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The following terms were ignored: [, ]
The following terms were not found in PubMed: 1-benzyl-4-phenyl-4H-pyrimidin-2-yl
Page 1
Synthetic analgesics: N-(1-[2-arylethyl]-4-substituted 4-piperidinyl) N-arylalkanamides.
Van Daele PG, De Bruyn MF, Boey JM, Sanczuk S, Agten JT, Janssen PA. Van Daele PG, et al. Arzneimittelforschung. 1976;26(8):1521-31. doi: 10.1002/chin.197646236. Arzneimittelforschung. 1976. PMID: 12769
Thus, methyl 4-[N-(1-oxopropyl)-N-phenylamino]-1-(2-phenylethyl)-4-piperidinecarboxylate (22),N-(4-(methoxymethyl)-2-[2-(2-thienyl)ethyl]-4-piperidinyl)-N-phenylpropranamide (67) and N-[4-acetyl-1-(2-phenylethyl)-4-piperidinyl]-N-phenylpropanamide (82) …
Thus, methyl 4-[N-(1-oxopropyl)-N-phenylamino]-1-(2-phenylethyl)-4-piperidinecarboxylate (22),N-(4-(methoxymethyl)-2-[2-(2- …
Bronchodilator activity of (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407), a potent, long-acting, and selective muscarinic M3 receptor antagonist.
Villetti G, Pastore F, Bergamaschi M, Bassani F, Bolzoni PT, Battipaglia L, Amari G, Rizzi A, Delcanale M, Volta R, Cenacchi V, Cacciani F, Zaniboni M, Berti F, Rossoni G, Harrison S, Petrillo P, Santoro E, Scudellaro R, Mannini F, Geppetti PA, Razzetti R, Patacchini R, Civelli M. Villetti G, et al. J Pharmacol Exp Ther. 2010 Dec;335(3):622-35. doi: 10.1124/jpet.110.170035. Epub 2010 Aug 30. J Pharmacol Exp Ther. 2010. PMID: 20805306
The novel quaternary ammonium salt (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407) showed subnanomolar affinities for human muscarinic M1 (hM1), M2 …
The novel quaternary ammonium salt (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]carbonyl]oxy]-1-[2-oxo-2-(2- …
N-4-Substituted 1-(2-arylethyl)-4-piperidinyl-N-phenylpropanamides, a novel series of extremely potent analgesics with unusually high safety margin.
Van Bever WF, Niemegeers CJ, Schellekens KH, Janssen PA. Van Bever WF, et al. Arzneimittelforschung. 1976;26(8):1548-51. Arzneimittelforschung. 1976. PMID: 12771
Methyl 4-[N-(1-oxopropyl)-N-phenyl-amino]-1-(2-phenylethyl)-4-piperidinecarboxylate (R 31 833; lowest ED50 = 0.00032 mg/kg) is the most potent compound (10 031 times morphine). cis-Methyl 3-methyl-4-[N-(1-oxopropyl)-N-phenylamino]-1-(2-phenylethyl)-4-piperidine carboxylate (R 32 …
Methyl 4-[N-(1-oxopropyl)-N-phenyl-amino]-1-(2-phenylethyl)-4-piperidinecarboxylate (R 31 833; lowest ED50 = 0.00032 mg/kg) is the most pote …
1-(Thienylalkyl)imidazole-2(3H)-thiones as potent competitive inhibitors of dopamine beta-hydroxylase.
McCarthy JR, Matthews DP, Broersma RJ, McDermott RD, Kastner PR, Hornsperger JM, Demeter DA, Weintraub HJ, Whitten JP. McCarthy JR, et al. J Med Chem. 1990 Jul;33(7):1866-73. doi: 10.1021/jm00169a006. J Med Chem. 1990. PMID: 2362264
The difference in activity is consistent with our proposal that thiophene may not always be a bioisostere for phenyl. The inhibitor of most interest, 1-[2-(2-thienyl)ethyl]imidazole-2(3H)-thione (5g), was selected for study in the spontaneously hyperte …
The difference in activity is consistent with our proposal that thiophene may not always be a bioisostere for phenyl. The inhibitor of most …
Sufentanil, a very potent and extremely safe intravenous morphine-like compound in mice, rats and dogs.
Niemegeers CJ, Schellekens KH, Van Bever WF, Janssen PA. Niemegeers CJ, et al. Arzneimittelforschung. 1976;26(8):1551-6. Arzneimittelforschung. 1976. PMID: 12772
Sufentanil (R 30 730), N-[4-methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenylpropanamide, is a chemically novel, highly potent and extremely safe intravenous morphine-like agent in laboratory animals. ...
Sufentanil (R 30 730), N-[4-methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenylpropanamide, is a chemi …