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Page 1
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.
Stevenson GI, Huscroft I, MacLeod AM, Swain CJ, Cascieri MA, Chicchi GG, Graham MI, Harrison T, Kelleher FJ, Kurtz M, Ladduwahetty T, Merchant KJ, Metzger JM, MacIntyre DE, Sadowski S, Sohal B, Owens AP. Stevenson GI, et al. Among authors: sadowski s. J Med Chem. 1998 Nov 5;41(23):4623-35. doi: 10.1021/jm980376b. J Med Chem. 1998. PMID: 9804702
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
Seward EM, Carlson E, Harrison T, Haworth KR, Herbert R, Kelleher FJ, Kurtz MM, Moseley J, Owen SN, Owens AP, Sadowski SJ, Swain CJ, Williams BJ. Seward EM, et al. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2515-8. doi: 10.1016/s0960-894x(02)00506-1. Bioorg Med Chem Lett. 2002. PMID: 12182850
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Finke PE, Meurer LC, Levorse DA, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Metzger JM, Macintyre DE. Finke PE, et al. Among authors: sadowski s. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4497-503. doi: 10.1016/j.bmcl.2006.06.035. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824752
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
Meurer LC, Finke PE, Owens KA, Tsou NN, Ball RG, Mills SG, Maccoss M, Sadowski S, Cascieri MA, Tsao KL, Chicchi GG, Egger LA, Luell S, Metzger JM, Macintyre DE, Rupniak NM, Williams AR, Hargreaves RJ. Meurer LC, et al. Among authors: sadowski s. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4504-11. doi: 10.1016/j.bmcl.2006.06.044. Epub 2006 Jul 10. Bioorg Med Chem Lett. 2006. PMID: 16831551
L-tryptophan urea amides as NK1/NK2 dual antagonists.
Qi H, Shah SK, Cascieri MA, Sadowski SJ, MaCcoss M. Qi H, et al. Among authors: sadowski sj. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2259-62. doi: 10.1016/s0960-894x(98)00395-3. Bioorg Med Chem Lett. 1998. PMID: 9873524
Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor.
Cascieri MA, Macleod AM, Underwood D, Shiao LL, Ber E, Sadowski S, Yu H, Merchant KJ, Swain CJ, Strader CD, et al. Cascieri MA, et al. Among authors: sadowski s. J Biol Chem. 1994 Mar 4;269(9):6587-91. J Biol Chem. 1994. PMID: 7509807 Free article.
M., Merchant, K. J., Cascieri, M. A., Sadowski, S., Ber, E., Swain, C. J., and Baker, R. (1993) J. Med Chem. 14, 2044-2045). We now report the detailed characterization of the interaction of N-acetyl-L-tryptophan-3,5-bistrifluoromethyl benzyl ester (L-732,138) with …
M., Merchant, K. J., Cascieri, M. A., Sadowski, S., Ber, E., Swain, C. J., and Baker, R. (1993) J. Med Chem. 14, 2044-2045). W …
4,4-Disubstituted piperidines: a new class of NK1 antagonist.
Stevenson GI, MacLeod AM, Huscroft I, Cascieri MA, Sadowski S, Baker R. Stevenson GI, et al. Among authors: sadowski s. J Med Chem. 1995 Apr 14;38(8):1264-6. doi: 10.1021/jm00008a003. J Med Chem. 1995. PMID: 7731011 No abstract available.
163 results