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4 selectivity. J Am Chem Soc 1998, 120:1368-1373. The first potent, selective nonpeptidic somatostatin receptor subtype 4 agonists, identified through a directed screening approach using peptide pharmacophore information, are described.
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Potent, orally bioavailable somatostatin agonists: Good absorption achieved by urea backbone cyclization
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Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry
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Xiong, Y.7
Hayes, E.C.8
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15444355594
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Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor
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Cho N, Harada M, Imaeda T, Imada T, Matsumoto H, Hayase Y, Sasaki S, Furuya S, Suzuki N, Okubo S et al.: Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J Med Chem 1998, 41:4190-4195.
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Distinct mechanism for antidepressant activity by blockade of central substance P receptors
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Kramer MS, Cutler N, Feighner J, Shrivastava R, Carman J, Sramek JJ, Reines SA, Liu G, Snavely D, Wyatt-Knowles E et al.: Distinct mechanism for antidepressant activity by blockade of central substance P receptors. Science 1998, 281:1640-1645. This paper describes the discovery of a new mechanistic approach for treating depression.
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Science
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Liu, G.8
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Wyatt-Knowles, E.10
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15144354434
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Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist
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Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J et al.: Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist. J Med Chem 1998, 41:4607-4614.
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J Med Chem
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Hale, J.J.1
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1 antagonists: Structure-activity relationships and in vivo activity. J Med Chem 1998, 41:4623-4635.
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J Med Chem
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Chicchi, G.G.6
Graham, M.I.7
Harrison, T.8
Kelleher, F.J.9
Kurtz, M.10
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15644373566
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1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models
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1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J Med Chem 1998, 41:3159-3173.
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J Med Chem
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Walpole, C.1
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Hughes, G.A.8
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Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist
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Rosen TJ, Coffman KJ, McLean S, Crawford RT, Bryce DK, Gohda Y, Tsuchiya M, Nagahisa A, Nakane M, Lowe JA III: Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist. Bioorg Med Chem Lett 1998, 8:281-284.
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Bioorg Med Chem Lett
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Rosen, T.J.1
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Gohda, Y.6
Tsuchiya, M.7
Nagahisa, A.8
Nakane, M.9
Lowe J.A. III10
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0032474518
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High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template
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Harrison T, Korsgaard MPG, Swain CJ, Cascieri MA, Sadowski S, Seabrook GR: High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template. Bioorg Med Chem Lett 1998, 8:1343-1348.
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Bioorg Med Chem Lett
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Harrison, T.1
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15644374841
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2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man
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2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man. J Med Chem 1998, 41:4055-4061. This paper describes the identification of the first potent, orally active bradykinin receptor antagonists.
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J Med Chem
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Abe, Y.1
Kayakiri, H.2
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Inamura, N.6
Asano, M.7
Hatori, C.8
Sawai, H.9
Oku, T.10
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15644367578
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2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a]pyridine moiety. J Med Chem 1998, 41:4062-4079.
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J Med Chem
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Abe, Y.1
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Asano, M.7
Aramori, I.8
Hatori, C.9
Sawai, H.10
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14444267777
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2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation
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2 receptor antagonists. 4. Discovery of novel frameworks mimicking the active conformation. J Med Chem 1998, 41:4587-4598.
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J Med Chem
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Abe, Y.1
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Asano, M.7
Aramori, I.8
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Sawai, H.10
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15444343988
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2 receptor antagonist, FR165649, and agonist, FR190997
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2 receptor antagonist, FR165649, and agonist, FR190997. Br J Pharmacol 1998, 124:441-446. This is an example of a modest structural change that switches an antagonist to an agonist.
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Br J Pharmacol
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Asano, M.1
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Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential
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Nargund RP, Patchett AA, Bach MA, Murphy MG, Smith RG: Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential. J Med Chem 1998, 41:3103-3127.
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J Med Chem
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Nargund, R.P.1
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7344221463
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1-[2(R)-(2-Amino-2-methylpropionyl-amino)-3-(1H-indol-3-yl)propionyl]-3-benzylpiperidine-3(S)-carboxylic acid ethyl ester (L-163,540): A potent, orally bioavailable, and short-duration growth hormone secretagogue
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Yang L, Morriello G, Patchett AA, Leung K, Jacks T, Cheng K, Schleim KD, Feeney W, Chan WW-S, Chiu S-Hl et al.: 1-[2(R)-(2-Amino-2-methylpropionyl-amino)-3-(1H-indol-3-yl)propionyl]-3-benzylpiperidine-3(S)-carboxylic acid ethyl ester (L-163,540): A potent, orally bioavailable, and short-duration growth hormone secretagogue. J Med Chem 1998, 41:2439-2441.
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J Med Chem
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Yang, L.1
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Feeney, W.8
Chan, W.W.S.9
Chiu, S.-H.L.10
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15644383589
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A potent, orally bioavailable benzazepinone growth hormone secretagogue
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DeVita RJ, Bochis R, Frontier AJ, Kotliar A, Fisher MH, Schoen WR, Wyvratt MJ, Cheng K, Chan Ww-S, Butler B et al.: A potent, orally bioavailable benzazepinone growth hormone secretagogue. J Med Chem 1998, 41:1716-1728.
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J Med Chem
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DeVita, R.J.1
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Cheng, K.8
Chan, W.W.-S.9
Butler, B.10
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15644365787
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Novel orally active growth hormone secretagogues
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Hansen TK, Ankersen M, Hansen BS, Raun K, Nielsen KK, Lau J, Peschke B, Lundt BF, THøgersen H, Johansen NL et al.: Novel orally active growth hormone secretagogues. J Med Chem 1998, 41:3705-3714.
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J Med Chem
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Hansen, T.K.1
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Lau, J.6
Peschke, B.7
Lundt, B.F.8
Thøgersen, H.9
Johansen, N.L.10
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15144345928
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Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives
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Astles PC, Brealey C, Brown TJ, Facchini V, Handscombe C, Harris NV, McCarthy C, McLay IM, Porter B, Roach AG et al.: Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives. J Med Chem 1998, 41:2732-2744.
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J Med Chem
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Astles, P.C.1
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Harris, N.V.6
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McLay, I.M.8
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Roach, A.G.10
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26
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15144360873
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a antagonist (A-216546)
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a antagonist (A-216546). J Med Chem 1998, 41:3261-3275.
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J Med Chem
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Liu, G.1
Henry K.J., Jr.2
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Von Geldern, T.W.8
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0032542312
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Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono-and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2′-amino-N-(3,4-dimethyl-5-isoxazolyl)-4′-(2-methylpropyl)[1,1′biphenyl]-2-sulfonamide (BMS-187308)
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Murugesan N, Gu Z, Stein PD, Bisaha S, Spergel S, Girotra R, Lee VG, Lloyd J, Misra RN, Schmidt J et al.: Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono-and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2′-amino-N-(3,4-dimethyl-5-soxazolyl)-4′-(2-methylpropyl)[1,1′biphenyl]-2-sulfonamide (BMS-187308). J Med Chem 1998, 41:5198-5218.
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J Med Chem
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Murugesan, N.1
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Lee, V.G.7
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Schmidt, J.10
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a selective antagonist. Bioorg Med Chem Lett 1998, 8:1771-1776.
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Bioorg Med Chem Lett
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Mederski, W.W.K.R.1
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Stereoselective synthesis of a novel and bifunctional endothelin antagonist IRL 3630
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Sakaki J, Murata T, Yuumoto Y, Nakamura I, Hayakawa K: Stereoselective synthesis of a novel and bifunctional endothelin antagonist IRL 3630. Bioorg Med Chem Lett 1998, 8:2247-2252.
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Bioorg Med Chem Lett
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Sakaki, J.1
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Cho N, Nara Y, Harada M, Sugo T, Musuda Y, Abe A, Kusumoto K, Itoh Y, Ohtaki T, Watanabe T et al.: Thieno[2,3-d]pyrimidine-3-acetic acids, a new class of nonpeptide endothelin receptor antagonists. Chem Pharm Bull 1998, 46:1724-1737.
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Chem Pharm Bull
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Studies on nonpeptide angiotensin II receptor antagonists. II. Synthesis and biological evaluation of 5H-Pyrazolo[1,5-b][1,2,4]triazole derivatives with a c-linked oxygen functional group at the 6-position
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Okazaki T, Suga A, Watanabe T, Kikuchi K, Kurihara H, Shibasaki M, Fujimori A, Inagaki O, Yanagisawa I: Studies on nonpeptide angiotensin II receptor antagonists. II. Synthesis and biological evaluation of 5H-Pyrazolo[1,5-b][1,2,4]triazole derivatives with a c-linked oxygen functional group at the 6-position. Chem Pharm Bull 1998, 46:287-293.
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Chem Pharm Bull
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Okazaki, T.1
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2 receptors. J Med Chem 1998, 41:2442-2444.
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J Med Chem
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Albright, J.D.1
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2-receptor antagonist: Pharmacological profile and aquaretic effect by single and multiple oral dosing in rats
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2-receptor antagonist: Pharmacological profile and aquaretic effect by single and multiple oral dosing in rats. J Pharmacol Exp Ther 1998, 287:860-867.
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J Pharmacol Exp Ther
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Tsujimae, K.8
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Kotosai, K.10
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15644378251
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Development of orally active oxytocin antagonists: Studies on 1-(1{4-1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy-2-methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenzd1,3oxazin-2-one (L-372,662) and related pyridines
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Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS et al.: Development of orally active oxytocin antagonists: Studies on 1-(1{4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2-methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines. J Med Chem 1998, 41:2146-2163.
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J Med Chem
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Bell, I.M.1
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Guidotti, M.T.6
Halpin, R.A.7
Hobbs, D.W.8
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Kuo, M.S.10
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Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists
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Zarrinmayeh H, Zimmerman DM, Cantrell BE, Schober DA, Bruns RF, Gackenheimer SL, Ornstein PL, Hipskind PA, Britton TC, Gehlert DR: Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists. Bioorg Med Chem Lett 1999, 9:647-652.
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Bioorg Med Chem Lett
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0032558515
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2) receptor antagonist
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2) receptor antagonist. Bioorg Med Chem Lett 1998, 8:2589-2594. This is another example of the peptoid approach to designing nonpeptidic receptor ligands.
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Bioorg Med Chem Lett
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Ashwood, V.1
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De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the δ-opioid receptor
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Liao S, Alfaro-Lopez J, Shenderovich MD, Hosohata K, Lin J, Li X, Stropova D, Davis P, Jernigan KA, Porreca F et al.: De novo design, synthesis, and biological activities of high-affinity and selective non-peptide agonists of the δ-opioid receptor. J Med Chem 1998, 41:4767-4776. The design of a potent nonpeptidic agonist, which mimics the structure and activity of a conformationally constrained cyclic peptide, is described.
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J Med Chem
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Liao, S.1
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Davis, P.8
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