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-Phosphaallenes are accessible on a new and facile rou

4 [3H]-Riboflavin uptake is saturable with K(m) and V(max)

5 [3H]PiB autoradiography and immunocytochemistry for beta-

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

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

10 yphenyl)imino)methyl) phenyl)isobenzofuran-1(3H)-one (HMBP) was designed as a ''turn-on" fluorogenic

11 zo[c] thiophen-1(3H)-ylidene)isobenzofuran-1(3H)-one, and (E)-3H,3'H-[1,1'-bibenzo[c] thiophenylidene

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

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

14 3-[(alkoxycarbonyl)methylene]isobenzofuran-1(3H)imines were selectively obtained when the oxidative c

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

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

17 -3,3'-dione, (E)-3-(3-oxobenzo[c] thiophen-1(3H)-ylidene)isobenzofuran-1(3H)-one, and (E)-3H,3'H-[1,1

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

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

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

21 imidazo[1,2-a]pyridin-3-yl)pyrimidine-2,4(1H,3H)-diones has been accomplished based on a one-pot mult

22 nonbiased GPR84 agonist 6-hexylamino-2,4(1H,3H)-pyrimidinedione (6) in tritium-labeled form ([(3)H]P

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

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

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

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

27 line-2-one (BQM), and 1-(2-benzaldehyde)-(1H,3H)-quinazoline-2,4-dione (BQD) in developing zebrafish

28 arbamazepine, 1-(2-benzaldehyde)-4-hydro-(1H,3H)-quinazoline-2-one (BQM), and 1-(2-benzaldehyde)-(1H,

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

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

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

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

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

34 -(1-methylpyridin-2(1H)-ylidene)benzofuran-2(3H)-one.

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

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

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

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

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

40 1,4'-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-1 (TBPB) displays unprecedented functional selectivi

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

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

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

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

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

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

47 , 2-((3-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl)thio)benzoic acid (GRI977143), 4,5-dichlor

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

49 1b), and 3-methyl-5-phenyl-1,3,4-oxadiazol-2(3H)-one (3b) affords the nitrile imine (2b), which rearr

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

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

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

53 -I(2)-mediated reactions of benzo[d]oxazol-2(3H)-ones with acyclic secondary amines.

54 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

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

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

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

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

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

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

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

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

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

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

65 elta,Lambda-[Cu(bpy)(2)(H(2)O)](2)[MF(6)](2).3H(2)O (M = Ti, Zr, Hf; bpy = 2,2'-bipyridine) family (s

66 synthesis of 3,3-disubstituted benzofuran-2-(3H)-ones through reacting alpha-aryl-alpha-diazoacetates

67 f 1,4,6-trisubstituted 1,6-dihydropyridin-2-(3H)-ones from 3-arylglutaconic acids, primary amines, an

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

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

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

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

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

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

74 [3-3H]glucose was used to estimate rates of glucose appeara

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

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

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

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

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

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

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

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

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

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

85 2-Aminoquinazolin-4(3H)-ones were identified as a novel class of malaria dig

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

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

88 3(2H)-ones and 2-phenyl-5-hydroxypyrimidin-4(3H)-ones were synthesized and evaluated as endonuclease

89 a hit compound, 2-methyl-8-nitroquinazolin-4(3H)-one (2) with moderate potency (MIC = 312/156 muM).

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

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

92 8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one (BPOET) stimulates resuscitation.

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

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

95 6a (2-methyl-7-nitrothieno[3,2-d]pyrimidin-4(3H)-one) with improved potency (MIC = 19/38 muM), select

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

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

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

99 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysin

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

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

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

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

104 -fluorophenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one) for further study.

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

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

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

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

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

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

111 ious substituted quinolines and quinazolin-4(3H)-ones under relatively mild reaction conditions (<=90

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

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

114 y of substituted quinolines and quinazolin-4(3H)-ones were synthesized in moderate to good isolated y

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

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

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

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

119 ein the syntheses of 79 derivatives of the 4(3H)-quinazolinones and their structure-activity relation

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

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

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

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

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

125 The reaction of gold reagents [HAuCl(4)*3H(2)O], [AuCl(tht)], or cyclometalated gold(III) precur

126 ated with solutions of (tht)AuCl or HAuCl(4).3H(2)O, respectively.

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

128 ]triazolo[4,5-b]pyridine-7,3'-indoline]-2',5(3H)-dione analogues were synthesized and evaluated as po

129 ,7-trimethyl-3a,4-dihydro-2,1-benzisoxazol-5(3H)-ylidene)ethanal (10), the trans isomers recombined f

130 of 2-(3-oxo-2H-[1,2,4]triazino[5,6-b]indol-5(3H)-yl)acetic acid derivatives (OTIs), designed by molec

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

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

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

134 dro-7H-1,4-methanobenzo[e][1,4]diazonine-2,7(3H)-diones in 30-81% yield.

135 (3-methyl-2-bute n-1-yl)-2H-1-benzopyran-4,7(3H,8H)-dione; 3-[(2-O-beta-d-glucopyranosyl-beta-d-gluco

136 solve the structures of K(5)[Mo(3)O(4)F(9)].3H(2)O (1), K(5)[Mo(3)O(4)F(9)].2H(2)O (2), and K(16)[Mo

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 c binding of the TSPO ligands 3H-PK11195 and 3H-PBR28 was determined in the same lesions.

140 TSPO targeting radioligands (3H-PK11195 and 3H-PBR28) in tissue sections from 42 multiple sclerosis

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

142 B1-specific signal using [3H] CP-55,940 and [3H] SR141716A, though the latter exhibited a lower signa

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

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

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

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

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 formation to yield spirocyclic- or bicyclic 3H-indoles or benzazepinones.

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

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

154 3H(Phl(NO2))), or 4-tert-butylcarboxyphenyl (3H(Phl(CO2tBu))) groups at the 15-meso-position.

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

156 bial metabolism - sulfur comproportionation (3H(2) S + SO42- + 2H(+) 4S(0) + 4H(2) O).

157 RNA sequencing, flow cytometry, 3H-labeled palmitic acid uptake, lipidomic analysis, con

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 o[2,3-c]pyrrol-6-ones, and (iii) 1,2-dihydro-3H-pyrrolo[1,2-c]imidazole-3-ones.

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

166 sh were developmentally exposed to 4,8-dioxa-3H-perfluorononanoate (ADONA), perfluoro-2-propoxypropan

167 anoic acid), ADONA (trade name for 4,8-dioxa-3H-perfluorononanoic acid), and 6:2 fluorotelomer carbox

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

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

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

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

172 3H)-ylidene)isobenzofuran-1(3H)-one, and (E)-3H,3'H-[1,1'-bibenzo[c] thiophenylidene]-3,3'-dione, are

173 imple heterocyclic stilbene derivatives, (E)-3H,3'H-[1,1'-biisobenzofuranylidene]-3,3'-dione, (E)-3-(

174 o evidence of CB2 in the brain using either [3H] CP-55,940 or [3H] A-836,339.

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

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

177 binding was increased up to seven times for 3H-PBR28 and up to two times for 3H-PK11195 in active le

178 n times for 3H-PBR28 and up to two times for 3H-PK11195 in active lesions and the centre of chronic a

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

180 mediates can enable access to functionalized 3H-indoles or benzazepinones.

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

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

183 9aR)-2-amino-6,7-dihydroxy-8-(hydroxymethyl)-3H,4H,5H,5aH,6H,7H,8H, 9aH,10H-pyrano[3,2-g]pteridin-4-o

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

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

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

187 inding, specific binding of the TSPO ligands 3H-PK11195 and 3H-PBR28 was determined in the same lesio

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

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

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

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

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

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

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

195 cross-coupling reaction of 1-acetyl-2-methyl-3H-pyrrolo[2,3-c]isoquinolin-5-yl triflate, easily prepa

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

197 A study of the ring-contraction of a model 3H-naphtho[2,1-b]pyran is described to elucidate and opt

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

199 PAM) 3a,4,5,9b-Tetrahydro-4-(1-naphthalenyl)-3H-cyclopentan[c]quinoline-8-sulfonamide (TQS) and the a

200 d by 3a,4,5,9b-tetrahydro-4-(1-naphthalenyl)-3H-cyclopentan[c]quinoline-8-sulfonamide were also linea

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

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

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

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

205 enta-1,3-dien-1-yl)-3,3-dimethyl-1-octadecyl-3H-indol-1-ium perchlorate.

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

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

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

209 annels for the formation of intermediates of 3H-pyrroles are considered.

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

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

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

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

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

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

221 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

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

223 in the brain using either [3H] CP-55,940 or [3H] A-836,339.

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

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

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

227 )-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta [g]quinazolin-6-yl]amino]benzoyl]-l-gamma-

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

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

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

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

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

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

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

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

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

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

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

239 The carbon analogue of EBS, namely, 2-phenyl-3H-isoindol-1-one, was included as a reference compound

240 45 and its cyclization to 3-(phenylethynyl)-3H-indazole 46b.

241 etic strategies to access novel photochromic 3H-naphtho[2,1-b]pyrans decorated with pyridyl units are

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

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

244 binding of two TSPO targeting radioligands (3H-PK11195 and 3H-PBR28) in tissue sections from 42 mult

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

246 uggesting that the hydrogen bonding in salts 3H(+)BF(4)(-)-6H(+)BF(4)(-) represents a previously unkn

247 retically estimated energies of IHB in salts 3H(+)BF(4)(-)-6H(+)BF(4)(-) vary between 7.0-10.7 and 6.

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

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

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

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

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

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

254 oquinolone, leads to variously 5-substituted 3H-pyrrolo[2,3-c]isoquinolines in excellent yields.

255 iles for the synthesis of alkoxy-substituted 3H-pyrrolo[3,4-b]quinolines using alcohols as nucleophil

256 The new pyridyl-substituted 3H-naphtho[2,1-b]pyrans display good photochromic proper

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

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

259 -7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl]pyridin-3-amine (28).

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 ,9bS)-4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (GAT107) and 3-(

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

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

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

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

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

269 ,5,6-tetramethylphenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide), consistent wit

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

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

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

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

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

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

276 ,7r)-3,5-dimethyladamantan-1-yl)-4-(3-thioxo-3H-1,2-dithiol-4-yl)-ben zamide (S-memantine) and examin

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

278 double salt cocrystal, [P(4444)](2)[Ad][Thy].3H(2)O.2HThy.

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

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

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

282 5,6-tetramethylphenyl)-3a,4,5,9b-te-trahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (2,3,5,6TMP-TQS)

283 5,6-tetramethylphenyl)-3a,4,5,9b-te-trahydro-3H-cyclopenta[c]quinoline-8-sulfonamide, originally repo

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

285 -2-yn-1-yloxy)methyl)-5-(3-(trifluoromethyl)-3H-diazirin-3-yl)phenol, AziPm-click (1)), for affinity-

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

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

288 beling with [(3)H]21-[4-(3-(trifluoromethyl)-3H-diazirine-3-yl)benzoxy]allopregnanolone ([(3)H]21-pTF

289 -2-O-[9-[[[2-[(125)I]iodo-4-(trifluoromethyl-3H-diazirin-3-yl)ben zyl]oxy]carbonyl]nonanoyl]-sn-glyce

290 -2-O-[9-[[[2-[(125)I]iodo-4-(trifluoromethyl-3H-diazirin-3-yl)ben zyl]oxy]carbonyl]nonanoyl]-sn-glyce

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

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

293 specific binding to LGR6 was confirmed using 3H-labeled MaR1.

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

295 We observe CB1-specific signal using [3H] CP-55,940 and [3H] SR141716A, though the latter exhi

296 of CB2 in prairie vole spleen tissue using [3H] CP-55,940.

297 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 ] (

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

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

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