ライフサイエンスコーパス: piperazine

1 luorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine).

2 utenyl linker between the aryl amide and the piperazine.

3 d molecular properties of IRK1 inhibition by piperazine.

4 with paraformaldehyde and 1-(diphenylmethyl)piperazine.

5 e 2-benzyl morpholine and N-methyl camphanyl piperazine.

6 on 1-N,N'-dimethylsulfamoyl-1-4-(2-pyrimidyl)piperazine.

7 f a set of 1-(3-biphenyl)- and 1-(2-biphenyl)piperazines.

8 ed: bicyclic guanidines, and pyrrolidine bis-piperazines.

9 for the racemic lithiation/trapping of N-Boc piperazines.

10 ective synthesis of 2,5-trans- and 2,6-trans-piperazines.

11 e concept through a direct synthesis of aryl piperazines.

12 d a wide range of alpha-functionalized N-Boc piperazines.

13 thylketones yields alpha-CF3 morpholines and piperazines.

14 luorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (1) and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phe

15 the investigated 1,4-disubstituted aromatic piperazines (1,4-DAPs) behaved as antagonists for beta-a

16 ty of 1,4-disubstituted aromatic piperidines/piperazines (1,4-DAPs) with different subtype selectivit

17 -thiazolo[5,4-b]pyridin-2-yl)-2-[4-(4-methyl-piperazine -1-sulfonyl)-phenyl]-propionamide (17c).

18 alysis indicates that for the reactions with piperazine, 1-(2-hydroxyethyl)piperazine, and morpholine

19 the reversible deprotonation of 2-NO(2)() by piperazine, 1-(2-hydroxyethyl)piperazine, and morpholine

20 Piperazine-1,4-diylbis(6-benzo[d]imidazole-2-yl)pyridine

21 ied [2,4-dinitrophenyl-4-(4-tert-butylbenzyl)piperazine-1-carbodithioate] (CK37), as the most potent

22 ogues, among them the 10-(4-(3-methoxyphenyl)piperazine-1-carbonyl)-10H-phenoxazine-3-carbonitrile (1

23 mistry optimization of 2-pyridinyl-N-(4-aryl)piperazine-1-carbothioamides, which exhibit submicromola

24 (4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide (BCTC) and clotrimazole or by e

25 (PF-750) and N-phenyl-4-(quinolin-2-ylmethyl)piperazine-1-carboxamide (PF-622) as a novel mechanistic

26 hanesulfonic acid (HEPES), 4-(2-hydroxyethyl)piperazine-1-propanesulfonic acid (HEPPS), and N-(2-hydr

27 Analogues of N,N-dimethyl-4-(pyrimidin-2-yl)piperazine-1-sulfonamide possessing a free radical scave

28 HTS hits, e.g. 5-(4-(2-(4-bromophenoxy)ethyl)piperazine-1-yl)-1H-1,2,4-triazol-3-amine 1, spanned fro

29 d by the D4 antagonist 3-[(4-[4-chlorophenyl]piperazine-1-yl)methyl]-[1H]-pyrrolo[2,3-b]pyridine but

30 of biphenyl-N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates, a novel class of molec

31 one) and Cimbi-717 (3-{4-[4-(3-methoxyphenyl)piperazine-1-yl]butyl}-1,3-dihydro-2H-indol-2-one) as se

32 uation of Cimbi-712 (3-{4-[4-(4-methylphenyl)piperazine-1-yl]butyl}p-1,3-dihydro-2H-indol-2-one) and

33 The (m-nitrophenethyl)piperazine 10 exhibits a subnanomolar affinity for the s

34 Piperazine 10 is a 5-HT(1A) agonist with an EC(50) compa

35 -4-[(2R )-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazin

36 y)-ethyl]-4-[2-(4-azido-3-iodophenyl) ethyl] piperazine ([125I]DEEP), a 1-(2-diphenylmethoxy)-ethyl-4

37 [2'-[N-(2'-pyridinyl)-p-iodobenzamido ]ethyl]piperazine ([125I]p-MPPI), a selective antagonist of 5-H

38 Arylpiperazines such as (heteroarylmethyl)piperazine 1a, benzamide 2, and acetamides such as 3a,b

39 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (1a) and 1-[2-[bis(4-fluorophenyl)methoxy]eth

40 luorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (1b) (GBR 12935 and GBR 12909, respectively),

41 saturated rings on morpholine 1 and N-acetyl piperazine 2 were changed by a single atom to tetrahydro

42 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) (GBR 12909 and GBR 12935, respectively) w

43 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) and 1- inverted question mark2-[bis(4-flu

44 The piperazine (+/-)-2 was synthesized, and its enantiomers

45 antagonist (2R,3S)-(1-biphenylyl-4-carbonyl)piperazine-2,3-dicarboxylic acid (PBPD, 16b) displays an

46 acid (D-AP5) and 1-(phenanthrene-2-carbonyl)piperazine-2,3-dicarboxylic acid (PPDA), have discrete b

47 hat some N(1)-substituted derivatives of cis-piperazine-2,3-dicarboxylic acid display improved relati

48 ubstituents attached to the N(1) position of piperazine-2,3-dicarboxylic acid have been synthesized t

49 The title 1,4-piperazine-2,5-dione was synthesized in 23% yield over s

50 Piperazine-2,5-diones are formed by Dieckmann cyclizatio

51 cally active and commercially available (2S)-piperazine-2-carboxylic acid dihydrochloride.

52 a variety of highly enantioenriched tertiary piperazine-2-ones.

53 luorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine] (2) analogs was synthesized and evaluated as

54 hyl inverted question mark-4-(3-phenylpropyl)piperazine (3) (GBR 12935 and GBR 12909, respectively),

55 -3-indolyl)cyclohexyl]ethyl]-4- (2-pyridinyl)piperazine (30a) was selected for further evaluation.

56 ee amino group of arylated diazeniumdiolated piperazine 4.

57 o-piperazine, phenyl- and benzyl-substituted piperazines, 4-aminomethylpiperidine, 4-aminophenylethyl

58 ylcyclopropyl)methyl]-4-(2, 4-dichlorophenyl)piperazine (5m) and (1S, 2S)-trans-1-[(2-phenylcycloprop

59 ylcyclopropyl)methyl]-4-(2, 4-dimethylphenyl)piperazine (5t) were selected for functional antagonists

60 olates studied, but N,N'-bis(4-amidinophenyl)piperazine (6) was the most effective agent in vivo agai

61 gent route involving addition of an acylated piperazine 7 to 2-chloroquinazoline 5.

62 , and either an alkyne (6), triazole (7), or piperazine (8) link to the PBD.

63 d N-phenylpropyl 3-methyl-4-(3-hydroxyphenyl)piperazines (8a,b) gives (4a,b), which are opioid antago

64 1-[2-(4-Methoxyphenyl)phenyl]piperazine (9a) showed 5-HT(7) agonist properties in a g

65 orophenyl)-methoxy]ethyl]-4-[3- phenylpropyl]piperazine), a specific blocker of the dopamine transpor

66 N-(3-Trifluoromethylphenyl)piperazine, a 5-HT(1B) receptor agonist, potently inhibi

67 ylamino)piperidine-containing bis(heteroaryl)piperazine (AAP-BHAP) class of non-nucleoside reverse tr

68 line A, a highly strained and reduced fungal piperazine alkaloid.

69 ategy to evaluate a newly described class of piperazine amide reversible inhibitors for the serine hy

70 Competitive ABPP identified individual piperazine amides that selectively inhibit LYPLA1 or LYP

71 ve 37, (Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172), a novel P

72 Interestingly, previous studies showed that piperazine, an inexpensive and safe anthelmintic, both i

73 ride (LDK1229), from the class of benzhydryl piperazine analogs.

74 The N(6)-(4-Trifluoromethylphenyl)piperazine analogue 11 displayed the best antitumor acti

75 We also examine the channel selectivity of piperazine and its molecular determinants.

76 r scaffolds of 1-arylpyrazole-4-arylsulfonyl-piperazine and spiro-piperidine-quinazolinone classes we

77 R)/(S)-BINOL, diethyl tartrate) and achiral (piperazine and trigol) linkers with varying stereogenic

78 s and antifungal activity of novel alkylated piperazines and alkylated piperazine-azole hybrids, thei

79 We conclude that pyrrolidine bis-piperazines and bicyclic guanidines represent promising

80 plained differential activities of the above piperazines and piperidines.

81 osubstituted and symmetrically disubstituted piperazines and trans-2,5-dimethylpiperazines, which lac

82 luorophenyl)methoxy)ethyl]-4-(3-phenylpropyl)piperazine ] and WIN 35,428 [3beta-(p-fluorophenyl)-2bet

83 iamines (R2N(CH2)nNR2, R = H, CH3; n = 1-4), piperazine, and 1,4-dimethylpiperazine to the cumyloxyl

84 l), tri(ethylene glycol), N,N'-disubstituted-piperazine, and 2-butyne-1,4-diol.

85 f 2-NO(2)() by piperazine, 1-(2-hydroxyethyl)piperazine, and morpholine in the same solvent.

86 reactions with piperazine, 1-(2-hydroxyethyl)piperazine, and morpholine it is deprotonation of T(+/-)

87 1,4-Disubstituted aromatic piperazines are privileged structural motifs recognized

88 The new non-peptide ligands use piperazine as a template to present the most important p

89 was generally poor, the use of 1-(2-pyridyl)piperazine as the amide component usually provided for e

90 surrogate and provides access to a range of piperazines (as single stereoisomers).

91 Piperazine, as an effective CO2-philic agent, is introdu

92 Methyl substitution of the piperazine at the 2- and 5-positions (with S and R absol

93 we demonstrate that the synthetic alkylated piperazine-azole hybrids do not function by fungal membr

94 of novel alkylated piperazines and alkylated piperazine-azole hybrids, their time-kill studies, their

95 tion based on a phenylpyrazole glutamic acid piperazine backbone is described.

96 ties afforded Sch-350634 (1), a prototypical piperazine-based CCR5 antagonist, which is a potent inhi

97 eloped for a large series of piperidine- and piperazine-based CCR5 antagonists as anti-HIV-1 agents r

98 ly identified a series of mitotically acting piperazine-based compounds that potently increase the se

99 mount of ENRO and other structurally related piperazine-based fluoroquinolones that bind to the MIP.

100 ctivity relationships study of aminotetralin-piperazine-based hybrid molecules developed earlier for

101 for the piperidine compounds relative to the piperazine-based ligands appear to arise as a consequenc

102 field analysis (CoMFA) for a novel series of piperazine-based matrix metalloproteinase inhibitors (MM

103 ns defining an overall scaffold geometry for piperazine-based MMP inhibitors.

104 hange of the linking oxygen for nitrogen (or piperazine), biaryl extension, and replacement of phenyl

105 anthracene and benzhydryl moieties through a piperazine bridge.

106 Bisquinolines with alkyl ether and piperazine bridges were substantially more effective tha

107 (pyrrolidines, piperidines, morpholines, and piperazines) by the cumyloxyl (CumO(*)) and benzyloxyl (

108 ly low IC(50) value of the N-(ethoxycarbonyl)piperazine byproduct of NO release suggests a role for t

109 tion forming MNPZ is first order in nitrite, piperazine carbamate species, and hydronium ion.

110 ips, and inhibitory activities of piperidine/piperazine carbamates against members of the serine hydr

111 Piperidine/piperazine carbamates show excellent in vivo activity, r

112 Additionally, a series of alkyl bridged piperazine carboxamides was identified as being of parti

113 Moreover, the energy barrier for the piperazine carboxylate was significantly lower than that

114 e synthesized a series of N,N'-disubstituted piperazine compounds (1-32).

115 These efforts led to the discovery of a piperazine-containing analogue, 17g (WY-46824), that exh

116 y a role in the antimalarial activity of the piperazine-containing compound ACT-213615.

117 We report that the piperazine-containing compound ACT-451840 exhibits singl

118 are an asymmetric synthesis of the 2-alkynyl piperazine core via a base-promoted isomerization and a

119 our was used to design agonists containing a piperazine core.

120 The piperazine derivative 54 displayed especially promising

121 rently in phase III clinical trials, and the piperazine derivative eperezolid 3.

122 Ranolazine, a piperazine derivative, reduces ischemia via inhibition o

123 These tests indicated that piperazine derivatives 4b and 4d may be suitable for coa

124 iphenylpiperazine and the 2,3-bis(1-naphthyl)piperazine derivatives are prepared by a resolution meth

125 ienyl(1,4-dichlorobenzene)ruthenium by using piperazine derivatives as nucleophiles is addressed.

126 the A2a binding affinity of some of the best piperazine derivatives is almost as good as that of comp

127 Piperazine derivatives of 2-furanyl[1,2,4]triazolo[1,5-a

128 A series of bicyclic piperazine derivatives of triazolotriazine and triazolop

129 A series of novel benzothiazole-piperazine derivatives that inhibit NAAA in a potent and

130 s now been improved by incorporating various piperazine derivatives.

131 linear region to less than 1% for one of the piperazine derivatives.

132 to the optimization of a series of acylated piperazine derivatives.

133 More significantly, some piperazines derivatives of [1,2,4]triazolo[1,5-a]triazin

134 We have discovered a novel piperazine-derived compound, EVT901, which interferes wi

135 tebrate receptor agonist, 1-(3-Chlorophenyl) piperazine dihydrochloride (m-CPP), for 1 week resulted

136 -(3,4-dimethoxyphenthyl)]-4-(3-phenylpropyl)-piperazine dihydrochloride) in tumor and brain and to ev

137 drug, 1,4-bis[N,N'-di(ethylene)-phosphamide]piperazine (Dipin) 2 hours before PH.

138 agent 1,4-bis[N,N'-di(ethylene)-phosphamide]piperazine (Dipin), followed by partial hepatectomy, dec

139 yl, amide, carbamide and sulfonamide) on the piperazine distal nitrogen, yielded the most predictive

140 Z, Rac-2), an over-the-counter antihistamine piperazine drug, possesses in vitro and in vivo activity

141 e and L = dansyl-imidazole (Ds-im) or dansyl-piperazine (Ds-pip).

142 owards structural analogs (aspirin, BPA, and piperazine) even in a mixture.

143 her convertases was limited: pyrrolidine bis-piperazines exhibited K(i) values greater than 25 microM

144 To provide alpha-substituted piperazines for early stage medicinal chemistry studies,

145 he piperazine moiety was replaced by bridged piperazines for structural rigidity, has been designed,

146 cture 2, 6-bis(omega-aminobutyl)-3,5-diimino-piperazine (for which we suggest the name "batrachamine"

147 zole, a scalable synthesis of an enantiopure piperazine fragment, and identification of conditions fo

148 -(diphenylmethoxyl) ethyl]-4-(3phenylpropyl) piperazine (GBR 12909), mazindol, 2beta-carbomethoxy-3be

149 2-(diphenylmethoxy)-ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935).

150 (2-diphenylmethoxy)-ethyl-4-(3-phenyl propyl)piperazine (GBR analog), and [125I]-3beta-(p-chloropheny

151 N-[2-(bisarylmethoxy)ethyl]-N'-(phenylpropyl)piperazines, GBR 12909 and 12935, were synthesized and e

152 uorophenyl)methoxy]ethyl)- 4-(3-phenylpropyl)piperazine (GBR12909) in vivo.

153 ibited by carbamates bearing an N-piperidine/piperazine group.

154 ptimally possessed tertiary dimethylamine or piperazine groups and potential buffering capacity.

155 that two of the four strongly basic N-methyl-piperazine groups can be replaced by less basic morpholi

156 action; 1-(5-isoquinolinylsulfonyl)-2-methyl-piperazine (H-7), a proposed myosin light-chain kinase i

157 ne and 1-(5-isoquinolinylsulphonyl)-2-methyl-piperazine (H-7).

158 ries of para-substituted 4-phenylpiperidines/piperazines have been synthesized and their affinity to

159 1-[3-(Trifluoromethyl)phenyl]-piperazine HCl (TFMPP), a 5-HT1B receptor agonist, reduc

160 e (quipazine) and N-(3-trifluoromethylphenyl)piperazine HCl (TFMPP).

161 ontains an organic alkali 1-(2-hydroxyethyl) piperazine (HEP), is used for CO2 absorption.

162 orophenyl] methoxy]ethyl)-4-(3-phenylpropyl) piperazine hydrochloride (GBR-12909).

163 e 5-HT2C receptor agonist 1-(m-chlorophenyl)-piperazine hydrochloride (mCPP), which enhances weight-s

164 0 or 2000 ng of N-(3-trifluoro-methylphenyl) piperazine hydrochloride (TFMPP) or 2-(1-piperazinyl) qu

165 2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-piperazine] (I) and GBR 12909 [1-[2-[bis(4-fluorophenyl)

166 groups and the synthesis of a bioactive aryl piperazine in an expeditious four-step sequence.

167 analogues (9-13) containing a 4-substituted piperazine in the substituent at N(6) were synthesized a

168 that the piperidine in 6ANI is replaced by a piperazine in which a para-X-phenyl, where X = H, F, Cl,

169 are synthesized from the readily accessible piperazines in 50-64% yield by cyclization using ethylen

170 1)H and (13)C NMR spectra of piperidines and piperazines in the presence of (-)-(18-crown-6)-2,3,11,1

171 ide dihydrochloride and 1-(1-naphthylmethyl)-piperazine indicated the involvement of efflux pumps in

172 omal peptide synthetase de-rived di-tyrosine piperazine intermediate.

173 measured by AUC) when the 4-position of the piperazine is substituted with an electron-poor benzoyl

174 enantioselective synthesis of 3-substituted piperazines is also demonstrated.

175 e cis- and trans-2-phenyl-3-(trifluoromethyl)piperazines is described.

176 ee differentially protected 2-(hydroxymethyl)piperazines is presented, starting from optically active

177 n this study, we report the syntheses of two piperazine JDTic-like analogues.

178 -[(5-chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ 7777120), we evaluated in this study the

179 -[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ7777120) has been described as a selectiv

180 oids, synthetic cathinones, phenethylamines, piperazines, ketamine and phencyclidine-type substances,

181 luoromethylated and stereochemically defined piperazines, key scaffold components in medicinal chemis

182 -isoquinolinesulfonyl)-N-methyl-l-tyrosyl]-4-piperazine (KN-62) and oxidized ATP also suppressed the

183 ation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic

184 of a series of N-arylsulfonyl-N'-2-pyridinyl-piperazines led to the identification of a novel bis-pyr

185 u/delta combination agonists compared to the piperazine ligands such as 1.

186 of the project focused on the preparation of piperazine-linked analogues (series 1 (7-16)).

187 This system consists of a piperazine-linked naphthalimide as a fluorescence off-on

188 ved only through further modification of the piperazine linker.

189 The dialkylated piperazine-linker segment contributes to an excellent so

190 erazine (TFMPP) (10 nmol), 1-(3-chlorophenyl)piperazine (m-CPP) (7.4 nmol), gepirone (70 nmol) and 2-

191 selective 5-HT(2C) agonist 1-(m-chlorophenyl)piperazine (m-CPP) were examined.

192 Z readily decomposes at 150 degrees C in 5 M piperazine, making thermal decomposition an important me

193 fluramine, d-fenfluramine, 1-(m-chlorophenyl)piperazine (mCPP) and 1-(m-trifluoromethylphenyl)piperai

194 compounds, indicating a contribution of the piperazine moiety in the observed enhanced affinity.

195 Replacing the piperazine moiety of 2 and 3 with (1S, 4S)-2,5-diazabicy

196 5 and GBR 12909, respectively), in which the piperazine moiety was replaced by bridged piperazines fo

197 starting point and focused on replacing the piperazine moiety.

198 raction between triphosphate unit of ATP and piperazine N atoms of probe 1 is attributed to synergist

199 the dirhodium core through the imidazole or piperazine N-atom and emit only weakly when excited at 3

200 labeling was performed in N-(2-hydroxyethyl)piperazine-N'-(2-ethanesulfonic acid) buffer with microw

201 sulfonic acid (HEPPS), and N-(2-hydroxyethyl)piperazine-N'-(2-hydroxypropanesulfonic acid) (HEPPSO).

202 of this enzyme, as well as N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid (HEPES) and benzoate

203 ium oxide (D(2)O) in 0.1 M N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid (HEPES) buffer in th

204 An N-(2-hydroxethyl)piperazine-N'-2-ethanesulfonic acid (HEPES) molecule is

205 panesulfonic acid), Hepes (N-[2-hydroxyethyl]piperazine-N'-[2-ethanesulfonic acid]), Bes (N,N-bis[2-h

206 d ligand resembling Hepes (N-[2-hydroxyethyl]piperazine-N'-[2-ethanesulfonic acid]).

207 5 +/- 0.03 and log Ka2m = 9.37 +/- 0.02; and piperazine-N,N'-bis(2-ethanesulfonic acid) (Pipes) for w

208 induced tubulin association in 10 and 100 mM piperazine-N,N'-bis(2-ethanesulfonic acid) (Pipes), 1 mM

209 ion of their characteristics in vitro: 20 mM piperazine-N,N'-bis(2-ethanesulfonic acid) (PIPES), 100

210 -[2'-[N-(2'-pyridinyl)-p-iodobenzamidoethyl] piperazine neither elicited degradation of Ikappa-B alph

211 It was found that substitution on the piperazine nitrogen caused an initial decrease in affini

212 e N-phenylpropyl group was the only terminal piperazine nitrogen substituent that retained moderate a

213 diphenylamino analogue in which the terminal piperazine nitrogen was unsubstituted, as in rimcazole,

214 luorophenyl)hexyl)-4-(3,4,5-trimethoxybenzyl)piperazine (NP078585) reduced ethanol intoxication.

215 Extensive modification of the piperazine nucleus led to the synthesis of a new series

216 The two nitrogen atoms on the piperazine nucleus showed different SAR in the interacti

217 ubstitution on the piperazine ring where the piperazine of LDK1203 and LDK1222 are substituted by an

218 Substitution of a piperidine for the piperazine of sabiporide followed by replacement of the

219 hile compounds 40, 41, 48, and 49, with C-28 piperazine or piperidine amide substitutions, increased

220 iphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed.

221 Initial pharmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predict

222 N-methyl piperazine-Phe-homoPhe-vinyl sulfone phenyl also rescued

223 th antitubercular activity derived from homo-piperazine, phenyl- and benzyl-substituted piperazines,

224 Coated and uncoated fully aromatic (FA) and piperazine (PIP) semi-aromatic PA membranes were treated

225 mine (MEA), methyldiethanolamine (MDEA), and piperazine (PIP) underwent oxidative and CO2-mediated de

226 mine (MEA), methyldiethanolamine (MDEA), and piperazine (PIP).

227 ctionalities (e.g., carboxamide, alkylamine, piperazine, piperidine, but not sulfonamide) were well t

228 ure, sodium laureth sulfate (SLA) and phenyl piperazine (PP).

229 d dendrons containing ethylenediamine (EDA), piperazine (PPZ), and methyl 2,2-bis(aminomethyl)propion

230 HT2C agonists (e.g., 3-trifluoromethylphenyl-piperazine) preferentially activated the PLC-IP pathway,

231 Reaction of 6 with piperazine proceeded irreversibly to provide an isomeric

232 reversibly to provide an isomeric mixture of piperazine products, with the syn:anti product ratio inc

233 Piperazine (PZ) is an efficient amine for carbon capture

234 Blends of tertiary amines with piperazine (PZ) showed n-nitrosopiperazine (MNPZ) yields

235 of magnitude higher for the secondary amine piperazine (PZ) than for the primary amines 2-amino-2-me

236 1-N-[2,5-(S, R)-Dimethyl-4-N-(4-cyanobenzoyl)piperazine]-(R)-3,3, 3-trifluoro-2-hydroxy-2-methylpropa

237 ned and synthesized among a small library of piperazine replacements.

238 Piperazine residues at position 4 bearing large phenylal

239 The introduction of these chiral tertiary piperazines resulted in imatinib analogues which exhibit

240 izing the terminal nitrogen with substituted piperazines, resulting in several novel leads such as 11

241 roup adjacent to either nitrogen atom of the piperazine ring (e.g. 25 and 27) was not well tolerated.

242 f the benzene ring after the cleavage of the piperazine ring (e.g., CIP product with m/z 280) is desc

243 Modifications to the piperidine/piperazine ring ablated inhibitory activity, suggesting

244 omatic hydrophobic moieties connected to the piperazine ring and bioisosteric replacement of the arom

245 he scaffold, we have maintained the original piperazine ring and introduced four different functional

246 (SAR) of the aromatic ring linked to the N-4-piperazine ring confirmed the superiority of 2-pyridine

247 e linker between the oxime group and the N-1-piperazine ring displayed the best profile.

248 DNA binding drug Hoechst 33258, in which the piperazine ring has been replaced by an amidinium group

249 example, analogues prepared by replacing the piperazine ring in the GBR structure with an N, N'-dimet

250 alkyl chain between the phenyl group and the piperazine ring influenced binding affinity and selectiv

251 s via direct functionalization of the intact piperazine ring is described.

252 sulfonamide group at the 1N-position of the piperazine ring to fill the S1' pocket of the enzyme, an

253 e) is attached to the distal nitrogen of the piperazine ring via alkyl chains of varying lengths or d

254 CIP oxidation proceeds through an opening of piperazine ring via N-dealkylation.

255 on spacer between the hydroxyl group and the piperazine ring was essential for enantioselectivity, an

256 n of compounds involving changes in the core piperazine ring was synthesized to improve antimalarial

257 ), which differed by the substitution on the piperazine ring where the piperazine of LDK1203 and LDK1

258 e incorporated at the central bridge region (piperazine ring) of GBR 12935.

259 in this series included an aryl-substituted piperazine ring, a varying alkyl chain linker (C3-C5), a

260 ridine ring and the terminal nitrogen of the piperazine ring, leading to compound (4S)-4-[({4-[4-(met

261 to form a five-ring compound with a central piperazine ring, which was characterized by electrospray

262 ing-containing buffers (e.g., Mops, Mes) and piperazine ring-containing zwitterionic buffers (e.g., P

263 nzyl moiety, respectively, on the piperidine/piperazine ring.

264 in which each of the linking arms contains a piperazine ring.

265 Evidence suggests that the piperazine rings of the H1 side-by-side complex are capa

266 -[2'-[N-(2'-pyridinyl)-p-iodobenzamidoethyl] piperazine, (-)-(S)-pindolol, and spiperone also stimula

267 ave made more subtle changes to the original piperazine scaffold (5 and 11).

268 rs of the GK-GKRP complex, where the central piperazine scaffold has been replaced by an aromatic gro

269 e receptor as SR141716A does, the benzhydryl piperazine scaffold is structurally distinct from the fi

270 tors based on the 2-((pyridin-3-yloxy)methyl)piperazine scaffold.

271 ical arylalkylamine or keto/amido-alkyl aryl piperazine scaffolds, prototype compound 10a was identif

272 Many compounds within this piperazine series of [1,2,4]triazolo[1,5-a]triazine have

273 In the N-(3-phenylpropyl)piperazine series, compounds with the ethylenediamine mo

274 ed di-cyclohexadienone, N-methylation of the piperazine serves as a trigger that leads to a cascade o

275 Para-substituted benzyl piperazines showed the most antituberculosis activity.

276 ctionalized with positively charged N-methyl-piperazine side-chains.

277 The use of the piperazine substituent allowed for excellent drug levels

278 the identification of a novel bis-pyridinyl piperazine sulfonamide (51) that was a potent disruptor

279 vity relationship, and in vivo evaluation of piperazine sulfonamides as 11beta-HSD1 inhibitors.

280 g-beta-naphthylamide and 1-(1-naphtylmethyl)-piperazine] tended to move out of the pocket at least pa

281 eptor agonists, 1-[3-(trifluoromethyl)phenyl]piperazine (TFMPP) (10 nmol), 1-(3-chlorophenyl)piperazi

282 5-HT1B/2C agonist 1-(3-trifluoromethylphenyl)piperazine (TFMPP; 0.5-2 mg/kg).

283 ion of a ring-fragmentation of the lithiated piperazines (that could be minimized with sterically hin

284 of spiroadducts and unusual polycyclic fused piperazines through a stepwise [3 + 3] cycloaddition pat

285 cular, its shallow voltage dependence, allow piperazine to be effective even in the presence of high-

286 5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl) piperazine to explore the SAR of this series of FPT inhi

287 e to complexation with nitrogen atoms of the piperazine unit and Hg(2+) in 1:2 stoichiometry, in whic

288 re linked to the free secondary amine of the piperazine unit by: (a) no linker (e.g., a glycosylamine

289 The piperidine/piperazine urea may thus represent a privileged chemical

290 A series of imidazo[1,5-a]quinoxaline piperazine ureas appended with a tert-butyl ester side c

291 Herein we describe piperidine/piperazine ureas represented by N-phenyl-4-(quinolin-3-y

292 f an alpha-methylbenzyl-functionalized N-Boc piperazine using s-BuLi/(-)-sparteine or (+)-sparteine s

293 e synthesis of enantiopure alpha-substituted piperazines via direct functionalization of the intact p

294 elective alpha- and beta- arylation of N-Boc piperazines via lithiation/Negishi coupling is reported.

295 A series of novel biphenyl piperazines was discovered as highly potent muscarinic a

296 thyl]-4-(3-(11)C-methoxymethylpyrid in-2-yl)-piperazine) was synthesized by (11)C-methylation of O-de

297 at N-substituted 3-methyl-4-(3-hydroxyphenyl)piperazines were a new class of opioid receptor antagoni

298 Pyrrolidine bis-piperazines were irreversible, time-dependent inhibitors

299 AGRP/MC4 binding based on (piperazinylethyl)piperazines were prepared, and their structure-activity

300 reduction affords the corresponding tertiary piperazines, which can be employed for the synthesis of

301 explored to prepare hydroxyethyl substituted piperazines with different substituents at the N-atoms.