ライフサイエンスコーパス: 3H

1 3H(2)O] at a rate that increased linearly with pCO(2).

2 3H-Diazirines were thermolyzed or photolyzed to generate

3 [3H]-Riboflavin uptake is saturable with K(m) and V(max)

4 [3H]PiB autoradiography and immunocytochemistry for beta-

5 aminopyrazoles 1 and 3-(3-oxo-2-benzofuran-1(3H)-ylidene)pentane-2,4-dione (2).

6 -[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and

7 approach to 5- or 4-substituted benzoxepin-1(3H)-ones by combining the hydroarylative/hydrovinylative

8 lbenzoic acids 1 or 3-hydroxyisobenzofuran-1(3H)-ones 2 with hydrazine to generate phthalazin-1(2H)-o

9 ',4',5',6'-tetrahydroxyspiro[isobenzofuran-1(3H),9'-(9H)xanthen]-3-one), and M119 (cyclohexanecarboxy

10 While the formation of an isobenzofuran-1(3H)-imine with two bulky substituents under Larock condi

11 talysis for the synthesis of isobenzofuran-1(3H)-ones is presented.

12 sented, for the synthesis of isobenzofuran-1(3H)-ones.

13 3-[(alkoxycarbonyl)methylene]isobenzofuran-1(3H)imines were selectively obtained when the oxidative c

14 one-flask procedure to give benzo[c]oxepin-1(3H)-ones directly from the starting alkyne has been also

15 e S to N alkyl migration of substituted S-(1(3H)-isobenzofuranon-3-yl)isothiuronium bromide to N,N'-d

16 ap-101), 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl}pyrrolidine-2-ca rboxamide

17 thro-pentofuranosyl)pyrimido-[1,2-a]purin-10(3H)-one (M(1)dG) is the major adduct derived from the re

18 o-pentofuranosyl)pyrimido[1,2-alpha]purin-10(3H)-one (M1dG).

19 tetrahydro-8-hydroxypyrimido[1, 2a] purin-10(3H)-ones, commonly referred to as the gamma-OH-PdG adduc

20 spiro[3H-indole-3,2'(1H)quinazoline]-2,4'(1H,3H)dione 8, which was also identified as an intermediate

21 y intermediate 5-amino-6-ribitylamino-2,4(1H,3H) pyrimidinedione 5'-phosphate (ARPP) has not been cha

22 5-Nitro-6-(2-hydroxystyryl)pyrimidine-2,4(1H,3H)-dione (9) was identified as a novel inhibitor of Sch

23 ethyl-1-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione displayed equal potency in the new assays, in

24 -(ethoxymethyl)-5-isopropylpyrimidine-2,4(1H,3H)-dione) were synthesized by reaction of 6-[(3,5-dimet

25 from 7-aminopyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione, a Janus-type nucleobase, has been synthesized

26 alogue, containing 5-aminoquinazoline-2,4(1H,3H)-dione, acts as a Forster resonance energy transfer a

27 Specifically, a 5-methoxyquinazoline-2,4(1H,3H)-dione-based emissive uracil analogue was identified

28 th types, uses 5-amino-6-ribitylamino-2,4(1H,3H)-pyrimidinedione and tyrosine as substrates but not 4

29 reaction of 5-amino-6-D-ribitylamino-2,4(1H,3H)-pyrimidinedione(1) with (S)-3,4-dihydroxybutanone 4-

30 phenethyl)-3-cyclopentylpyrimidine-2,4,6-(1H,3H,5H)-trione (8), a potent and highly selective Ca(V)1.

31 e following main TPs: 1-(2-benzoic acid)-(1H,3H)-quinazoline-2,4-dione (BaQD), 1-(2-benzoic acid)-(1H

32 ine-2,4-dione (BaQD), 1-(2-benzoic acid)-(1H,3H)-quinazoline-2-one (BaQM), 9-aldehyde-acridine, 9-car

33 ith Pb(OAc)4 or hydrogen abstraction from 1H-3H by the tert-butoxyl radical and characterized by UV-v

34 Chiral N-hydroxybenzamides (1H-3H) have been synthesized as precursors of chiral short-

35 ecies have been generated by oxidation of 1H-3H with Pb(OAc)4 or hydrogen abstraction from 1H-3H by t

36 lusively to a single tautomeric form, the 1H-3H or the 2H-3H, respectively.

37 methyl-3-(pyridin-2(1H)-ylidene)benzofuran-2(3H)-one.

38 -(1-methylpyridin-2(1H)-ylidene)benzofuran-2(3H)-one.

39 s of 3-(pyrimidin-2(1H)-ylidene)benzofuran-2(3H)-ones and 6-methyl-3-(pyridin-2(1H)-ylidene)benzofura

40 lorophenyl)-1,5-dihydro-4,1-benzothiazepin-2(3H)-one [CGP-37157 (CGP)], a benzothiazepine derivative

41 lidin-1-ylmethyl)-1H-benzo[e][1,4]diazepin-2(3H)-one), provided with an high lipophilicity index and

42 Glycine-derived 1H-benzo[e][1,4]diazepin-2(3H)-ones (BZDs) 5d-g featuring C9- and N1- substitution

43 mino-acid derived 1H-benzo[e][1,4]diazepin-2(3H)-ones (BZDs) undergo highly retentive deprotonation/a

44 oxaldehyde, 1-hydroxy-2-propanone, dihydro-2(3H)-furanone, 5-methyl-(E)-2-hepten-4-one, acetic acid,

45 -N-(3-(2-methoxyethyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetra methyl-cyclopropanecarboxamid

46 )-N-(3-(4-fluorobutyl)-4,5-dimethylthiazol-2(3H)-ylidene)-2,2,3,3-tetramethyl-c yclopropanecarboxamid

47 ve, spiro[imidazo[1,2-a]pyridine-3,2-idan]-2(3H)-one (ST101 or ZSET1446).

48 1,4'-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-1 (TBPB) displays unprecedented functional selectivi

49 lohexylpiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-1 (VCP794), lost agonistic selectivity for the M(1)

50 )piperidin-1-yl)butyl)-1H-benzo[d]imidazol-2(3H)-one (79) and 1-(6-(4-(4-fluorobenzoyl)piperidin-1-yl

51 )piperidin-1-yl)hexyl)-1H-benzo[d]imidazol-2(3H)-one (81) were identified as full antagonist ligands

52 nalogues 1'-beta-[1-naphtho[2,3-d]imidazol-2(3H)-one)]-2'-deoxy-d-ribofuranose and 1'-beta-[1-naphtho

53 amine-bearing N-alkylated benzo[d]imidazol-2(3H)-ones, imidazo[4,5-b]pyridin-2(3H)-ones, imidazo[4,5-

54 ones and N,N'-dialkylated benzo[d]imidazol-2(3H)-ones.

55 , 2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid (GRI977143), 4,5-dichlor

56 um thermolysis (FVT) of 3-methylidenefuran-2(3H)-ones 3 causes cheletropic extrusion of CO with forma

57 1b), and 3-methyl-5-phenyl-1,3,4-oxadiazol-2(3H)-one (3b) affords the nitrile imine (2b), which rearr

58 tylphenyl)ethyl)-5-methoxy-1,3,4-oxadiazol-2(3H)-one (JZP-327A, 51), inhibited human recombinant FAAH

59 f) led to the formation of 1,3,4-oxadiazol-2(3H)-ones (4a-f, 5a) and dibenzo[c,e]azepines (6a-f) when

60 riety of 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-ones in good to excellent yields.

61 o[4,5-c]pyridin-2(3H)-ones, benzo[d]oxazol-2(3H)-ones, oxazolo[4,5-b]pyridin-2(3H)-ones and N,N'-dial

62 methyl)-tetrahydrofuran-2-yl)-1H-perimidin-2(3H )-one] (dPer) recognizes in DNA the O(6)-benzyl-2'-de

63 erved via which a 1H-pyrrolo[3,2-b]pyridin-2(3H)-one derivative was furnished.

64 al derivatives of 1H-pyrrolo[2,3-b]pyridin-2(3H)-one have been obtained.

65 d]oxazol-2(3H)-ones, oxazolo[4,5-b]pyridin-2(3H)-ones and N,N'-dialkylated benzo[d]imidazol-2(3H)-one

66 to 3-benzylidene-1H-pyrrolo[2,3-b]pyridin-2(3H)-ones, as these substrates are exocyclic methylene la

67 ]pyridin-2(3H)-ones, imidazo[4,5-c]pyridin-2(3H)-ones, benzo[d]oxazol-2(3H)-ones, oxazolo[4,5-b]pyrid

68 imidazol-2(3H)-ones, imidazo[4,5-b]pyridin-2(3H)-ones, imidazo[4,5-c]pyridin-2(3H)-ones, benzo[d]oxaz

69 l)-3-(2-(azepan-1-yl)ethyl)benzo[d]thiazol-2(3H)-one ((18)F-FTC-146).

70 l)-3-(2-(azepan-1-yl)ethyl)benzo[d]thiazol-2(3H)-one ([(18)F]FTC-146, [(18)F]13).

71 z)(4)}(CN)(3)](2)[Co(bik)(2)](2)}(ClO(4))(2).3H(2)O [B(pz)(4) = tetrapyrazolylborate, bik = bis(1-met

72 te), which is isostructural to Cu(3)(BTC)(2).3H(2)O.

73 This led to the discovery of 2-(3H-imidazo[4,5-b]pyridin-2-ylthio)-N-(3,4-dimethoxypheny

74 yl-8,9-disubstituted-6,9-dihydro-1H-purin-2-(3H)-ones 25-26 were synthesized in one step using formic

75 d that the reaction proceeds through a 2e(-)/3H(+)-bearing intermediate.

76 asibility of bypassing the high energy 2e(-)/3H(+)-intermediate through disproportionation of earlier

77 2H,3H,6aH-pyrrolidino[2'',1''-3',2']1,3-oxazino[6',5'-5,4]-

78 esented by cyclothiazide and the ampakine 2H,3H,6aH-pyrrolidino(2,1-3',2')1,3-oxazino(6',5'-5,4)benzo

79 single tautomeric form, the 1H-3H or the 2H-3H, respectively.

80 For [2H](+), [3H](+), and [4H](+), the acid-independent rate constants

81 here PR(3) = P(OPh)(3) ([2H]BF(4)); PPh(3) ([3H]BF(4)); PPh(2)Py ([4H]BF(4), where Py = 2-pyridyl).

82 magnesium carbonate, nesquehonite (MgCO(3) . 3H(2)O), and magnesite (MgCO(3)) after 72 h.

83 [3-3H]glucose was used to estimate rates of glucose appeara

84 ed are those reported in Figures 3C, 3D, 3G, 3H, 5A and 5B, and in Supplemental Figures 3A and B.

85 d 3-(1-methylethenyl)-1H-2,3-benzoxazine-1,4(3H)-diones (16a-e).

86 give N-unsubstituted 1H-2,3-benzoxazine-1,4(3H)-diones (17a-e) at rates that were dependent on tempe

87 des and 3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-dione derivatives as potential antiosteoclastogenic

88 des and 3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-diones could be potential lead compounds for the dev

89 covery of a novel antibacterial (2) with a 4(3H)-quinazolinone core.

90 Most of the 2-aminoquinazolin-4(3H)-one based inhibitors show a similar activity against

91 d efficient synthesis of 2-aminoquinazolin-4(3H)-ones and N1-substituted 2-aminoquinazolin-4(1H)-ones

92 r, these results suggest 2-aminoquinazolin-4(3H)-ones as perspective leads for future development of

93 he structure showed that 2-aminoquinazolin-4(3H)-ones bind to the open flap conformation of the enzym

94 2-Aminoquinazolin-4(3H)-ones were identified as a novel class of malaria dig

95 pharmaceutically relevant 3-arylquinazolin-4(3H)-ones (quinazolinones) with high levels of enantioind

96 inazolin-2-yl)amino)-5,6-dimethylpyrimidin-4(3H)-one RNAsplicing inhibitor), was studied in more deta

97 3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease

98 esence of HCl to produce 2-chloro-3-phenyl-4(3H)-quinazoliniminium chloride (Qz) involves the formati

99 ersion reactions were studied of pyrimidin-4(3H)-imine (PMI), pyridin-2(1H)-imine (PYI), and 1H-purin

100 Pyrido[4,3-d]pyrimidin-4(3H)-one (1) was prepared by reacting 2-trifluoromethyl-4

101 yl-2-(4-nitrophenyl)thieno[2,3-d]pyrimidin-4(3H)-one (DNTP) occupies the interface between the p66 ri

102 gue (5-hydroxy-2-(4-fluorophenyl)pyrimidin-4(3H)-one) did exhibit significant activity as an endonucl

103 amino-6-ethyl-5-iodothieno[2,3-d]pyrimidin-4(3H)-one, 7, to which various arylthiols were attached at

104 bitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one.

105 oro-6-fluorobenzyl)-2-(alkylthio)pyrimidin-4(3H)-ones (2-Cl-6-F-S-DABOs) 7-12 and the related 6-(2,6-

106 ated tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-ones with mesyl, tosyl, and p-cyanobenzenesulfonyl c

107 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysin

108 carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one (compound 2) as an antibiotic effective in vivo

109 yl)pyridin-3-yl)meth yl)benzo[h]quinazolin-4(3H)-one (referred to herein as benzoquinazolinone 12) as

110 no-9H-purin-9-yl pendant to the quinazolin-4(3H)-one nucleus of both aS and aR isomers of 1 had a cri

111 around the bond connecting the quinazolin-4(3H)-one nucleus to the o-tolyl is sterically hampered, w

112 -yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one)] is a potent PI3K inhibitor selective for the d

113 erts benzyl alcohol to 2-phenyl-quinazolin-4(3H)-one.

114 brary of 26 synthetic, sulfated quinazolin-4(3H)-ones (QAOs) resulting in the identification of six m

115 easy access to 2-(alpha-styryl)quinazolin-4(3H)-ones and 3-(alpha-styryl)-1,2,4-benzothiadiazine-1,1

116 The sulfonylation of quinazolin-4(3H)-ones and related tetrahydrobenzothieno[2,3-d]pyrimid

117 amdidines afforded substituted quinazolin-4(3H)-ones in 44-89% yields.

118 he one-pot cascade synthesis of quinazolin-4(3H)-ones via acceptorless dehydrogenative coupling of o-

119 A wide variety of substituted quinazolin-4(3H)-ones were synthesized in high yields starting from r

120 roviding an expedient access to quinazolin-4(3H)-ones, N-aryl-2-arylbenzimidazoles, and 4H-3,1-benzox

121 applicable for the syntheses of quinazolin-4(3H)-ones.

122 order to selectively get 2-aryl quinazolin-4(3H)-ones.

123 methyl ketones produced 2-aryl quinazolin-4(3H)-ones.

124 ontain the (E)-3-phenyl-2-styrylquinazolin-4(3H)-one backbone.

125 action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypno

126 of 6-phenyl-3-(pyridin-2-yl)-1,2,4-triazin-4(3H)-ol (4-OH), which rapidly isomerizes to a 3,4-dihydro

127 tion and yielded 3-arylbenzo-1,2,3-triazin-4(3H)-ones in good to moderate yields in the presence of o

128 ive formation of 3-arylbenzo-1,2,3-triazin-4(3H)-ones in the presence of CO and1-aryl-(1H)-benzo-1,2,

129 he corresponding 3-arylbenzo-1,2,3-triazin-4(3H)-ones with high selectivity and in excellent yields.

130 Complexes [2H]BF(4), [3H]BF(4), and [4H]BF(4) undergo reductions near -1.46 V

131 ,-trimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4-(3H,5H)-d ione (17f), which acts as a dual human A(2a) an

132 ,7-trimethyl-3a,4-dihydro-2,1-benzisoxazol-5(3H)-ylidene)ethanal (10), the trans isomers recombined f

133 access to new oxazolo[3,2-d][1,4]oxazepin-5(3H)-ones starting from alpha-bromoamido alcohols and Mic

134 nits in the linear nucleocapsid, and a (5H + 3H) motif that forms a proper cavity for sequestration o

135 ert-butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione].

136 (3-methyl-2-bute n-1-yl)-2H-1-benzopyran-4,7(3H,8H)-dione; 3-[(2-O-beta-d-glucopyranosyl-beta-d-gluco

137 raightforward synthesis of various 2-alkynyl-3H-imidazo[4,5-b]pyridines, a valuable scaffold in drug

138 tuted 2,3-dihydro-1H-2-benzazepin-1-ones and 3H-2-benzoxepin-1-ones by an I-MCR/Wittig sequence was d

139 rd well-characterized hydrides ([2H](+) and [3H](+)) and mixed-valence derivatives ([2](+) and [3](+)

140 For [2H](+) and [3H](+), the overpotentials for H(2) evolution are estima

141 the known distribution of [3H]8-OH-DPAT and [3H]WAY-100635.

142 (CQ)-dependent yeast growth inhibition and [3H]CQ transport specifically due to a given PfCRT isofor

143 Parallel [3H]-leucine and [3H]-thymidine incubations indicated active protein and D

144 gulation of SREBP1c, ACC, FAS, and SCD1 and [3H]H2O incorporation into lipids), FB treatment markedly

145 ith [3H]GlcNAc, both [3H]GlcNAc-P-P-Und and [3H]GalNAc-P-P-Und were detected.

146 raphic properties of [3H]GlcNAc-P-P-Und and [3H]GalNAc-P-P-Und, suggesting that strain O157 contained

147 olites, the detected transport from applied [3H]IBA may have resulted from the transport of IBA metab

148 Certain 2-aryl-3H-1-benzazepines are conformationally mobile on the NMR

149 has been suggested that stoichiometry may be 3H(+)/2e(-) based on the identification of only 3 proton

150 Because the isotopic discrimination between 3H and H is small, organically bound tritium (OBT) and H

151 esityl (3H(Phl(Mes))), 2,6-bismethoxyphenyl (3H(Phl(OMe))), 4-nitrophenyl (3H(Phl(NO2))), or 4-tert-b

152 metabolically labeled with [3H]GlcNAc, both [3H]GlcNAc-P-P-Und and [3H]GalNAc-P-P-Und were detected.

153 Time-dependent dissociation of bound [3H]vesamicol is biphasic, but equilibrium saturation cur

154 s treated with 2 equiv of KC8 and LiB(sec-Bu)3H to yield a deep blue-colored dicarbene zinc compound

155 3H(Phl(NO2))), or 4-tert-butylcarboxyphenyl (3H(Phl(CO2tBu))) groups at the 15-meso-position.

156 the rate constant for transfer from CpCr(CO)3H to n-butyl vinyl ether and have examined the chemistr

157 e only inhibitor that did not also decrease [3H]2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane (WIN

158 )TiCl(thf)2 ] (2) can access the dianionic [(3H-pyr-ONO)TiCl2 (thf)] (1-THF) and monoanionic [(3H,4H-

159 t both the in situ synthesis of 3,3-difluoro-3H-indol-2-yl (OFox) glycosyl donors and activation ther

160 mediated glycosylations wherein 3,3-difluoro-3H-indol-2-yl (OFox) imidates were found to be key inter

161 pyrrol-6-ones (10), and 1-phenyl-1,2-dihydro-3H-benzo[4,5]thieno[2,3-c]pyrrol-3-ones (12)), and notab

162 dazol-3-yl benzoates and 2-alkyl-1,2-dihydro-3H-indazol-3-ones, which are known privileged structures

163 aryl-2-(trimethylsilylmethylene)-1,2-dihydro-3H-pyrrol-3-ones.

164 The reaction between 2,4-dihydro-3H-pyrazol-3-ones and ortho-halo aryl carboxaldehydes fu

165 und 2) and N-{4-[4-2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)butyl]benzoyl} *-L-glut

166 e carbons (N-{4-[3-2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)propyl]benzoy l}-L-glut

167 Prazosin did not measurably displace [3H]CUMI-101 binding in baboon or human brain sections, t

168 38), a digoxigenin derivative that displaces 3H-ouabain from Na+, K+ -ATPase, and attenuates some for

169 ave been used to construct 2,3-disubstituted-3H-quinazolin-4-ones in a one-pot procedure.

170 anthranilate then affords 2,3-disubstituted-3H-quinazolin-4-ones in good to excellent yields under m

171 um efflux reaction, pointing to electrogenic 3H(+)/propidium(2+) antiport.

172 , N-[1(R)-1, 2-dihydro-1-ethanesulfonylspiro-3H-indole-3,4'-piperidin)-1'-yl]carbonyl-2-(pheny lmetho

173 We examined [3H]PiB binding and Abeta and beta-amyloid precursor prot

174 We found that: (1) CLIC2 facilitated [3H]ryanodine binding to skeletal SR and purified RyR1, b

175 phorylations on eukaryotic initiation factor 3H (eIF3H), a protein integral to overall eukaryotic pro

176 ylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro- 3H-quinazolin-4-one), a noncompetitive antagonist of AMP

177 de binding to generate complexes of the form 3H(Phl(R)).2F(-) modulates the redox potentials of the p

178 s and intestinal permeability to the gliadin 3H-p31-49 peptide were analyzed in polarized monolayers

179 The homoleptic [(3H-pyr-ONO)2 Zr] (4) was synthesized and characterized b

180 9aR)-2-amino-6,7-dihydroxy-8-(hydroxymethyl)-3H,4H,5H,5aH,6H,7H,8H, 9aH,10H-pyrano[3,2-g]pteridin-4-o

181 nyls and 3-alkylidene-2-oxindoles results in 3H-spiro[furan-2,3'-indolin]-2'-ones.

182 The re-expression of AQP3, which increased [3H]glycerol uptake, also induced mRNA and protein expres

183 kade of which was found to partially inhibit 3H-thymidine incorporation as a result of increased cell

184 or SIgA against p31-49, transport of intact 3H-p31-49 increased significantly across Caco-2 monolaye

185 ith 4-MeO-TEMPO-H(D) also has a large KIE, k(3H)/k(3D) = 21 +/- 3 in MeCN.

186 trapping time for the [M + 2H](2+) and [M + 3H](3+) charge states.

187 tified for the [M + 2H](2+) and for the [M + 3H](3+) charge states.

188 such as melittin (2845 Da), CID of the [M + 3H](3+), [M + 4H](4+), and [M + 5H](5+) ions yields amin

189 ions, and compact and elongated forms of [M+3H](3+) ions.

190 cting CCS values remained similar for the [M+3H](3+) ions observed as the glycan antennae were shorte

191 MDR1-WT (expresses wild-type P-gp), LLC-MDR1-3H (expresses common haplotype P-gp), and LLC-MDR1-3HA (

192 , cytotoxicity assays show that the LLC-MDR1-3H cells are more resistant to mitoxantrone than the LLC

193 ary pentafluorophenyl (3H(Phl(F))), mesityl (3H(Phl(Mes))), 2,6-bismethoxyphenyl (3H(Phl(OMe))), 4-ni

194 of 1, adamantane-1-carboxylic acid (3-methyl-3H-benzothiazol-2-ylidine) hydrazide, a potent KCNQ2/Q3

195 [(3)H]2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(phenylethyl)-1H-imidazole-5-ca

196 [[2-(1H-tetrazol-5-yl)biphe nyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine ((11)C-KR31173) was injected i

197 r-ONO)TiCl2 (thf)] (1-THF) and monoanionic [(3H,4H-pyr-ONO)TiCl2 (OEt2 )][B{3,5-(CF3 )2 C6 H3 }4 ] (3

198 of this binding is supported by neocortical [3H]PiB binding in regions of amyloid deposition in the p

199 ienes results from use of Ag(2)O and Bu(4)NF.3H(2)O, respectively, as activators.

200 methoxyphenyl (3H(Phl(OMe))), 4-nitrophenyl (3H(Phl(NO2))), or 4-tert-butylcarboxyphenyl (3H(Phl(CO2t

201 rsor protein by immunocytochemistry, but no [3H]PiB binding.

202 zymatic synthesis of [3H]GlcNAc-P-P-Und nor [3H]GalNAc-P-P-Und was detected.

203 C2 direct alkynylation of 3H-imidazo[4,5-b]pyridine derivatives is explored for th

204 The single-operation deracemization of 3H indolines and tetrahydroquinolines is described.

205 was evaluated by radioligand displacement of 3H-PK 11195 with PBR06 in vitro and by displacement of 1

206 By quantifying the distribution of 3H-sitostanol along the length of the small intestine fo

207 re assessed in vitro by the incorporation of 3H-thymidine and flow cytometry.

208 Valence isomerization of 3H-diazirines also afforded diazo compounds.

209 unprecedented enantioselective synthesis of 3H pyrroles, a simple procedure using PPh3 produced a wi

210 X-ray crystallographic analysis of [3H]BF(4) revealed a highly unsymmetrical bridging hydrid

211 We evaluated specific binding of [3H]CUMI-101 by quantitative autoradiography studies in p

212 , which can be prepared by deprotonation of [3H]BF(4) with NaOMe, is about 10(4) stronger base than i

213 nity (IC50 of 8.9 nmol) for displacement of [3H]ifenprodil, thus showing improved potency with respec

214 sections matched the known distribution of [3H]8-OH-DPAT and [3H]WAY-100635.

215 The regional and laminar distributions of [3H]CUMI-101 binding in baboon and human brain sections m

216 Inhibition of [3H]-taurocholic acid efflux was observed after 30 minute

217 titatively track RCT following injection of [3H]-cholesterol-loaded macrophages upstream of blocked o

218 chemical and chromatographic properties of [3H]GlcNAc-P-P-Und and [3H]GalNAc-P-P-Und, suggesting tha

219 ant role in the intracellular regulation of [3H]-riboflavin.

220 Solutions of [3H]BF(4) undergo substitution by dppe to give [2H](+).

221 ]GalNAc, neither the enzymatic synthesis of [3H]GlcNAc-P-P-Und nor [3H]GalNAc-P-P-Und was detected.

222 Apical and baso-lateral uptake of [3H]-riboflavin clearly indicates that a riboflavin speci

223 The uptake of [3H]-riboflavin is sodium, temperature and energy depende

224 B{C6 H3 (CF3 )2 }4 ] yields [(3H,4H-pyr-ONO)(3H-pyr-ONO)Zr][B{3,5-(CF3 )2 C6 H3 }4 ] (5), thus demons

225 the 2,3-dihydro-1H-2-benzazepin-1-ones 8 or 3H-2-benzoxepin-1-ones 10 in good yields via a sequentia

226 aque-associated amyloid immunoreactivity or [3H]PiB binding was seen in cerebellar gray matter in aut

227 or human brain sections, thereby ruling out [3H]CUMI-101 binding to alpha1-adrenergic receptors.

228 necarboxylic acid [2-(4,5,6-trihydroxy-3-oxo-3H-xanthen-9-yl)-(9CI)]) suppressed citral's inhibition

229 removable protecting group, (6-hydroxy-3-oxo-3H-xanthen-9-yl)methyl (1), with a molar absorption coef

230 )-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta [g]quinazolin-6-yl]amino]benzoyl]-l-gamma-

231 t cytotoxic agent 4-[(7-bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(3-pyrid y

232 Furthermore, ttksr39 in a p21-3H reporter construct provides a potential combination w

233 In vivo tumor xenografts carrying p21-3H also showed increased luciferase activity by luminesc

234 hostatin A or SAHA, H1299 cells carrying p21-3H showed a significant increase of luciferase activity,

235 The therapeutic efficacy on p21-3H-expressing tumor xenografts was assessed by daily adm

236 riven triple-fused reporter gene system (p21-3H) to evaluate the efficacy of HDACI and the ganciclovi

237 The p21-3H construct was generated and stably or transiently tra

238 Furthermore, when cells transfected with p21-3H or p21/PstI-3H (which lacks p53-binding sites) were t

239 Parallel [3H]-leucine and [3H]-thymidine incubations indicated act

240 vatives contain ancillary pentafluorophenyl (3H(Phl(F))), mesityl (3H(Phl(Mes))), 2,6-bismethoxypheny

241 6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl )piperazin-1-yl)methyl)-5-

242 Eight 2-phenyl-3H-imidazo[4,5-b]quinoline-9-carbonitriles 15 are prepar

243 azoles 14 in diphenyl ether affords 2-phenyl-3H-imidazo[4,5-b]quinoline-9-carbonitriles 15 in near qu

244 45 and its cyclization to 3-(phenylethynyl)-3H-indazole 46b.

245 u(MeCN)(+) with 0.5 and 1 equiv of KB(O(i)Pr)3H, respectively.

246 phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one (CAL-101), a highly selective and po

247 constant for the complex between protonated [3H]vesamicol and VAChT decreases from 12 nM at neutral p

248 en cells transfected with p21-3H or p21/PstI-3H (which lacks p53-binding sites) were treated, the inc

249 Autoradiography revealed [3H]PiB binding in neocortical gray matter, in regions wh

250 (H2O)n (n = 0 to approximately 50) and [SP + 3H](3+) (H2O)n (n = 0 to approximately 30), and that maj

251 In the case of [SP + 3H](3+), the results demonstrate that a compact dehydrat

252 and contains a single Substance P (SP) [SP + 3H](3+) ion (SP(3+); amino acid sequence RPKPQQFFGLM-NH2

253 centration-dependent inhibition of specific [3H]DA uptake.

254 ble spiro-oxindole compounds bearing a spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one scaffold that are n

255 merization as observed for the initial spiro[3H-indole-3,3'-pyrrolidin]-2(1H)-one scaffold.

256 amide led to the spirocyclic molecule, spiro[3H-indole-3,2'(1H)quinazoline]-2,4'(1H,3H)dione 8, which

257 In the present study, [3H]ryanodine binding, Ca2+ efflux from skeletal sarcopla

258 the versatile 2-hydroxy-5,6,7,7a-tetrahydro-3H-pyrrolizin-3-one core.

259 preparation of 2-hydroxy-5,6,7,7a-tetrahydro-3H-pyrrolizin-3-ones and 2-hydroxy-6,7,8,8a-tetrahydroin

260 ch as 4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c] quin oline-8-sulfonamide (4BP-TQS) acti

261 ,9bS)-4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8- sulfonamide) have the combi

262 nist, cis-cis-4-p-tolyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4MP-TQS), toget

263 QS (4-(naphthalen-2-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide ) and allosteric

264 QS (4-(4-chloroophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide )] or an iodine

265 TQS (4-(4-fluorophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) ] generated a c

266 -TQS (4-(2-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) and 3BP-TQS (4-

267 -TQS (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) interact at an

268 -TQS (4-(3-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide), rather than at

269 -TQS (4-(4-iodoophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide)] results in com

270 cemic 4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide, is a strong pos

271 substituted benzopyrrolizidines (tetrahydro-3H-pyrrolo[2,1-a]isoindol-3-ones) is reported.

272 ctive small molecule derived from tetrahydro-3H-cyclopenta[c]quinoline.

273 Selected iodo-substituted tetrahydro-3H-cyclopenta[c]quinolines exhibited IC(50) values lower

274 A series of iodo-substituted tetrahydro-3H-cyclopenta[c]quinolines was synthesized as potential

275 umulates to lower intracellular levels than [3H]ER-076349, yet is retained longer and at higher level

276 ake and washout/retention studies show that [3H]eribulin accumulates to lower intracellular levels th

277 DNA methylation was measured using the [3H]-methyl incorporation assay, which provides disintegr

278 ,7r)-3,5-dimethyladamantan-1-yl)-4-(3-thioxo-3H-1,2-dithiol-4-yl)-ben zamide (S-memantine) and examin

279 ing a slow releasing H(2)S donor 4-(3-thioxo-3H-1,2-dithiol-4-yl)-benzoic acid (ACS48) with a NMDAR a

280 liferation was evaluated using 3H-thymidine (3H-TdR) uptake, carboxyfluorescein diacetate, succinimid

281 toichiometry has changed from 4H(+)/2e(-) to 3H(+) or 2H(+)/2e(-) without affecting the direct coupli

282 lyzes the transformation of 2-nitroarenes to 3H-indoles through a tandem cyclization-[1,2] shift reac

283 l-1H-1,2,4-triazol-5-yl)-2,7,8,9-te trahydro-3H-pyrido[4,3,2-de]phthalazin-3-one).

284 amino)ethoxy)ethoxyl]-4-[2-(trifluoromethyl)-3H-dia zirin-3-yl]benzoyl]-1,3-bis(mannopyranosyl-4-ylox

285 omers of ethyl 1-(1-(4-(3-((trifluoromethyl)-3H-diazirin-3-yl)phenyl)ethyl)-1H-imidazole-5-carbo xyla

286 -2-yn-1-yloxy)methyl)-5-(3-(trifluoromethyl)-3H-diazirin-3-yl)phenol, AziPm-click (1)), for affinity-

287 (3)H]TDBzl-etomidate (4-[3-(trifluoromethyl)-3H-diazirin-3-yl]benzyl-[(3)H]1-(1-phenylethyl)-1H-imida

288 propofol (2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol ([(3)H]AziPm)) to identify propo

289 propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm).

290 etomidate (ethyl-1-(1-(4-(3-trifluoromethyl)-3H-diazirin-3-yl)phenylethyl)-1H-imidazole-5-c arboxylat

291 -2-O-[9-[[[2-[(125)I]iodo-4-(trifluoromethyl-3H-diazirin-3-yl)ben zyl]oxy]carbonyl]nonanoyl]-sn-glyce

292 -2-O-[9-[[[2-[(125)I]iodo-4-(trifluoromethyl-3H-diazirin-3-yl)ben zyl]oxy]carbonyl]nonanoyl]-sn-glyce

293 molar potencies, including 6-trifluoromethyl-3H-benzoimidazole-4-carboxylic acid [3-(1H-tetrazol-5-yl

294 rexpressing strain, were incubated with UDP-[3H]GalNAc, neither the enzymatic synthesis of [3H]GlcNAc

295 ns from strain O157 were incubated with UDP-[3H]GlcNAc, two enzymatically labeled products were obser

296 ray crystallographic analysis has an unusual 3H-benzo[d]pyrrolo][1,3]oxazine-3,5-dione core.

297 lymphocyte proliferation was evaluated using 3H-thymidine (3H-TdR) uptake, carboxyfluorescein diaceta

298 strain O157 was metabolically labeled with [3H]GlcNAc, both [3H]GlcNAc-P-P-Und and [3H]GalNAc-P-P-Un

299 y [H(OEt2 )2 ][B{C6 H3 (CF3 )2 }4 ] yields [(3H,4H-pyr-ONO)(3H-pyr-ONO)Zr][B{3,5-(CF3 )2 C6 H3 }4 ] (

300 razin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H -imidazo[4,5-b]pyridine (27e), a potent inhibitor of

301 ro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin -4-one (28), identified following a careful

302 ro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (7) and the optimization of this new