ライフサイエンスコーパス: piperazinyl

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1 he HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3

2 -2-[2-[4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl ]-2-oxoethoxy]phenyl]urea hydrochloric acid

3 dihydro-6-oxo-5H-dibenz[b,e]az epin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide) (BIIE024

4 pha-R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- hydroxybenzyl)-N,N-diethylbenzamide ([3H

5 lphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydro xybenzyl)-N-(4-fluorophenyl)-N-meth

6 lphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxyben zyl)-N-alkyl-N-arylbenzamides

7 lphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-meth oxybenzyl]-N,N-diethylbenzamide], a

8 [(alphaR)-alpha-(2S,5R)-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxy-benzyl ]-N-N-diethylbenzamide] re

9 lphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenz yl]-N,N-diethylbenzamide), wh

10 lphaR)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzy l]-N,N-diethylbenzamide.

11 pha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N ,N- diethylbenzamide, (+

12 pha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N -diethyl-benzamide (SN

13 pha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N -diethylbenzamide (SNC

14 alphaR)-alpha(2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC-

15 lphaR)-alpha-(2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamide [SNC80

16 f the D4 agonist N-(methyl)-4-(2-cyanophenyl)piperazinyl-3-methylbenzamide maleate caused a reversibl

17 benzamide,4-([2,5-dimethyl-4-(2-propenyl)-1-piperazinyl](3-methoxyphenyl)m ethyl]-N,-,(2S[1(S*),2alp

18 +)-1-[4-[2-[bis(4-fluorophenyl)methoxy]ethyl]piperazinyl]-3-phenylpro pan-2-ol (6) displayed the high

19 , and (S)-(+)-1-[4-[2-(diphenylmethoxy)ethyl]piperazinyl]-3-phenylpropan-2-ol (8) had the highest sel

20 empt to enhance potency, racemic 10-fluoro-9-piperazinyl (35) and related analogues were synthesized

21 nd that the 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazolines can function as p

22 The 2-(piperazinyl) analogues were associated with diminished c

23 t, and -NO(2) groups, including morpholinyl, piperazinyl, and pyrrolidinyl heterocycles, are compatib

24 The 4-piperazinyl- and 4-piperidinyl-substituted 3,4-dihydro-1

25 arge species differences were found, e.g., 2-piperazinyl-AOPCP (21) was >12-fold less potent against

26 and dimeric ligands having 1,3-phenylene-bis(piperazinyl benzimidazole) unit with G-quadruplex DNA (G

27 2,2'-p-Phenylene bis[6-(4-methyl-1-piperazinyl)]benzimidazole, 2,2'-bis(3,5-dihydroxyphenyl

28 kyl-4-[alpha-[(2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl] benzyl]-benzamides were synthesized and eva

29 2-[4-(tert-Butoxycarbonyl)piperazinyl]benzylidene-tert-butanesulfinamides underwen

30 A series of piperazinyl butyl thiazolidinones structurally related t

31 3-amino-N-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl) -2-thiophenecarboxamide (29).

32 3-amino-N-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2 -pyridinecarboxamide (16) and 3-ami

33 (2-amino-N-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)ben zamide hydrochloride) was selected

34 ubstituted (4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)benzamide derivatives was prepared and

35 2-amino-N-(4-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-butyl) benzamide hydrochloride (1), were pr

36 -236 (3-[4-[4-(6-Fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone mal

37 oxamide, N-[2-[[5amino-1-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl]pentyl]amino]-1-[ (3,5-dibromo-4-hy

38 xamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-d ibromo-4-hy

39 henyl)sulfonyl]amino}-3-hydroxypropanoyl)-1 -piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-

40 henyl)sulfonyl]amino}-3-hydroxypropanoyl) -1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-

41 Among the 37 tested biphenylthiazoles, piperazinyl-containing derivatives 10, 30, and 36 were t

42 Of these, the 4'-trifluoromethylarylurea piperazinyl derivative WHN-11 demonstrated cytotoxic act

43 Especially, N-(2-iodoethyl)piperazinyl derivatives were rapidly produced in good yi

44 on 11-labeled N-(2-(1-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl))-N-(2-pyridyl)-cyclohexanecarbo xamid

45 HT1A antagonist [N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexane carboxami

46 antagonist, 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-benzamide hydrochlorid

47 Compound 1, 2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl adamantyl-1-carboxylate, demonstrated

48 use (11C-labeled N-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-(2-pyridinyl)cyclohexaneca rboxamide

49 1D-AR antagonist 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7, 9-dione (BMY

50 )-8-OH-DPAT) and n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-(2-pyridinyl)cyclohe xanecarboxamid

51 cific antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxam id

52 antagonist 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl- benzamide (p-MPPI; 1-1

53 antagonist 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-ben benzamide hydrochlo

54 antagonist 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-ben zamide hydrochlorid

55 receptors, 4-iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-benzamid e (3 mg/kg, i.

56 antagonist, 4-iodo-N-[2-[4(methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-benzamide (3 mg/kg, i.p

57 retreatment with N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexane-ca rboxamide

58 7-[2-[4-[4-(2-[(11)C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-p yrazolo[4,3-e][1,2,4]triazolo[1,5

59 eptor antagonist, N-[2[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]N-(2-pyridinyl)cyclohexanecar boxamide

60 identified 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzox azine-3-

61 h 4-[F-18]fluoro-N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-pyridin yl)benzamide and 2-(1-{6

62 4-[F-18]fluoro-N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-pyridin yl)benzamide, a selectiv

63 We have synthesized N-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(4-18F-fluorom ethylc

64 agonist radioligand N-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(trans-4-(18)F-fluoro

65 tyl-1-carboxylic acid 2-[4-(2-pyrimidinyl)-1-piperazinyl]ethylamide, and 13, adamantyl-1-carboxylic a

66 l-1-carboxylic acid 2-[4-(2-methoxyphenyl)-1-piperazinyl]ethylamide, demonstrated high affinity for 5

67 lel library synthesis was used to discover a piperazinyl glutamate pyridine as a P2Y(12) antagonist.

68 to linker and reversal agent changes, but a piperazinyl group adjacent to the quinoline, at least fo

69 We have replaced the piperazinyl group with a variety of linear, monocyclic,

70 rly potent and selective replacement for the piperazinyl group.

71 -bismethylenecyclopropyl, phenyl, pyridinyl, piperazinyl, homopiperazinyl, and piperidinyl groups wer

72 question mark(2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl inverted question mark-3-methoxybenzyl-N,N-d

73 8 and 1,2,3-triazoles 9 connected via a 1,1'-piperazinyl linker.

74 omophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indol e dimesylate monohydrate (5

75 -2-methoxy-9-acridinyl)amino]-2-[(4-methyl-1-piperazinyl)methyl]] was shown to act synergistically wi

76 N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-pi peridinamine 12 (

77 nt KDR inhibitor 3-[5-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-1H-indole-2-yl]quinolin-2( 1H)-one (

78 razine 1-[3-[[4-[2-(1-methylethoxy)phenyl]-1-piperazinyl]methyl]benzoyl]p ipe ridine (mazapertine, 6)

79 series of antipicornaviral agents containing piperazinyl moieties was synthesized with the objective

80 om substrates (quinoline moieties and phenyl(piperazinyl) moieties, respectively).

81 yl)-5,5-dimethyl-1-cyclohexen-1-yl]methyl}-1-piperazinyl)-N-[(4-{[(2R)-4-(4-morpholinyl)-1-(phenylsul

82 the antibacterial properties of a series of piperazinyl oxazolidinones in which the distal nitrogen

83 no-3-pyridinyl)sulfonyl)-2-(1-propyn-1-yl)-1-piperazinyl)phen yl)-1,1,1,3,3,3-hexafluoro-2-propanol (

84 es, 6-(2,6-dimethylphenyl)-2-((4-(4-methyl-1-piperazinyl)phenyl)amino)pyrimido[5',4': 5,6]pyrimido-[1

85 ith this strategy, we identified a family of piperazinyl phenylethanone compounds as inhibitors of tr

86 This quinolyl-piperazinyl piperidine analogue displayed potent, select

87 a small-molecule allosteric ligand from the piperazinyl-piperidine class, also known as VUF11211 [(S

88 -ethylpiperazin-1-yl)-N-et hylnicotinamide] (piperazinyl-piperidine) with a rigid elongated structure

89 ngener OPC4392 [7-[3-(4-(2,3-dimethylphenyl) piperazinyl) propoxy] 2-(1H)-quinolinone].

90 nyl 2-((3,5-bis(methyloxy)-4-((3-(4-methyl-1-piperazinyl)propyl)oxy)phenyl)ami no)-4-pyrimidinyl(2,4-

91 nds were prepared, based on a series of 3-(1-piperazinyl)propyl-N,N-bis(4-fluorophenyl)amines, as mol

92 9-[3-(cis-3,5-Dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) has been charac

93 based on rimcazole (9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole, 2), a compound that has be

94 A 5-HT2C selective agonist, 6-chloro-2-[1-piperazinyl]-pyrazine (MK-212, 5 mg/kg, s.c.) also inhib

95 d and successfully synthesized two series of piperazinyl pyrrolidin-2-one derivatives as novel revers

96 , CT52923, a potent selective small molecule piperazinyl quinazoline kinase inhibitor of the PDGFR, w

97 amined whether doxazosin and terazosin (both piperazinyl quinazolines) affect prostate growth via an

98 yl) piperazine hydrochloride (TFMPP) or 2-(1-piperazinyl) quinoline dimaleate (quipazine).

99 the non-selective 5-HT receptor agents, 2-(1-piperazinyl)quinoline dimaleate (quipazine) and N-(3-tri

100 The 6-amino-7-[4-(2-pyridinyl)-1-piperazinyl]quinolone derivative 8 proved to be the best

101 idinones in which the distal nitrogen of the piperazinyl ring is substituted with a six-membered hete

102 y N-acetylation at the amino nitrogen on its piperazinyl substituent.

103 N,N-dialkyl, pyrrolidinyl, piperidinyl, and piperazinyl substituents at the 2-position of the 5-ethy

104 the title compound was constructed from the piperazinyl terminus via a Pinner-type cyclization follo

105 ves bridged to 4-(1,2-benzisothiazol-3-yl)-1-piperazinyl was prepared.