ライフサイエンスコーパス: beta-carboline

1 phthol phosphoric acid to give an asymmetric beta-carboline.

2 omo-kynurenine and new-to-nature halogenated beta carbolines.

3 in AcOH at 200 degrees C leads to 1-hydroxy-beta-carbolines.

4 N2 is the directing group than N9 in C1-aryl-beta-carbolines.

5 s that allow specific positive modulation by beta-carbolines.

6 -e, which is known as the sulfur analogue of beta-carbolines.

7 llosteric regulatory site of benzodiazepines/beta-carbolines.

8 reaction of 1,2,3-trisubstituted tetrahydro-beta-carbolines.

9 o give 1-methyl-6-hydroxy-1,2,3,4-tetrahydro-beta-carboline (1), known to be formed at elevated level

10 We also show that 1-ethoxycarbonyl-beta-carboline (1-ECBC), a compound previously shown to

11 , and tetrahydro-beta-carbolines (tetrahydro-beta-carboline, 1-methyltetrahydro-beta-carboline and pi

12 1,2-dihydronaphthalene for the synthesis of beta-carboline-1-one derivatives at room temperature.

13 s a wide range of functionalities, affording beta-carboline-1-one derivatives in good yields.

14 boxamides with bicycloalkenes, to synthesize beta-carboline-1-one derivatives under mild conditions.

15 unctional groups and affords a good yield of beta-carboline-1-one derivatives.

16 Treatment of tetrahydro-beta-carboline-1-thione with 2-bromooct-7-enoyl chloride

17 xin or with the BDZ inverse agonist n-methyl-beta-carboline-3-carboxamide (beta-CC), and a seizure ra

18 ne receptor partial inverse agonist N-methyl-beta-carboline-3-carboxamide (FG-7142).

19 challenge with the anxiogenic drug, N-methyl-beta-carboline-3-carboxamide (FG-7142; a partial inverse

20 oxylate ethyl ester (beta-CCE), and N-methyl-beta-carboline-3-carboxamide (FG7142), but not including

21 creasing GABA(A) tone with FG-7142 (N-methyl-beta-carboline-3-carboxamide) improved DMTP at low but n

22 ors by 1 muM diazepam, 30 mM EtOH, and 1 muM beta-carboline-3-carboxy ethyl ester (but not 1 muM Zn(2

23 ts treated with methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (1 microgram) and simply re

24 seizure threshold, a beta carboline [methyl-beta-carboline-3-carboxylate (beta-CCM)]-induced model o

25 rse BZ agonist, methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM; 1 or 10 microM), fai

26 pidem (EC50 = 75 nM), and dimethoxyl-4-ethyl-beta-carboline-3-carboxylate (IC50 = 60 nM).

27 inity, whereas methyl-6, 7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate inhibited GABAR currents.

28 flumazenil, and methyl-6,7-dimethoxy-4 ethyl-beta-carboline-3-carboxylate were inactive.

29 cation zinc and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, and differences in enhance

30 s, CGS-9895 and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, had qualitatively similar

31 ce against PTZ, methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, picrotoxin, and amygdala-k

32 tors with the exception of dimethoxy-4-ethyl-beta-carboline-3-carboxylate, which behaved as a partial

33 beta-carboline methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate.

34 synthesis of 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC, 24,

35 Tetrahydro-beta-carboline-3-carboxylic acids were active against th

36 dimerization model studies on the tetrahydro beta-carboline (35).

37 ogical pH yields 1-methyl-1,2,3,4-tetrahydro-beta-carboline-5,6-dione (8) that reacts avidly with fre

38 8-S-glutathionyl-1-methyl-1,2,3,4-tetrahydro-beta-carboline-5,6-dione (9A and 9B).

39 hibition of Twist1 signaling with Harmine, a beta-carboline alkaloid, improved extracellular matrix d

40 lation approach has been developed utilizing beta-carboline alkaloids as the directing group.

41 A number of tremorogenic beta-carboline alkaloids have been found in common plant

42 Thus, comutagenicity of beta-carboline alkaloids with aromatic amines is shown t

43 d comutagen norharman along with two related beta-carboline alkaloids, carboline, and 5-carboline, wh

44 he synthesis of two biologically interesting beta-carboline alkaloids, ZK93423 and abecarnil (ZK11211

45 that structurally related 1,2,3,4-tetrahydro-beta-carbolines also bind at 5-HT(5A) receptors, and (d)

46 The versatility of beta-carboline amides as directing groups is evidenced b

47 We report here beta-carboline amides as intrinsic directing groups for

48 The highest content of the beta-carbolines among the traditional raw materials was

49 A reversal of the behavioural phenotype with beta-carboline, an anxiogenic inverse benzodiazepine rec

50 etrahydro-beta-carboline, 1-methyltetrahydro-beta-carboline and pinoline) were good OH radical scaven

51 C-H activation toward hydroxymethylation of beta-carbolines and isoquinolines as effective directing

52 re metabolic conversion products, especially beta-carbolines and isoquinolines, act as neurotoxins th

53 The reaction between substituted 1-formyl-9H-beta-carbolines and terminal alkynes in the presence of

54 droisoquinoline, 2-methyl-1,2,3,4-tetrahydro-beta-carboline, and 9-methyl-norharmon, suspected to ind

55 henanthridine, quinazoline, phthalazine, and beta-carboline, and electrophiles included acetyl chlori

56 These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate amon

57 enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidat

58 Maillard reaction could be used to generate beta-carboline antioxidants.

59 , 2,8-quinolinediols, and 1-methyl-3-carboxy-beta-carboline are described.

60 ng ChemGPS-NP, we found that the more active beta-carbolines are all more lipophilic and larger than

61 beta-Carbolines are bioactive pyridoindole alkaloids occ

62 Additionally, the identification of beta-carbolines as selective enhancers of GABA(A)Rs in O

63 which contain a tetrahydro-beta-carboline or beta-carboline backbone, respectively.

64 ovel class of substituted 7,8-dichloro-1-oxo-beta-carbolines based on the distinct structural feature

65 cal assays produced two promising compounds; beta-carboline-based (5c) and hybrid (13a).

66 d intramolecular cyclization of a tetrahydro-beta-carboline-based dipeptide has been developed to pre

67 Herein, a beta-carboline-based lead (KMA) was developed through li

68 A series of novel beta-carboline-based N-heterocyclic carbenes was prepare

69 Topical application of an anti-inflammatory beta-carboline compound, perlolyrine, was sufficient to

70 k not only demonstrates that biosynthesis of beta-carboline compounds is rich in unexpected chemistry

71 The beta-carboline compounds norharman and harman exhibit ne

72 inal bacterial species, produces a family of beta-carboline compounds with anti-inflammatory activity

73 Chicory coffee has proved to be a source of beta-carboline compounds.

74 unique N-acetylcysteine moiety linked to the beta-carboline core through a thioether bond.

75 Harmaline, a beta-carboline derivative thought to induce tremor by fa

76 Harmaline, a beta-carboline derivative, is known to produce tremor th

77 Library of biologically relevant new beta-carboline derivatives and isolation of its cyclorut

78 ophobic advanced reaction products including beta-carboline derivatives and Strecker aldehyde, alongs

79 The metal-free protocol provided tetrahydro-beta-carboline derivatives atom-efficiently under room t

80 ization of allenamides, providing tetrahydro-beta-carboline derivatives embedded with a C1-vinyl func

81 be a versatile precursor to different fused beta-carboline derivatives via simple synthetic transfor

82 ethod to determine blood levels of two major beta-carboline derivatives, harmane and harmine.

83 Various 6-methoxytetrahydro-beta-carboline derivatives, namely BEN (6-methoxy-1-phen

84 pharmacologically investigated 37 tetrahydro-beta-carboline derivatives.

85 e been achieved for the synthesis of dihydro-beta-carboline derivatives.

86 We also observed that beta-carbolines differentially enhance GABA responses in

87 These novel beta-carbolines display similar growth inhibitory activi

88 gative [3-carbomethoxy-4-ethyl-6,7-dimethoxy-beta-carboline (DMCM)] BZD ligands.

89 zepine agonist, methyl-6,7-dimethoxy-4-ethyl-beta-carboline (DMCM, 10(-2)M).

90 delta receptors is blocked by flumazenil and beta-carboline-ethyl ester (beta-CCE).

91 Here, we show that harmol, a member of the beta-carbolines family with anti-depressant properties,

92 The anxiogenic beta-carboline, FG 7142 (20 mg/kg) significantly increas

93 ctive tetrahydroisoquinolines and tetrahydro-beta-carbolines frequently with 99% ee's.

94 d direct pathway to access the benzene fused beta-carboline from 2-(1H-indol-3-ylsulfanyl)-phenylamin

95 through one-pot cascade synthesis of dihydro-beta-carbolines from alkyne and their conversion to vita

96 The synthesis of C1-functionalized beta-carbolines from N-Boc norharman is described.

97 hydroxy-beta-carbolines, whereas tetrahydro-beta-carbolines gave oxidative and degradation products.

98 ne lung extract allowed the isolation of the beta-carbolines harmane and harmalan as confirmed by ESM

99 We therefore propose that the beta-carbolines harmane and harmalan represent active co

100 The naturally occurring beta-carboline, harmane, has been implicated in various

101 identified several alkaloids, including the beta-carboline harmine and the isoquinoline berberine, t

102 2-benzyl-3-ethoxycarbonyl-1,2,3,4-tetrahydro-beta-carbolines has been synthesized via the Pictet-Spen

103 To accomplish this, we developed 3-propoxy-beta-carboline hydrochloride (3-PBC), a mixed agonist-an

104 thyl moiety to a carbazole (e.g., 34, 36) or beta-carboline (i.e., 37), result in reduced affinity an

105 -tryptophan and 1-carboxy-1-methyltetrahydro-beta-carboline in the active CDS extract.

106 tional groups and afford the diverse dihydro-beta-carbolines in good yield.

107 one-pot construction of N-fused benzimidazo-beta-carbolines in good yields.

108 Previous literature indicates that certain beta-carbolines including harmane modulate central monoa

109 ation of cis-1,2,3-trisubstituted tetrahydro-beta-carbolines into the trans isomers via a potential c

110 In contrast, beta-carboline inverse-agonism was unaltered in chimeric

111 Kitasetaline is one of the very few beta-carbolines isolated from bacteria.

112 selective formation of monohydroxymethylated beta-carboline/isoquinoline products exclusively.

113 he two subunits differ in sensitivity to the beta-carboline methyl-6,7-dimethoxy-4-ethyl-beta-carboli

114 dividual differences in seizure threshold, a beta carboline [methyl-beta-carboline-3-carboxylate (bet

115 Further, intra-DRN administration of a beta-carboline mimicked the effects of IS, because rats

116 r groove of double-stranded DNA and that its beta-carboline moiety plays a role in the binding throug

117 On the basis of IC50 and reaction rates (k), beta-carbolines (norharman and harman), and tetrahydro-b

118 The tetrahydro-beta-carboline of strictosidine aglycone is converted in

119 tet-Spengler reaction, which yields either a beta-carboline or a tetrahydroquinoline product from an

120 alkaloid harmine, which contain a tetrahydro-beta-carboline or beta-carboline backbone, respectively.

121 zolidin-4-ones expand the menu of tetrahydro-beta-carboline oxidation products.

122 led mechanism for enzymatic catalysis of the beta-carboline product is proposed from these data.

123 atalyzing the stereoselective synthesis of a beta-carboline product.

124 N dimerization of substituted carbazoles and beta-carbolines, providing entry into seldom explored ch

125 beta-Carbolines reacted with hydroxyl radicals (OH) affo

126 rresponding triazolo-fused isoquinolines and beta-carbolines, respectively, in good yields.

127 r the construction of the bridged tetrahydro-beta-carboline ring system 5 has been developed that fea

128 nase (KslA) that generate the characteristic beta-carboline ring system.

129 ler condensation that generates a tetrahydro-beta-carboline scaffold characterized by a 3S stereocent

130 e, allowing for rapid diversification of the beta-carboline scaffold in moderate to excellent yields.

131 strategy for the synthesis of benzene-fused beta-carboline scaffolds has been developed.

132 to the 3-(2-nitrovinyl)-indole and 1-hydroxy-beta-carboline series were identified to have single-dig

133 igned and synthesized approximately 50 novel beta-carbolines structurally related to harmine.

134 by mild stress can be mimicked by anxiogenic beta-carbolines such as FG7142.

135 )9 and the two isomers of 1,2,3,4-tetrahydro-beta-carboline (Tca)9 Modifications in the cyclic templa

136 lines (norharman and harman), and tetrahydro-beta-carbolines (tetrahydro-beta-carboline, 1-methyltetr

137 on is a valuable route to 1,2,3,4-tetrahydro-beta-carboline (THBC) and isoquinoline scaffolds found i

138 ence for the synthesis of 1,2,3,4-tetrahydro-beta-carbolines (THBCs) relying on a ruthenium hydride/B

139 s the first report on the synthesis of spiro-beta-carbolines through a multicatalytic cascade process

140 agents were designed as hybrid molecules of beta-carboline (topoisomerase inhibition moiety) and bis

141 for both laboratory and clinical studies of beta-carboline toxicities.

142 Substituted and 1,1-disubstituted tetrahydro-beta-carbolines undergo sodium periodate oxidative ring

143 subjected to the action of high temperature, beta-carboline was not detected.

144 Synthesis of substituted beta-carbolines was accomplished by utilizing the cataly

145 l group tolerance for C1-phenyl/thienyl/PAHs-beta-carbolines was demonstrated.

146 od to prepare 1-substituted N-Boc-tetrahydro-beta-carbolines was developed by lithiation followed by

147 s of 1-phenyl-substituted 1,2,3,4-tetrahydro-beta-carbolines was investigated via a Hammett study.

148 These and other related beta-carbolines were also examined in five recombinant G

149 totoxicity properties of 6-methoxytetrahydro-beta-carbolines were demonstrated for the first time.

150 on of the 3-amino ligands 40 and 41, all the beta-carbolines were found to exhibit high binding affin

151 beta-Carbolines were scavengers of OH in the three assay

152 ith hydroxyl radicals (OH) affording hydroxy-beta-carbolines, whereas tetrahydro-beta-carbolines gave

153 The latter undergoes rearrangement to a beta-carboline, which upon brominative oxidation undergo

154 n of 1,2,3-trisubstituted 1,2,3,4-tetrahydro-beta-carbolines, while the olefinic mechanism had been r

155 for the formylation/acylation of indoles and beta-carbolines with (NH(4))(2)S(2)O(8) via direct decar

156 esis of various 1,4-disubstituted tetrahydro-beta-carbolines with excellent stereoselectivity (de, ee

157 to develop a suite of 10 bio-inspired 1-aryl-beta-carbolines with varying DeltaG(rot), from which a s

158 rnish both cis- and trans-1,2,3,4-tetrahydro-beta-carbolines, with the trans isomer predominating.