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 thylketones yields alpha-CF3 morpholines and piperazines.

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

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

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

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

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

13 e concept through a direct synthesis of aryl 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 talyst-free synthesis of N-pyrrolyl(furanyl)-piperazines, 1,4-diazepanes, and 1,4-diazocanes through

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

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

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

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

25 (4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide (BCTC) and clotrimazole or by e

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

27 chlorophenyl)acetyl)-3-((diethylamino)methyl)piperazine-1-carboxylate ((11)C-EKAP) and its comparison

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

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

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

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

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

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

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

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

36 -4-[(2R )-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazin

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

38 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (1a) and 1-[2-[bis(4-fluorophenyl)methoxy]eth

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

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

41 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) (GBR 12909 and GBR 12935, respectively) w

42 [2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) and 1- inverted question mark2-[bis(4-flu

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

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

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

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

47 1-(7-(2-carboxyethyl)phenanthrene-2-carbonyl)piperazine-2,3-dicarboxylic acid) inhibits GluN2C/2D wit

48 1-(7-(2-carboxyvinyl)phenanthrene-2-carbonyl)piperazine-2,3-dicarboxylic acid) which shows over 50-fo

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 vity, into either cis or trans 5-substituted piperazine-2-acetic acid esters that could be chromatogr

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

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

54 l)sulfinyl)alkyl alicyclic amines, where the piperazine-2-propanol scaffold was modified, were design

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

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

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

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

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

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

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

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

74 pellanes (n = 2-4 ), advanced morpholine and piperazine analogues, is developed.

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

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

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

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

85 tyl)azetidine-based isosteres of piperidine, piperazine, and morpholine were designed and synthesized

86 engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, pr

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

88 bes the identification of 1-(2-hydroxyethyl)-piperazine as a new, cost-effective, highly efficient or

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

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

91 set of 24 protected chiral 2,5-disubstituted piperazines, as single stereoisomers in multigram quanti

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 A piperazine-based compound, MMV665917, has in vitro and i

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

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

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

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

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

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

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

106 anthracene and benzhydryl moieties through a piperazine bridge.

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 These diverse and versatile piperazines can be functionalized on either nitrogen ato

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

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

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

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

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

115 trogen atoms, rationalizing the expansion of piperazine chemical diversity through carbon substitutio

116 cent discovery of an LpxH-targeting sulfonyl piperazine compound (referred to as AZ1) by AstraZeneca.

117 Remarkably, none of the sulfonyl piperazine compounds occupies the active site of LpxH, f

118 ted production of more complex C-substituted piperazine compounds.

119 Compared to piperazine congener 31, which retains a high-affinity or

120 oxazoline reduction that sets the stage for piperazine construction.

121 benzene isomers ( o-, m-, and p-fluorophenyl piperazine) containing the diamine ring structure and a

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

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

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

125 ceptors (GPCRs), common off-target sites for piperazine-containing D(3)R scaffolds.

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

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

128 The piperazine derivative 54 displayed especially promising

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

130 Piperazine-derivative MMV665917 may potentially be used

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

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

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

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

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

136 A series of bicyclic piperazine derivatives of triazolotriazine and triazolop

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

138 s now been improved by incorporating various piperazine derivatives.

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

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

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

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

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

144 -(3,4-dimethoxyphenthyl)]-4-(3-phenylpropyl)-piperazine dihydrochloride) in tumor and brain and to ev

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

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

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

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

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

150 presence of ND(3) while only one NPS (benzyl piperazine) exchanged with D(2)O.

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

152 Piperazine exhibits high selectivity 1:400 horse radish

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

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

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

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

157 2-(diphenylmethoxy)-ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935).

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

159 arp kink, and its N-CF(3)-phenyl substituted piperazine group reaching out to the far side of the Lpx

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

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

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

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

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

165 1-[3-(Trifluoromethyl)phenyl]-piperazine HCl (TFMPP), a 5-HT1B receptor agonist, reduc

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

167 The piperazine heterocycle is housed within a large number o

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

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

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

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

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

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

174 e to highly substituted and functionalizable piperazines in high yields with excellent stereoselectiv

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

176 etic cannabinoids, synthetic cathinones, and piperazines in the U.S. communities.

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

178 ynthetic cannabinoids, synthetic cathinones, piperazines, indole, and amphetamine) in wastewater was

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

180 nhibitors verapamil and 1-(1-naphthylmethyl)-piperazine is consistent with a role for efflux pumps in

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

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

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

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

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

186 -[(5-chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ 7777120), we evaluated in this study the

187 -[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ7777120) has been described as a selectiv

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

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

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

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

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

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

194 on guided by X-ray studies, a novel class of piperazine-like NBTIs with outstanding enzymatic activit

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

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

197 ved only through further modification of the piperazine linker.

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

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

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

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

202 linopropiophenone (MMMP), 1-(3-chlorophenyl) piperazine (mCPP), and 5-(2-Aminopropyl) Indole (5IT) we

203 ichment of glycopeptides and glycans using a piperazine modified polymeric monolithic tip.

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

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

206 5 and GBR 12909, respectively), in which the piperazine moiety was replaced by bridged piperazines fo

207 starting point and focused on replacing the piperazine moiety.

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

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

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

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

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

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

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

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

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

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

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

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

220 The cyclic peptides have a combination of piperazine or hydrazine linker with or without a xylene

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

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

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

224 Additionally, the piperazine oxidation state is accessible via an iron-cat

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

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

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

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

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

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

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

232 We have chosen one of these compounds [piperazine (PPZ)] for further testing.

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

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

235 propargyl carbonates gives rise to the final piperazine products.

236 rby charged site; the diamine ring of benzyl piperazine provided this charge site at a fixed length.

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

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

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

240 1-N-[2,5-(S, R)-Dimethyl-4-N-(4-cyanobenzoyl)piperazine]-(R)-3,3, 3-trifluoro-2-hydroxy-2-methylpropa

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

242 Piperazine residues at position 4 bearing large phenylal

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

259 6 (generated from the destruction of the CFC piperazine ring) maintained 41%, 44%, and 30% of the ant

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

283 Piperazine tips also enrich glycans from ovalbumin and h

284 Thus, piperazine tips can be used as an enrichment tool for sw

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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