gao Y, Ewing T, Fleck BA, Gogas K, Aparicio A, Wang H, Wen J, Wade WS. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6151-5. Epub 2008 Oct 7.

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Moorjani M, Luo Z, Lin E, Vong BG, Chen Y, Zhang X, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Crespo MI, Díaz JL, Saunders J, Slee DH. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5402-5. Epub 2008 Sep 14.

Effects of the transient receptor potential vanilloid 1 antagonist A-425619 on body temperature and thermoregulation in the rat.
Mills C, McMackin M, Jaffe R, Yu J, Zininberg E, Slee D, Gogas K, Bradbury M. Neuroscience. 2008 Sep 22;156(1):165-74. Epub 2008 Jul 25.

Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
Moree WJ, Goldman P, Demaggio AJ, Christenson E, Herendeen D, Eksterowicz J, Kesicki EA, McElligott DL, Beaton G. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5126-9. Epub 2008 Jul 27.

Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Marinkovic D, Tucci FC, Tran JA, Fleck BA, Wen J, Chen C. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4817-22. Epub 2008 Jul 25.

Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.
Hudson S, Kiankarimi M, Eccles W, Dwight W, Mostofi YS, Genicot MJ, Fleck BA, Gogas K, Aparicio A, Wang H, Wen J, Wade WS. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4491-4. Epub 2008 Jul 17.

Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Hudson S, Kiankarimi M, Eccles W, Mostofi YS, Genicot MJ, Dwight W, Fleck BA, Gogas K, Wade WS. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. Epub 2008 Jul 17.

Gene array analysis comparison between rat collagen-induced arthritis and human rheumatoid arthritis.
Soto H, Hevezi P, Roth RB, Pahuja A, Alleva D, Acosta HM, Martinez C, Ortega A, Lopez A, Araiza-Casillas R, Zlotnik A. Scand J Immunol. 2008 Jul;68(1):43-57. Epub 2008 May 14.

Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Wu D, Pontillo J, Ching B, Hudson S, Gao Y, Fleck BA, Gogas K, Wade WS. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. Epub 2008 May 20.

Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Zhang M, Jovic F, Vickers T, Dyck B, Tamiya J, Grey J, Tran JA, Fleck BA, Pick R, Foster AC, Chen C. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6. Epub 2008 May 23.

Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Tamiya J, Dyck B, Zhang M, Phan K, Fleck BA, Aparicio A, Jovic F, Tran JA, Vickers T, Grey J, Foster AC, Chen C. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3328-32. Epub 2008 Apr 15.

Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Vickers T, Dyck B, Tamiya J, Zhang M, Jovic F, Grey J, Fleck BA, Aparicio A, Johns M, Jin L, Tang H, Foster AC, Chen C. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3230-5. Epub 2008 Apr 25.

Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D. Bioorg Med Chem. 2008 May 15;16(10):5606-18. Epub 2008 Apr 1.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J. J Med Chem. 2008 Mar 27;51(6):1730-9. Epub 2008 Feb 29.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J. J Med Chem. 2008 Mar 27;51(6):1719-29. Epub 2008 Feb 29.

Post-bedtime dosing with indiplon in adults and the elderly: results from two placebo-controlled, active comparator crossover studies in healthy volunteers.
Farber RH, Burke PJ. Curr Med Res Opin. 2008 Mar;24(3):837-46. Epub 2008 Feb 6.

Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series.
Moree WJ, Kataoka K, Ramirez-Weinhouse MM, Shiota T, Imai M, Tsutsumi T, Sudo M, Endo N, Muroga Y, Hada T, Fanning D, Saunders J, Kato Y, Myers PL, Tarby CM. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1869-73. Epub 2008 Feb 10.

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. Epub 2008 Feb 16.

Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.
Tran JA, Tucci FC, Arellano M, Jiang W, Chen CW, Marinkovic D, Fleck BA, Wen J, Foster AC, Chen C. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1931-8. Epub 2008 Feb 7.

Ro5-4864 promotes neonatal motor neuron survival and nerve regeneration in adult rats.
Mills C, Makwana M, Wallace A, Benn S, Schmidt H, Tegeder I, Costigan M, Brown RH Jr, Raivich G, Woolf CJ. Eur J Neurosci. 2008 Feb;27(4):937-46.

Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Chen C, Dyck B, Fleck BA, Foster AC, Grey J, Jovic F, Mesleh M, Phan K, Tamiya J, Vickers T, Zhang M. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. Epub 2008 Jan 9.

Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Slee DH, Zhang X, Moorjani M, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Wen J, O'Brien Z, Saunders J. J Med Chem. 2008 Feb 14;51(3):400-6. Epub 2008 Jan 12.

Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Chen C. Curr Med Chem. 2008;15(21):2173-91. Review.